MedWorm.com provides a medical RSS filtering service. Over 6000 RSS medical sources are combined and output via different filters. This feed contains the latest items from the 'Arzneimittel-Forschung' source. Wed, 08 Feb 2012 14:04:00 +0100 http://www.medworm.com/index.php?rid=5662870&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22297684%26dopt%3DAbstract In conclusion, the validation results showed that this method was sensitive, economical and less toxic and it can successfully fulfill the requirement of clinical pharmacokinetic study of domperidone oral preparation in Chinese healthy volunteers. PMID: 22297684 [PubMed - as supplied by publisher] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5662870 Wed, 01 Feb 2012 05:00:00 +0100 5662870 http://www.medworm.com/index.php?rid=5662871&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22290114%26dopt%3DAbstract In conclusion, the proposed model may prospectively guide the dosing strategies and would greatly aid the development of novel compounds in this class. PMID: 22290114 [PubMed - as supplied by publisher] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5662871 Mon, 30 Jan 2012 05:00:00 +0100 5662871 http://www.medworm.com/index.php?rid=5643824&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22286975%26dopt%3DAbstract Authors: Li DL, Dong CY, Gao Y Abstract A simple, rapid, selective and sensitive HPLC-UV method was developed and validated for the determination of swainsonine (SWSN) in rat plasma. The analyte was extracted from rat plasma with methanol as the extraction solvent. The LC separation was performed on a Diamonsil® C18 (250×4.6 mm, 5 µm) analytical column with a mobile phase consisting of acetonitrile-potassium dihydrogen phosphate (25 mmol/l, pH=7.5) at a flow rate of 1.0 ml/min. There was a good linearity over the range of 10-500 ng/ml (r=0.9995) with a weighted (1/C2) least square method. The lower limit of quantification was proved to be 10 ng/ml. The accuracy was within 4.8% in terms of relative error and the intra- and inter-day precisions were less than 9.0% in t... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5643824 Fri, 27 Jan 2012 05:00:00 +0100 5643824 http://www.medworm.com/index.php?rid=5643823&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22286976%26dopt%3DAbstract In this study, novel condensed 1,4-dihydropyridines bearing cyclopentanone (1-21) or tetrahydrothiophene-1,1-dioxide ring (22-42) with various ester substituents were synthesized via a modified Hantzsch reaction and their calcium channel modulator activities were investigated on isolated rat ileum and rat thoracic aorta. The introduction of a cyclopentanone ring fused to the 1,4-dihydropyridine nucleus and methyl, ethyl and allyl moieties to the ester group led to more active calcium modulators. PMID: 22286976 [PubMed - as supplied by publisher] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5643823 Fri, 27 Jan 2012 05:00:00 +0100 5643823 http://www.medworm.com/index.php?rid=5643822&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22286977%26dopt%3DAbstract Authors: Piao FY, Peng B, Zhang WB, Zhang W, Han RB Abstract A novel series of 9-alkoxy-6,7-dihydro-5H-benzo[c][1,2,4]triazolo[4,3-a]azepine derivatives was synthesized and screened for anticonvulsant activity by the maximal electroshock (MES) test and the subcutaneous pentylenetetrazol (scPTZ) test. Neurotoxic effects were also determined by the rotarod neurotoxicity test. The results revealed that all of the compounds exhibited anticonvulsant activity, Compound 5d was found to possess the most potential anticonvulsant activity in the anti-MES potency test; it had a median effective dose (ED50) of 12.3 mg/kg, a median toxicity dose (TD50) of 73.5 mg/kg, and a protective index (PI) of 6.0, which is slightly lower than the PI of the prototype drug carbamazepine (ED50=8.8, PI=8.1... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5643822 Fri, 27 Jan 2012 05:00:00 +0100 5643822 http://www.medworm.com/index.php?rid=5643821&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22286978%26dopt%3DAbstract Authors: Chen J, Jiang B, Lou H, Yu L, Ruan Z Abstract An open-label, single-dose, randomized, crossover study was carried out in 20 Chinese healthy male subjects to compare the pharmacokinetics of 2 cefaclor (CAS 53994-73-3) formulations after administration of a single 250 mg dose of each drug with a 1-week wash-out period. Blood samples were collected before and with 6 h after drug administration. Plasma concentrations were determined by high-performance liquid chromatography (HPLC) with UV detector. 2 formulations were evaluated using the following pharmacokinetic parameters: AUC0-t, Cmax and tmax was analyzed nonparametrically. The 90% confidence interval (CI) of the ratios (teat/reference) of log-transformed AUC0-t and Cmax fell within the bioequivalence acceptance range ... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5643821 Fri, 27 Jan 2012 05:00:00 +0100 5643821 http://www.medworm.com/index.php?rid=5643827&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22278629%26dopt%3DAbstract In this study, Aβ25-35 treatment is found to increase GSK-3β activity and pretreatment with puerarin preventesAβ-induced activation of GSK-3β based on Western blot analysis. In addition, puerarin is shown to activate protein kinase B (PKB)/Akt, an important upstream kinase of GSK-3β, possibly promoting subsequent GSK-3β inhibition. Our data suggest that puerarin attenuates cell death induced by Aβ25-35 via various mechanisms, which might be beneficial for the treatment of Alzheimer's disease. PMID: 22278629 [PubMed - as supplied by publisher] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5643827 Wed, 25 Jan 2012 05:00:00 +0100 5643827 http://www.medworm.com/index.php?rid=5643826&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22278630%26dopt%3DAbstract Authors: Li HL, He JC, Bai M, Song QY, Feng EF, Rao GX, Xu GL Abstract An LC-MS/MS method was developed for the quantification of swertiamarin (CAS 17388-39-5) in rat plasma and tissues using gentiopicroside as the internal standard (IS). Swertiamarin and an IS were extracted from plasma and tissues by a simple solid-phase extraction (SPE) procedure. Separation was achieved on a Phenomenex kinetex-C18 column (100 mm×2.1 mm, 2.6 µm) with an isocratic mobile phase consisting of methanol and water (22:78, v/v) with 0.1% acetic acid at a flow rate of 0.2 mL/min. The analyte and IS were detected by negative ion electrospray ionisation in multiple-reaction monitoring mode while monitoring the transitions of m/z 433 [M + CH3COO] - →179 and m/z 415 [M + CH3COO] -�... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5643826 Wed, 25 Jan 2012 05:00:00 +0100 5643826 http://www.medworm.com/index.php?rid=5643825&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22278631%26dopt%3DAbstract Authors: Agarwal S, Das A, Ghosh D, Sarkar AK, Chattaraj TK, Pal TK Abstract The pharmacokinetics of teriflunomide [CAS No. 163451-81-8], the metabolite of leflunomide [CAS No. 75706-12-6] has been evaluated in adult human volunteers after oral administration of tablet formulation. However, no published data is available regarding the bioavailability of this in the Indian population. In light of the above, a study was designed to carry out a bioequivalence study of 2 preparations of leflunomide 20 mg in healthy Indian male volunteers.24 healthy male volunteers (age, 25±4.1 years; weight, 57.58±7.01 kg) were enrolled in this study. Each subject received a test and reference formulation in a single dose, fasting 2 period, 2 way crossover study with a wash out period of 4 weeks.... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5643825 Wed, 25 Jan 2012 05:00:00 +0100 5643825 http://www.medworm.com/index.php?rid=5626106&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22270843%26dopt%3DAbstract Authors: El-Said MS, El-Gazzar MG, Al-Dosari MS, Ghorab MM Abstract Based on the reported anticancer activity of 2-pyridone, a new series of 6-amino-5-cyano-1-(3-ethylphenyl)-2-oxo-4-substituted-1,2-dihydropyridine-3-carbo-nitriles 4a-p were synthesized and tested for in-vitro anticancer activity against Ehrlich Ascites Carcinoma (EAC) cell line and liver human tumor cell line (HEPG2). Radiosensitizing activity was also evaluated. The starting material 2-cyano-N-(3-ethylphenyl)-acetamide 3 was obtained via reaction of 3-ethyl aniline 1 with ethyl cyanoacetate under condition of fusion. Upon treatment of compound 3 with aromatic aldehyde and malononitrile in the presence of catalytic amount of piperidine yielded the corresponding 1,2-dihydropyridine derivative 4a-p. Also chromenes 5... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5626106 Mon, 23 Jan 2012 05:00:00 +0100 5626106 http://www.medworm.com/index.php?rid=5626105&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22270844%26dopt%3DAbstract This study identifying naringin in several organs including lung and trachea may explain its effects as antitussive. PMID: 22270844 [PubMed - as supplied by publisher] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5626105 Mon, 23 Jan 2012 05:00:00 +0100 5626105 http://www.medworm.com/index.php?rid=5626104&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22270845%26dopt%3DAbstract This study was designed to investigate the preparation, in vitro release, in vivo pharmacokinetics and tissue distribution of a PTX-loaded microspheres system. Microspheres are characterized according to drug loading, size and shape. With a dynamic light scattering sizer and a transmission electron microscopy, it is shown that the PTX-loaded microspheres had a mean size of approximately 10.24 µm with narrow size distribution and a spherical shape. The in vitro release profiles indicate that the release of PTX from the microspheres exhibit a sustained release behavior. A similar phenomenon is observed in a pharmacokinetic study in rats, in which AUC of the microspheres formulation were 3.7-fold higher than that of PTX injection. The biodistribution study in mice showed that the PTX-loade... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5626104 Mon, 23 Jan 2012 05:00:00 +0100 5626104 http://www.medworm.com/index.php?rid=5515766&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22164962%26dopt%3DAbstract Authors: Bienert A, Wiczling P, Zaba C, Zaba Z, Wolc A, Marciniak R, Grześkowiak E, Kusza K Abstract The aim of the study was to examine population pharmacokinetics (PK) and pharmacodynamics (PD) of propofol (CAS 2078-54-8) during total intravenous anesthesia monitored by spectral frequency index (SFx). Twenty-eight patients of ASA physical status I-III (ASA: American Society of Anesthesiologists) scheduled for laparoscopic cholecystectomy were included. In group I an anesthesia was induced with a bolus of propofol (2 mg/kg) and remifentanil (CAS 132875-61-7) (1.0 microg/kg), followed by a continuous infusion of remifentanil. In group II, an alfentanil (CAS 71195-58-9) (10 microg/kg) bolus dose was followed by a continuous infusion of alfentanil. The general anesthetic technique i... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5515766 Mon, 19 Dec 2011 07:30:02 +0100 5515766 http://www.medworm.com/index.php?rid=5515765&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22164963%26dopt%3DAbstract Authors: Toblli JE, Cao G, Oliveri L, Angerosa M Abstract The physicochemical characteristics of intravenous iron complexes affect the extent of weakly-bound iron and thus the degree of oxidative stress. The new preparation iron isomaltoside 1000 (IIM) was compared to iron sucrose (IS) and a control group in terms of biochemistry, oxidative stress, inflammatory markers and iron deposition in the liver, heart and kidneys of healthy rats. Renal function was significantly impaired in the IIM group versus both IS and controls. Liver enzymes were also significantly higher in IIM-treated animals versus the other groups, indicative of hepatic injury. Systolic blood pressure was significantly lower following IIM administration compared to IS or control animals. Oxidative stress in the live... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5515765 Mon, 19 Dec 2011 07:30:02 +0100 5515765 http://www.medworm.com/index.php?rid=5515764&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22164964%26dopt%3DAbstract Authors: Basmenji S, Valizadeh H, Zakeri-Milani P Abstract The aim of this study was the comparison of in vitro dissolution and in vivo bioavailability of two different brands of diclofenac sodium (CAS 15307-86-5) enteric coated tablets in healthy male Iranian volunteers in a single-dose, randomized, open-label, single blind study, which was conducted according to a crossover design in healthy volunteers. A washout interval of two weeks was selected between administrations to each subject in this study. Serial venous blood samples over 10 h after each administration to measure diclofenac sodium concentration in serum were obtained, and placed into tubes containing sodium heparin. Then the plasma was separated and kept frozen at -20 degrees C for subsequent analysis with a modified ... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5515764 Mon, 19 Dec 2011 07:30:02 +0100 5515764 http://www.medworm.com/index.php?rid=5515763&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22164965%26dopt%3DAbstract Authors: Xue M, Jiang ZZ, Wu T, Yan M, Liu JP, Mu XM, Su YW, Zhang LY Abstract The protective effects of tripterygium glycoside-loaded solid lipid nanoparticles (TG-SLNs) on male reproductive toxicity were investigated in rats. Thirty-six male Sprague-Dawley rats were randomly divided into three groups of 12: control group, tripterygium glycoside (TG) group, and TG-SLN group. After the animals had been orally administered with the substances for 28 consecutive days, their sperm count and sperm motility, organ coefficients, serum testosterone levels, testicular ultrastructure, and reproductive ability were observed. The results showed that the sperm motility rate in the TG group was only 3%, whereas the rates in the TG-SLN and control groups were 33% and 71%, respectively. Compared ... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5515763 Mon, 19 Dec 2011 07:30:02 +0100 5515763 http://www.medworm.com/index.php?rid=5515762&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22164966%26dopt%3DAbstract Authors: Jagani HV, Josyula VR, Hariharapura RC, Palanimuthu VR, Gang SS Abstract The purpose of this research work was to prepare poly(d,l-lactide-co-glycolide) (PLGA) nanoparticles for delivery of siRNA (small interfering RNA) for silencing anti-apoptotic Bcl-2 gene in cancerous cells by using the double emulsion solvent diffusion (DESE) method. Overexpression of Bcl-2 is often seen in a wide variety of human cancers. This prevents the induction of programmed cell death (i.e., apoptosis) in cancerous cells. It is also reported that over-expression of Bcl-2 contributes to resistance in chemotherapy and inhibits the apoptosis induced by chemotherapeutic agents. Agents antagonizing the anti-apoptotic Bcl-2 protein have been shown to restore normal apoptotic processes in cancer cells... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5515762 Mon, 19 Dec 2011 07:30:02 +0100 5515762 http://www.medworm.com/index.php?rid=5515761&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22164967%26dopt%3DAbstract Authors: Feng Z, Zou Q, Tan X, Che W, Zhang Z Abstract A simple, rapid, and specific high-performance liquid chromatograph coupled with a tandem mass spectrometry method has been developed and validated for the determination of fenticonazole (CAS 72479-26-6) enantiomers in rat plasma. Simple protein precipitation by acetonitrile was utilized for extracting analytes from the plasma samples. Chromatography separation was performed on a C18 analytical column (150 mm x 2.0 mm, 5 microm) with a mobile phase consisting of methanol-10 mM aqueous ammonium acetate (adjusted to pH 3.5 with acetic acid) (90:10, v/v) at a flow rate of 0.2 ml/min. Detection was carried out on a triple quadrupole mass spectrometer equipped with electrospray ionization (ESI) source, and operated in multiple-react... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5515761 Mon, 19 Dec 2011 07:30:02 +0100 5515761 http://www.medworm.com/index.php?rid=5515760&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22164968%26dopt%3DAbstract Authors: Sultana TA, Islam MS, Bhuiyan NH, Shohag MH, Ahmed MU, Naznin SR, Al Maruf A, Huq SM, Hasnat A Abstract Azithromycin (AZT; CAS 83905-01-5) is an efficient antibiotic and is widely prescribed in Bangladesh. The taste of uncoated AZT suspension is bitter. Although several taste masked oral suspensions of AZT are available in Bangladesh, information regarding the bioavailability of these formulations in Bangladeshi population is unavailable. The purpose of this study was to compare the relative bioavailability and other pharmacokinetic properties of two oral formulation of AZT (200 mg/5 ml) suspensions, the uncoated reference product and coated test product (Tridosil 200 mg/5 ml) and to evaluate whether these formulations meet the FDA criteria to assume bioequivalence in Bang... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5515760 Mon, 19 Dec 2011 07:30:02 +0100 5515760 http://www.medworm.com/index.php?rid=5363362&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22029223%26dopt%3DAbstract Authors: Cánovas M, Torres F, Domenech G, Cebrecos J, Pelagio P, Martínez G, Polonio F, Cabré F Abstract One bioequivalence study was carried out in healthy volunteers in order to compare the rate and extent of absorption of two oral formulations of quetiapine fumarate (CAS 111974-72-2) 25 mg film-coated tablet. Thirty subjects were administered quetiapine fumarate film-coated tablet of test and reference formulation in an open-label, randomised, fasting, two-period, two-sequence, crossover study. Blood samples were taken before and within 48 h after drug administration. Plasma concentrations were determined by LC/MS/MS. Log-transformed AUC and Cmax values were tested for bioequivalence based on the ratios of the geometric means (test/reference). Tmax was analysed nonparametrica... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5363362 Wed, 02 Nov 2011 01:40:04 +0100 5363362 http://www.medworm.com/index.php?rid=5363361&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22029224%26dopt%3DAbstract Authors: Huang M, Tian Y, Zhang Z, Zhang H, Lin H Abstract A rapid, sensitive and reliable high performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method was developed and validated for the determination of propiverine hydrochloride (CAS 54556-98-8) in human plasma using cetirizine di-hydrochloride as internal standard (IS, CAS 8388-51-0). Following liquid-liquid extraction with ethyl acetate, the separation was performed on a reverse phase C18 column with a mobile phase consisted of methanol-ammonium acetate (pH 4.0; 10 mM) (70:30, v/v). The detection was performed by a triple-quadrupole mass spectrometer in the positive ion and multiple reaction monitoring (MRM) mode, m/z 368.3 --> 116.1 for propiverine and m/z 389.2 --> 201.0 for the IS. The calibratio... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5363361 Wed, 02 Nov 2011 01:40:04 +0100 5363361 http://www.medworm.com/index.php?rid=5363360&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22029225%26dopt%3DAbstract Authors: Cai W, Wang ZT, Li J, Hu JJ, Zhong J Abstract A bioequivalence study of two esomeprazole (CAS 119141-88-7) enteric-coated formulations was carried out in 20 healthy Chinese volunteers according to a single dose, two-sequence, crossover randomized design. The two formulations were administered in two treatment days, separated by a washout period of 7 days. Blood samples were collected at specified time intervals over 10 h post-dosing. Plasma samples were separated and assayed for esomeprazole using a selective and sensitive HPLC method with UV detection. The pharmacokinetic parameters AUC(0-12h), AUCmax, Cmax, tmax, t1/2 and MRT were determined from the plasma concentration-time profile of both formulations. ANOVA and two one-sided t-test procedures showed no significant di... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5363360 Wed, 02 Nov 2011 01:40:04 +0100 5363360 http://www.medworm.com/index.php?rid=5363359&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22029226%26dopt%3DAbstract Authors: Venkatesh S, Durga KD, Padmavathi Y, Reddy BM, Mullangi R Abstract Piperine (CAS 94-62-2), an alkaloid obtained from Piper nigrum and P. longum, is a known inhibitor of various enzymes (CYP isozymes) responsible for biotransformation of drugs. By inhibiting the metabolism of drugs, piperine improves the bioavailability of drugs. In the present study piperine (10 mg/kg) significantly increased the dose-dependent antinociceptive activity of ibuprofen evaluated by both acetic acid writhing and formalin test, when it was administered with ibuprofen. Ibuprofen plasma concentration was also increased when it was administered with piperine. The synergistic antinociception activity of ibuprofen when administered with piperine can be attributed to increased plasma concentration of ... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5363359 Wed, 02 Nov 2011 01:40:04 +0100 5363359 http://www.medworm.com/index.php?rid=5363358&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22029227%26dopt%3DAbstract Authors: Ruikar AD, Misar AV, Jadhav RB, Rojatkar SR, Mujumdar AM, Puranik VG, Deshpande NR Abstract The present study was carried out to investigate the anti-inflammatory activities of bioactive secondary metabolites of Artemisia pallens Wall, an aromatic herb from family Asteraceae. The results provide evidence for the topical anti-inflammatory properties of Artemisia pallens Wall. The compounds were isolated from the acetone extract of the plant material. The isolates were tested on Swiss albino mice using 12-O-tetradecanoyl phorbol-13-acetate (TPA) induced ear edema. One of the molecules from the extract indicated potent anti-inflammatory activity equivalent to indometacin (CAS 53-86-1). Elucidation of the molecular structures by single crystal x-ray diffraction studies reveale... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5363358 Wed, 02 Nov 2011 01:40:04 +0100 5363358 http://www.medworm.com/index.php?rid=5363357&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22029228%26dopt%3DAbstract The objectives of this study were to investigate whether chlormadinone acetate (CMA, Prostal, CAS 302-22-7) more markedly decreased ventral prostate and seminal vesicle weights and exerted more beneficial effects on intraprostatic androgen levels than dutasteride (DUT, CAS 164656-23-9) in rats. Dose-dependent inhibiting effects on prostate and seminal vesicle enlargement were observed after the 14-day administration of CMA (30, 100 mg/kg/day) and DUT (0.3, 1 mg/kg/day). The prostate atrophy rates calculated as the percentages relative to the vehicle-treated group were 50.5 and 67.9% with 30 and 100 mg/kg CMA and 34.9 and 37.0% with 0.3 and 1 mg/kg DUT, respectively, and the atrophying effect of CMA was significantly greater than that of DUT (p < 0.05). The results of 7-day administratio... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5363357 Wed, 02 Nov 2011 01:40:04 +0100 5363357 http://www.medworm.com/index.php?rid=5363356&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22029229%26dopt%3DAbstract Authors: Bashandy MS, Al-Said MS, Al-Qasoumi SI, Ghorab MM Abstract This paper describes the synthesis of some novel sulfones having biologically active hydrazides (4-9, 22, 23, 26 and 27), hydrazonoyl cyanide (24), 1,2-dihydropyridines (16-21), chromene (28) and benzochromene (29) moieties starting with 1-[4-(piperidin-1-ylsulfonyl)phenyl]-ethanone 1. The structures of the the newly synthesized compounds were confirmed by elemental analysis, IR, 1H NMR and 13C NMR. All the newly synthesized compounds were evaluated for their in vitro anticancer activity against breast cancer cell line (MCF7). PMID: 22029229 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5363356 Wed, 02 Nov 2011 01:40:04 +0100 5363356 http://www.medworm.com/index.php?rid=5363355&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22029230%26dopt%3DAbstract Authors: Al-Said MS, Bashandy MS, Ghorab MM Abstract The present paper describes the synthesis of some novel 2-amino-4-substituted aryl-5-oxo-1-(3,4,5-trimethoxy)-1,4,5,6,7,8-hexahydroquinoline-3-carbo-nitriles 6a-s starting with 3-(3,4,5-trimethoxyanilino)cyclohex-2-enone 3. All the newly synthesized compounds were evaluated for their in vitro antitumor activity. Compounds 6j, 6p and 6 q showed higher activity with IC50 values 10, 10, 15 microg/mL, respectively, when compared with doxorubicin as a reference drug (IC50 value 37.5 microg/mL). PMID: 22029230 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5363355 Wed, 02 Nov 2011 01:40:04 +0100 5363355 http://www.medworm.com/index.php?rid=5363354&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22029231%26dopt%3DAbstract CONCLUSIONS: Considering the high correlation of rat Peff values with those of human reported values, it can be concluded that the developed in-house model is reliable and can be used preliminarily, to predict human permeability and fraction dose absorbed of any test compound. From predicted results, 99/411 was found to have high permeability and possibly complete absorption in human. PMID: 22029231 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5363354 Wed, 02 Nov 2011 01:40:04 +0100 5363354 http://www.medworm.com/index.php?rid=5363353&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22029232%26dopt%3DAbstract Authors: Sanki UK, Mandal BK, Chandrakala V Abstract The comparative pharmacokinetic (PK) study of two brands of clindamycin hydrochloride (CAS 21462-39-5) was carried out on 32 healthy Indian subjects in an open label randomized, two way crossover, two period, two sequence, two treatment trial with a minimum washout period of 7 days. Plasma samples were collected at 10 min interval for the 1st hour, at 1 h interval for the next 6 h, at 2 h interval for next 12 h and finally at the 24th hour (pre-dose as baseline value) after drug administration. The concentrations of clindamycin in plasma were determined using high performance liquid chromatography (HPLC) technique with UV detector [lower limit of quantitation (LLOQ) 0.05 microg x mL(-1)). All PK parameters were calculated from da... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5363353 Wed, 02 Nov 2011 01:40:04 +0100 5363353 http://www.medworm.com/index.php?rid=5267062&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21950146%26dopt%3DAbstract Authors: Deng Y, Wang Q, Liu X, Wang Y, Ding Z Abstract Tyrosol galactoside (TG) is a new candidate anti-fatigue agent under development. In order to have a good understanding of its pharmacokinetic characters, the paper describes the dose-dependent pharmacokinetics of TG in rats after oral and intravenous administration. TG was rapidly absorbed after oral administration and cleared with first-order rate, for the plasma half-life was independent of dose. C(max) and AUC(0-infinity) after both intravenous and oral dosing were all linearly correlated with the dose, as the regression correlation coefficient (R) was 0.998, 0.989 and 0.994 for AUC(0-infinity) (i.v., P < 0.01) AUC(0-infinity) (i.g., P < 0.01) and C(max) (i. g., P < 0.01), respectively. However, these parameters i... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5267062 Fri, 30 Sep 2011 06:05:02 +0100 5267062 http://www.medworm.com/index.php?rid=5267061&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21950147%26dopt%3DAbstract Authors: Zakeri-Milani P, Nemati M, Ghanbarzadeh S, Hamishehkar H, Valizadeh H Abstract The purpose of this study was to compare the pharmacokinetics and bioavailability of two commercial brands of delayed release divalproex sodium (CAS 76584-70-8) tablets in healthy male Iranian volunteers in fasted state. Each single-dose, randomized, open-label, blind study was conducted according to a crossover design in subjects. A washout interval of 14 days separated the doses in each study. Serial venous blood samples were obtained over 24 h after each administration to measure drug in serum, and placed into tubes containing sodium heparin. Then the separated plasma was kept frozen at -20 degrees C for subsequent analysis. The plasma concentrations of drug were analyzed by a validated sensi... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5267061 Fri, 30 Sep 2011 06:05:02 +0100 5267061 http://www.medworm.com/index.php?rid=5267060&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21950148%26dopt%3DAbstract The objective of this study was to investigate the pharmacokinetics of felodipine (CAS 72509-76-3) in healthy male Taiwanese subjects. This is a retrospective review of five felodipine pharmacokinetic studies completed in Taiwan. A total of 100 evaluable healthy Taiwanese males were enrolled in these studies. The subjects received 5 mg (n = 80) or 10 mg (n = 20) of Plendil (felodipine extended-release tablets; felodipine ER) once daily for 6 days. The mean +/- SD t(max,ss,) CG(max,ss) and AUG(tau) of dose normalized to 10 mg felodipine was 3.32 +/- 1.33 h, 13.12 +/- 5.34 nmol/L and 136.33 +/- 63.18 nmol x h/L, respectively. By using Kolmogorov-Smirnov's test and probit plots, the results indicated that the frequency distribution of AUC/dose, C(min)/dose and CL/F was bimodal. Compared to da... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5267060 Fri, 30 Sep 2011 06:05:02 +0100 5267060 http://www.medworm.com/index.php?rid=5267059&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21950149%26dopt%3DAbstract Authors: Chhabria MT, Suhagia BN, Brahmkshatriya PS, Raval PM Abstract Hyperlipidemia is considered one of the key factors for cardiovascular diseases. Based on earlier work on a series of 5-alkyl-4-aryl-3-mercapto-(4H)-1,2,4-triazoles, for further lead modification, a series of 4-(substituted)amino-5-substituted-3-mercapto-(4H)-1,2,4-triazoles was designed. Target compounds were synthesized by the well known Hoggarth synthesis of substituted 1,2,4-triazoles. Synthesized compounds were screened for lipid lowering activity using the "Poloxamer 407 induced hyperlipidemia in rats" model at a dose of 100 mg/kg p.o. Compounds were found to alter serum lipid levels significantly. Most of the compounds significantly reduced serum cholesterol and triglyceride levels. Some of the compounds ... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5267059 Fri, 30 Sep 2011 06:05:02 +0100 5267059 http://www.medworm.com/index.php?rid=5267058&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21950150%26dopt%3DAbstract Authors: Jinno F, Kakehi M, Takeuchi T, Tagawa Y, Kondo T, Asahi S Abstract The pharmacokinetics of TAK-242 (ethyl (6R)-6- [N-(2-chloro-4-fluorophenyl)sulfamoyl]cyclohex-1-ene-1-carboxylate, CAS 243984-11-4) and its metabolites were investigated in rats and dogs after intravenous (i.v.) dosing of TAK-242 using two types of radiolabeled TAK-242: [phenyl ring-U-14C]TAK-242 and [cyclohexene ring-U-14C]TAK-242. The phenyl ring moiety of TAK-242 yielded 2-chloro-4-fluoroaniline, M-I, and M-I was further acetylated and conjugated to form M-II and the glucuronide (M-I-G), respectively. M-I was also converted to M-III and M-IV by hydroxylation and subsequent sulfate conjugation. Meanwhile, the cyclohexene ring moiety of TAK-242 was metabolized to glutathione conjugate, M-SG, followed by fu... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5267058 Fri, 30 Sep 2011 06:05:02 +0100 5267058 http://www.medworm.com/index.php?rid=5267057&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21950151%26dopt%3DAbstract Authors: Seif S, Kazempour ZB, Pourmand MR, Shahverdi HR, Amanlou M, Bazl R, Nazari ZE, Shahverdi AR Abstract In the present research study, ciprofloxacin-coated zinc oxide nanoparticles were prepared using a precipitation method. The nature of interactions between zinc oxide nanoparticles and ciprofloxacin (CAS 85721-33-1) was studied by Fourier transform infrared spectroscopy. The results show that the carbonyl group in ciprofloxacin is actively involved in forming chemical--rather than physical--bonds with zinc oxide nanoparticles. Also the antibacterial activity of free zinc oxide nanoparticles and ciprofloxacin-coated zinc oxide nanoparticles have been evaluated against different clinical isolates of Staphylococcus aureus and Escherichia coli. The free zinc oxide nanoparticles... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5267057 Fri, 30 Sep 2011 06:05:02 +0100 5267057 http://www.medworm.com/index.php?rid=5267056&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21950152%26dopt%3DAbstract Authors: Foroutan SM, Zarghi A, Shafaati A, Movahed H, Khoddam A Abstract A rapid, sensitive and reproducible HPLC method was developed and validated for the analysis of adefovir (CAS 106941-25-7) in human plasma. The separation was achieved on a monolithic silica column (Chromolith Performance RP-18e, 100 x 4.6 mm) using acetonitrile-ammonium dihydrogen phosphate buffer (6:94, v/v), pH 5.2, as the mobile phase at a flow rate of 1.5 ml min(-1). The wavelength was set at 260 nm. The assay enables the measurement of adefovir for therapeutic drug monitoring with a minimum quantification limit of 1 ng ml(-1). The method involves a simple protein precipitation procedure. Analytical recovery was complete. The calibration curve was linear over the concentration range 1-40 ng ml(-1). The c... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5267056 Fri, 30 Sep 2011 06:05:02 +0100 5267056 http://www.medworm.com/index.php?rid=5267055&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21950153%26dopt%3DAbstract The objective of this study was to compare rate and extent of absorption and to assess the bioequivalence between a new pharmaceutical equivalent tablet formulation containing 500 mg of SAQ mesylate and the innovator film coated tablet formulation. A randomized, single-center, open-label, two-treatment, two-sequence, three-period, replicated crossover bioequivalence study in 40 healthy male subjects was conducted. All subjects received 100 mg ritonavir (CAS 155213-67-5) twice daily for a run-in period of 3 days before treatment. Dosing was separated by a wash-out period of 14 days. Blood samples were collected over 72 h and plasma levels of SAQ were determined by a validated HPLC/UV assay. The 90% confidence interval (CI) of the ratio of the geometric means for log-transformed C(max), AUC(... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5267055 Fri, 30 Sep 2011 06:05:02 +0100 5267055 http://www.medworm.com/index.php?rid=5221324&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21899203%26dopt%3DAbstract Authors: Piplani P, Rani A, Saihgal R, Sharma M Abstract The present paper describes the synthesis of a series of substituted 6-amino (1a-c) and 8-aminoquinoline derivatives (2b-c) and the evaluation of their ability to prevent the memory decline using a behavioural model, i.e. the elevated plus maze test. The effect of the candidate drugs on the activity of acetylcholinesterase was studied using the enzyme source from the mouse brain. The structures of the synthesized compounds were confirmed by UV, IR, 1H-NMR and elemental analysis. The 6-aminoquinoline derivative [6-(4-pyridyl)methylaminoquinoline] (1c) oxalate showed maximum % retention (50% at 5 mg/kg and 75% at 10 mg/kg) in the elevated plus maze test and maximum % inhibition (71% at 25 microM) of AChE on biochemical evaluati... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5221324 Thu, 15 Sep 2011 20:48:02 +0100 5221324 http://www.medworm.com/index.php?rid=5221323&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21899204%26dopt%3DAbstract Authors: Elhelby AA, Ayyad RR, Zayed MF Abstract In view of their expected anticonvulsant activity, some new derivatives of quinonxaline (V1-7) were designed and synthesized by condensation of different aromatic aldehydes with 2-(2-oxo-3-phenylquinoxalin-1(2H)-yl)acetohydrazide (IV). All synthesized compounds were isolated and confirmed by IR, 1H-NMR, MS, elemental analysis and then tested as anticonvulsant agents. Compound V3 and V1 showed the highest anticonvulsant effect with anticonvulsant potency relative to phenobarbital sodium of 0.8 and 0.75 whereas compound V5 exhibited the lowest relative potency of 0.09. The other compounds showed variable activity between these values as follows: V2 = 0.19, V4 = 0.41, V6 = 0.1 and V7 = 0.15. All compounds showed less activity than the r... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5221323 Thu, 15 Sep 2011 20:48:02 +0100 5221323 http://www.medworm.com/index.php?rid=5221322&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21899205%26dopt%3DAbstract Authors: Andreu GL, Maurmann N, Reolon GK, de Farias CB, Delgado R, Roesler R Abstract Mangiferin (1,3,6,7-tetrahydroxy-2-[3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl] -xanthen-9-one, CAS 4773-96-0), a naturally occurring glucosylxanthone, is widely distributed in higher plants and a constituent of folk medicine. In the present study the effect of systemic administration of mangiferin on behavioural outcomes of neurological function in normal rats was investigated. A single intraperitoneal injection of mangiferin (10, 50 and 100 mg/kg body weight) immediately post-training produced an impairment of long-term memory for aversive training and a reduced freezing in a dose independent manner, when given immediately post-training. The administration of mangiferin 6 h post-training did n... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5221322 Thu, 15 Sep 2011 20:48:02 +0100 5221322 http://www.medworm.com/index.php?rid=5221321&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21899206%26dopt%3DAbstract CONCLUSION: These results show that agents possessing positive or negative inotropic action significantly relaxed the isolated vein samples precontracted with phenylephrine. These responses point to a different mechanism of action underlying both calcium antagonist and agonist effects even though their action ultimately resulted in vasodilatation. PMID: 21899206 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5221321 Thu, 15 Sep 2011 20:48:02 +0100 5221321 http://www.medworm.com/index.php?rid=5221320&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21899207%26dopt%3DAbstract Authors: Chowdhury MM, Ullah MA, Iqbal N, Al Maruf A, Shohag MH, Harun S, Akter KA, Begum B, Latif AH, Hasnat A Abstract Trimetazidine (CAS 5011-34-7) is an effective and well-tolerated antianginal drug that possesses protective properties against ischemia-induced heart injury. The relative bioavailability and pharmacokinetic characteristics of two modified release formulations of 35 mg trimetazidine, one as the test product (Metacard MR) and one as the reference product, were compared in healthy Bangladeshi male volunteers. The randomized, two-way crossover study was conducted in 24 healthy male volunteers after administration of a single 35 mg dose of each modified release formulation after 12-h overnight fasting, with a washout period of two weeks. Blood samples were collected a... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5221320 Thu, 15 Sep 2011 20:48:02 +0100 5221320 http://www.medworm.com/index.php?rid=5221319&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21899208%26dopt%3DAbstract Authors: Toblli JE, Cao G, Oliveri L, Angerosa M Abstract Intravenous (i.v.) iron is associated with a risk of oxidative stress. The effects of ferumoxytol, a recently approved i.v. iron preparation, were compared with those of ferric carboxymaltose, low molecular weight iron dextran and iron sucrose in the liver, kidneys and heart of normal rats. In contrast to iron sucrose and ferric carboxymaltose, low molecular weight iron dextran and ferumoxytol caused renal and hepatic damage as demonstrated by proteinuria and increased liver enzyme levels. Higher levels of oxidative stress in these tissues were also indicated, by significantly higher levels of malondialdehyde, significantly increased antioxidant enzyme activities, and a significant reduction in the reduced to oxidized glutat... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5221319 Thu, 15 Sep 2011 20:48:02 +0100 5221319 http://www.medworm.com/index.php?rid=5221318&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21899209%26dopt%3DAbstract Authors: Tang W, Liu X, Qiu X, Yuan S, Wang J, Chen H Abstract A simple, sensitive and modified method was developed for determination of low dihydrocodeine (CAS 125-28-0) concentrations in human plasma by high performance-liquid chromatography (HPLC) with diode array detector. Measurement was performed on a Zorbax XDB-C18 analytical column together with a XDB-C18 precolumn at 40 degrees C after a simple one-step extraction. An isocratic mobile phase consisting of acetonitrile-0.1% trifluoroacetic acid (TFA)-water (12:40:48, v/v/v), was run at a flow rate of 1.0 mL/min. Good chromatographic separation was achieved in less than 6.2 min. This assay was linear over a concentration range of 2.50-100 ng/mL with a lower limit of quantification at 2.50 ng/mL. The intra- and inter-day prec... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5221318 Thu, 15 Sep 2011 20:48:02 +0100 5221318 http://www.medworm.com/index.php?rid=5221317&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21899210%26dopt%3DAbstract Authors: He C, Fan H, Tan J, Zou J, Zhu Y, Yang K, Hu Q Abstract The aim of this study was to evaluate the pharmacokinetic profiles of betamethasone (BOH, CAS 378-44-9) and betamethasone 17-monopropionate (B17P), the active metabolites of betamethasone phosphate (BSP) and betamethasone dipropionate (BDP), respectively, after administration of betamethasone i.m. (BSP 2 mg and BDP 5 mg). After ten healthy volunteers had received a single-dose intramuscular adminitration of betamethasone i.m., blood samples were collected pre-dose and for 336 h postdose. The plasma levels of B17P and BOH were measured by liquid chromatography-tandem mass spectrometry (LC-MS/ MS). When compared to BOH, B17P exhibited a longer time to maximum concentration (15.0 +/- 9.0 h vs. 2.8 +/- 1.7 h), a lower Cma... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5221317 Thu, 15 Sep 2011 20:48:02 +0100 5221317 http://www.medworm.com/index.php?rid=5221316&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21899211%26dopt%3DAbstract CONCLUSIONS: The Th1/Th2 ratio increased significantly after administration of suplatast tosilate, shifting to Th1 dominance. Therefore suplatast tosilate improves Th2 dominance and may inhibit subsequent progression of allergy over the long term. PMID: 21899211 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5221316 Thu, 15 Sep 2011 20:48:02 +0100 5221316 http://www.medworm.com/index.php?rid=5221315&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21899212%26dopt%3DAbstract Authors: Kushwaha HN, Gautam N, Singh SK Abstract A sensitive, selective and specific LC-MS/ MS assay for simultaneous quantification of compound 97/78 and its active in vivo metabolite 97/63, a novel 1,2,4-trioxane antimalarial, in human plasma has been developed and validated using alpha-arteether as internal standard (IS). Extraction from plasma involves a simple protein precipitation method. The analytes were chromatographed on a Columbus C18 column with guard by isocratic elution with acetonitrile:ammonium acetate buffer (10 mM, pH 4.0) (80:20 v/v) as mobile phase at a flow rate of 0.45 mL min(-1) and analyzed in multiple reaction-monitoring (MRM) positive ion mode. The chromatographic run time was 4.0 min. The weighted (1/x2) calibration curves were linear over a range of 1.5... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5221315 Thu, 15 Sep 2011 20:48:02 +0100 5221315 http://www.medworm.com/index.php?rid=5142608&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21827042%26dopt%3DAbstract Authors: Caliş U, Septioğlu E, Aytemir MD Abstract A number of novel 2-(1H-imidazole-1-yl)-1-aryl-substituted ethane-1-one N-substituted phenyl(thio)semicarbazones (1-14) were synthesized to test for their anticonvulsant activity against the two seizure models, maximal electroshock (MES) and subcutaneous pentylenetetrazol (scPTZ). Title compounds were prepared by the reaction of appropriate (thio)semicarbazides with ketones. Neurotoxicity was screened by the rotarod test. The structure of compounds was confirmed by elemental analysis results and the spectroscopic techniques such as IR, 1H-NMR, 13C-NMR, ESI-MS and HRMS. As a result of activity studies, when the thiosemicarbazone compounds were compared at different doses, 2-(1H-imidazole-1-yl)-1-(2-naphthyl)ethane-1-one N-(3-chlor... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5142608 Sat, 20 Aug 2011 10:02:03 +0100 5142608 http://www.medworm.com/index.php?rid=5142607&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21827043%26dopt%3DAbstract Authors: González-Esquivel DF, Castro N, Ramírez-Bermúdez J, Custodio V, Rojas-Tomé S, Castro-Román R, Jung-Cook H Abstract The aim of the present study was to determine the prescribing practice for clozapine (CAS 5786-21-0) as well as the plasma levels of clozapine and its main metabolite norclozapine (CAS 6104-71-8) in Mexican patients. A prospective study was performed in 69 in and out psychotic patients taking clozapine. Blood samples were taken at steady state. Plasma concentrations of clozapine and norclozapine were determined by HPLC. The results showed that the mean daily dose administered was 250 mg/d. Plasma levels showed a large interindividual variability. Mean plasma levels were 411.3 +/- 328.12 ng/mL, for clozapine and 172.0 +/- 129.9 ng/mL for norclozapine. When... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5142607 Sat, 20 Aug 2011 10:02:03 +0100 5142607 http://www.medworm.com/index.php?rid=5142606&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21827044%26dopt%3DAbstract Authors: Chae JW, Baek IH, Kang W, Kwon KI Abstract Nitric oxide (NO) is synthesized from L-arginine (Arg) by NO synthase (NOS), and asymmetric dimethylarginine (ADMA) and symmetric dimethylarginine (SDMA) are endogenous inhibitors of NO formation. Normal distribution values of Arg, ADMA, and SDMA are required to evaluate the effects of cardiovascular drugs on blood vessels, but insufficient normal reference values from rat and mouse plasma exist for new drug development and screening. To determine the means and variations in the basal endogenous materials concentration, Arg, ADMA, and SDMA in blank rat (n = 24) and mouse (n = 37) plasma samples were quantified using LC-MS/MS equipped with an electrospray ionization interface to generate positive mode ions. Accuracy and precision w... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5142606 Sat, 20 Aug 2011 10:02:03 +0100 5142606 http://www.medworm.com/index.php?rid=5142605&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21827045%26dopt%3DAbstract Authors: Huang Y, Zhao L, Bai Y, Liu P, Wang J, Xiang J Abstract A rapid and specific HPLC method has been developed and validated for the simultaneous determination of liensinine (CAS 2586-96-1), isoliensinine (CAS 6817-41-0) and neferine (CAS 2292-16-2) in rat plasma. The sample was prepared by a liquid-liquid extraction with diethyl ether and the recovery was above 80% from the plasma for the three compounds. Chromatographic separation was achieved with a Hypersil BDS C18 column (4.0 mm x 250 mm, particle size 5 microm). A mobile phase consisting of methanol: 0.2 M KH2PO4:0.2 M NaOH:triethylamine (71:17:12:0.002, v/v/v/v, pH 9.2-9.3) was slowly delivered at 0.8 ml/min in isocratic mode with a detection wavelength of 282 nm. The linearity of calibration curves were good (r > 0... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5142605 Sat, 20 Aug 2011 10:02:03 +0100 5142605 http://www.medworm.com/index.php?rid=5142604&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21827046%26dopt%3DAbstract This study shows that CP form I has better bioavailability in rats than CP form II. PMID: 21827046 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5142604 Sat, 20 Aug 2011 10:02:03 +0100 5142604 http://www.medworm.com/index.php?rid=5142603&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21827047%26dopt%3DAbstract Authors: N'Da DD, Breytenbach JC, Smith PJ, Lategan C Abstract New 4-aminoquinoline-derived esters containing the redox-active ferrocene group brought in by either ferrocenyformic or 4-ferrocenylbutanoic acids were synthesized and tested in vitro for their antiplasmodial activity. The results revealed that only esters derived from ferrocenylformic acid were active against both chloroquine (CQ)-resistant Dd2 and CQ-sensitive D10 strains of Plasmodium falciparum. However, none of these showed higher actvity than CQ against the sensitive strain. Ester 16, which possesses a butyl branch in the structure, was the most active of all. With an IC50 of 0.13 mM on the resistant strain, this ester possessed 2.5-fold higher activity than CQ (IC50 = 0.34 mM). All tested esters showed good selec... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5142603 Sat, 20 Aug 2011 10:02:03 +0100 5142603 http://www.medworm.com/index.php?rid=5142602&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21827048%26dopt%3DAbstract Authors: Kucukoglu K, Gul M, Atalay M, Mete E, Kazaz C, Hanninen O, Gul HI Abstract 1-Aryl-3-dimethylamino-1-propanone hydrochlorides type mono Mannich bases, D series, and corresponding hydrazone derivatives, K series, were synthesized and their cytotoxicity was tested against Jurkat cells (transformed human T-lymphocytes). The aryl part was changed as phenyl in D1 and K1, 4-methylphenyl in D2 and K2, 4-methoxyphenyl in D3 and K3, 4-hydroxyphenyl in D4 and K4, 4-chlorophenyl in D5 and K5, 3-methoxyphenyl in D6 and K6, 4-fluorophenyl in D7 and K7, 4-bromophenyl in D8 and K8, 3-hydroxyphenyl in D9 and K9, and 2-acetylthiophene in D10 and K10. Of the compounds synthesized, K2, K3, K5, K6, K7, K8, K9, and K10 are reported for the first time. Cytotoxic activities of the D and K series ... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5142602 Sat, 20 Aug 2011 10:02:03 +0100 5142602 http://www.medworm.com/index.php?rid=5067159&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21755809%26dopt%3DAbstract Authors: Bailie GR, Hörl WH, Verhoef JJ Spontaneously-reported rates of adverse events (AEs) of intravenous (i.v.) iron products have not been compared since 2007. AEs in Europe (Eur) and North America (NA) have never been compared. New products have been marketed and many changes in prescribing habits have occurred since then, and the effect on AEs reporting is unclear. It was hypothesized that changing practices for i.v. iron products has caused changes in the rates of serious AEs and large differences exist between Eur and NA. Rates of AEs for three i.v. iron preparations (iron sucrose [IS], ferric gluconate [FG] and high and low MW iron dextran [HMWID, LMWID]) were compared by product and continent from January 1, 2003 to June 30, 2009 for selected countries in Eur and NA, using t... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5067159 Wed, 27 Jul 2011 09:15:03 +0100 5067159 http://www.medworm.com/index.php?rid=5067158&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21755810%26dopt%3DAbstract Authors: Kim JK, Jee JP, Park JS, Kim HT, Kim CK A sensitive and selective reverse-phase liquid chromatography electrospray ionization mass spectrometry (LC-ESI-MS) method was developed and validated to quantify pseudoephedrine (CAS 90-82-4) in human plasma. Phenacetin was used as the internal standard (I.S.). Sample preparation was performed with a deproteinization step using acetonitrile. Pseudoephedrine and I.S. were successfully separated using gradient elution with 0.5% trifluoroacetic acid (TFA) in water and 0.5% TFA in methanol at a flow-rate of 0.2 mL/min. Detection was performed on a single quadrupole mass spectrometer by a selected ion monitoring (SIM) mode via electrospray ionization (ESI) source. The ESI source was set at positive ionization mode. The ion signals of m/z 166... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5067158 Wed, 27 Jul 2011 09:15:03 +0100 5067158 http://www.medworm.com/index.php?rid=5067157&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21755811%26dopt%3DAbstract Authors: Gatchev E, Petrov A, Kolev E, Hristova R, Demircheva I, Koytchev R, Richter W, Tegel F, Thyroff-Friesinger U The aim of the present study was to assess the pharmacodynamic equivalence (lowering of intraocular pressure) of two preparations of eye drops containing 20 mg dorzolamide (CAS 120279-96-1) and 5 mg timolol (CAS 26839-75-8). PMID: 21755811 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5067157 Wed, 27 Jul 2011 09:15:03 +0100 5067157 http://www.medworm.com/index.php?rid=5067156&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21755812%26dopt%3DAbstract Authors: Ren XL, Tian Y, Zhang ZJ, Chen Y, Wu LL, Huang J A rapid, sensitive and selective HPLC-MS/ MS method was developed and validated for the quantification of cetirizine dihydrochloride (CAS 83881-51-0) in human plasma using mosapride citrate as internal standard (IS, CAS 112885-42-4). Following liquid-liquid extraction, the analytes were separated using a mobile phase consisting of methanol and aqueous ammonium acetate solution (10 mM) (60:40, v/v) on a reverse phase C18 column and analyzed by a triple-quadrupole mass spectrometer in the selected reaction monitoring (SRM) mode using the respective [M+H]+ ions, m/z 398 --> 201 for cetirizine and m/z 422 --> 198 for mosapride. The analysis time for each run was 8.0 min. The assay exhibited a linear dynamic range of 0.5-500 ng... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5067156 Wed, 27 Jul 2011 09:15:03 +0100 5067156 http://www.medworm.com/index.php?rid=5067155&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21755813%26dopt%3DAbstract In this study, new pyrrole derivatives of I (1-(1-phenylcyclohexyl)pyrrole, II and 1-[1-(4-methylphenyl)(cyclohexyl)]pyrrole, III) and their intermediates were synthesized and the acute and chronic pains were examined on mice using tail immersion (as a model of acute thermal pain) and formalin (as a model of acute and chronic chemical pain) tests and the results were compared with the PCP and control groups. The results indicated that III generated higher analgesic effects in the tail immersion test compared to the PCP and control (dimethyl sulfoxide, DMSO) groups, demonstrating a marked and significant increase in tail immersion latency, but this effect was not observed for II in the dose of 1 mg/kg. The formalin test showed that III was effective in acute chemical pain (phase I, 0-5 min ... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5067155 Wed, 27 Jul 2011 09:15:03 +0100 5067155 http://www.medworm.com/index.php?rid=5067154&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21755814%26dopt%3DAbstract Authors: Nirogi R, Kandikere V, Mudigonda K, Ajjala D, Suraneni R, Thoddi P A simple analytical method using liquid chromatography-tandem mass spectrometry (LC-MS/MS) in atmospheric chemical ionization mode (APCI) for the simultaneous estimation of acetylsalicylic acid (ASA, CAS 50-78-2) and its active metabolite salicylic acid (SA, CAS 69-72-7) in human plasma has been developed and validated. ASA and SA were analyzed simultaneously despite differences in plasma concentration ranges of ASA and SA after oral administration of ASA. In spite of having different chemical, ionization and chromatographic properties, ASA and SA were extracted simultaneously from the plasma sample using acetonitrile protein precipitation followed by liquid-liquid extraction. The analytes were separated on a r... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5067154 Wed, 27 Jul 2011 09:15:03 +0100 5067154 http://www.medworm.com/index.php?rid=5067153&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21755815%26dopt%3DAbstract Authors: Gupta R, Bhatia J, Gupta SK Combination of disease-modifying antirheumatic drugs (DMARDs) is increasingly used in the treatment of rheumatoid arthritis (RA) patients. Hepatotoxicity has been an important safety concern with DMARDs therapy. Though leflunomide (CAS 75706-12-6) has emerged as an effective oral DMARD, its use is associated with hepatotoxicity. Limited data is available regarding hepatotoxic risk when leflunomide is used in combination therapy in RA patients. An open-label, prospective study was conducted to evaluate the hepatotoxic risk after addition of leflunomide with other DMARDs in RA patients, who did not respond to their ongoing DMARD therapy. A total of 46 patients were enrolled and leflunomide was given as add-on therapy with earlier DMARDs. Biochemical p... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5067153 Wed, 27 Jul 2011 09:15:03 +0100 5067153 http://www.medworm.com/index.php?rid=5067152&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21755816%26dopt%3DAbstract Authors: Cloete TT, Johansson CC, N'Da DD, Vodnala SK, Rottenberg ME, Breytenbach JC, Ashton M The aim of this study was to synthesize a series of mono-, di- and trisubstituted derivatives of the human African trypanosomiasis drug eflornithine (alpha-difluoromethylornithine, DMFO, CAS 70052-12-9) to determine their partition coefficients, and to assess whether they deliver the parent drug in the plasma. If increased plasma concentrations of eflornithine could be achieved in this way, an oral dosage form would be possible. The derivatives, nine in total, were successfully synthesized by multi-step derivatisation of eflornithine on either its alpha-carboxylic or/and alpha-amino or/and delta-amino groups by either esterification or/and amidation or/and carbamylation, and their structures ... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=5067152 Wed, 27 Jul 2011 09:15:03 +0100 5067152 http://www.medworm.com/index.php?rid=4922493&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21650079%26dopt%3DAbstract Authors: Marzo A, Fontana E The market of generic drugs has been greatly developing during the last 15 years in various European Union (EU) member states, mainly in the Mediterranean area, including non-EU countries, i.e., in the Middle East. This has required a more detailed support from EMA (European Medicines Agency) as guidelines are concerned. Previous EU guidelines on bioavailability and bioequivalence neglected some relevant issues often met in bioequivalence trials, defined in the literature as "open questions on bioequivalence". In the absence of EU specific directives these problems were managed by EU investigators in compliance with U.S. FDA (Food and Drug Administration) guidelines that had already considered some of these "open problems". The latest EMA guideline operating... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4922493 Mon, 13 Jun 2011 03:00:03 +0100 4922493 http://www.medworm.com/index.php?rid=4922492&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21650080%26dopt%3DAbstract Authors: Schall P, Wehling M The benefits of lowering blood pressure are obvious for the population up to the age of 65 years, but whether and, if so, which treatment is beneficial in the very elderly population remains still a matter of debate. We conducted a meta-analysis of randomised controlled clinical trials with duration of at least 12 months and the analysis of cardio- and cerebrovascular endpoints in participants aged 75 years and over. MEDLINE, CENTRAL (Cochrane Central Register of Controlled Trials) and the WHO-ISH Collaboration register were searched until October 20, 2009. Further, references from reviews, trials and previously published meta-analyses were analysed. A total of 10 studies were included providing morbidity and mortality data with a total of 8667 participants... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4922492 Mon, 13 Jun 2011 03:00:03 +0100 4922492 http://www.medworm.com/index.php?rid=4922491&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21650081%26dopt%3DAbstract Authors: Gill F, Pelit T, Terzioğlu B, Ekinci O, Gören MZ Agmatine (CAS 2482-00-0), an amine formed by decarboxylation of L-arginine, interacts with several targets like alpha2-adrenergic, imidazoline and N-methyl-D-aspartic acid (NMDA) receptors and besides it is involved in the nitric oxide mediated effects. It has also been proposed that it possesses vasodilator effects and increases glomerular filtration rate in rats. The aim of this study was to supply evidence for the effects of agmatine in a rat model of hemorrhagic shock and explain the possible mechanisms of action. The iliac arteries and veins of Sprague-Dawley rats were catheterized under urethane anesthesia and around 2 ml/100 g blood was withdrawn within 20 min until the mean arterial blood pressure was stabilized around... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4922491 Mon, 13 Jun 2011 03:00:03 +0100 4922491 http://www.medworm.com/index.php?rid=4922490&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21650082%26dopt%3DAbstract This study was a randomized, single-blind, two-period, two-sequence cross-over study which included 20 healthy adult male and female subjects under fasting conditions. In this study, one subject withdrew from the study and one reserve subject did not appear at both periods. The pharmacokinetic parameters were assessed based on the concentrations of perindopril (CAS 82834-16-0) and perindoprilat (CAS 95153-31-4) because perindopril has litte pharmacologic activity until hydrolized in the liver into its active metabolite, perindoprilat. The blood samples from 18 subjects were analyzed for plasma concentrations of perindopril and perindoprilat. In each of the two study periods (separated by a washout of three weeks) a single dose of test or reference drug was administered. Plasma concentratio... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4922490 Mon, 13 Jun 2011 03:00:03 +0100 4922490 http://www.medworm.com/index.php?rid=4922489&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21650083%26dopt%3DAbstract Authors: Zhao ZW, Cai W, Lin YL, Lin QF, Jiang Q, Lin Z, Chen LL The present study was designed to examine whether astaxanthin (ASX, 3,3-dihydroxybeta, beta-carotene-4,4-dione, CAS 472-61-7), a dietary antioxidant carotenoid that is naturally present in algae, crustaceans, and fish, has a protective effect on endothelial dysfunction of aortas in diabetic rats and the possible molecular mechanism involved. Male Wistar rats were randomly divided into four groups: control rats, diabetic rats, diabetic rats treated with ASX (10 mg/kg/d), and control rats treated with ASX. Type 1 diabetes was induced by a single intraperitoneal injection of streptozotocin (STZ; 60 mg/ kg). STZ-induced diabetes in rats was complicated with excessive oxidative stress and endothelial dysfunction, increased ser... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4922489 Mon, 13 Jun 2011 03:00:03 +0100 4922489 http://www.medworm.com/index.php?rid=4922488&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21650084%26dopt%3DAbstract Authors: Seiler D, Doser K, Salem I Prasugrel (CAS 150322-43-3), an inhibitor of platelet activation and aggregation, is indicated to reduce the rate of thrombotic cardiovascular events in patients with acute coronary syndrome. If a proton pump inhibitor is co-administered with prasugrel, a pH dependent salt-to-base conversion rate of prasugrel could become clinically meaningful. In an open-label, randomized, four-period, 2 x two-way crossover study, the relative bioavailability of tablets containing prasugrel free base compared to prasugrel hydrochloride (originator product) both in the presence and in the absence of the proton pump inhibitor lansoprazole (CAS 103577-45-3) was investigated. In the absence of lansoprazole, the extent of absorption (AUC) of prasugrel free base was about... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4922488 Mon, 13 Jun 2011 03:00:03 +0100 4922488 http://www.medworm.com/index.php?rid=4922487&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21650085%26dopt%3DAbstract Authors: Uckun F, Dibirdik I, Sarkissian A, Qazi S The present study documents the chemosensitizing anti-leukemic activity of the leflunomide metabolite (LFM) analog, LFM-A13, a dual-function inhibitor of Bruton's tyrosine kinase (BTK) and Polo-like kinases (PLK), against human leukemic B-cell precursors. The results in 135 xenografted NOD/SCID mice regarding the anti-leukemic activity of GMP-grade LFM-A13, obtained with only 4-days of LFM-A13 therapy at nontoxic dose levels corresponding to 1-20% of its NOAEL (no observable advserse effect level), alone or in combination with the standard chemotherapy drug vincristine, demonstrate the potential of LFM-A13 as a new anti-leukemic drug candidate. All 82 LFM-A13-treated mice, including those receiving a combination of vincristine + LFM-A1... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4922487 Mon, 13 Jun 2011 03:00:03 +0100 4922487 http://www.medworm.com/index.php?rid=4922486&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21650086%26dopt%3DAbstract Authors: Petersen EE, Genet M, Caserini M, Palmieri R A randomised, double blind, parallel groups, placebo controlled clinical trial was conducted to assess the efficacy and safety profile of 250 mg ascorbic acid (Vit. C, Vagi C) in women with bacterial vaginosis (BV). Overall, 277 out-patients with at least three of the following signs (white discharge that smoothly coats the vaginal walls, pH of vaginal fluid > 4.5, a fishy odour of vaginal discharge before or after addition of 10% KOH and presence of clue cells on microscopic examination) were randomised to apply a tablet deeply into the vagina once daily for 6 days. The primary efficacy endpoint was the cure rate, defined as the recovery of all inclusion criteria. In the intent-to-treat (ITT) population, cure was achieved by 55.... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4922486 Mon, 13 Jun 2011 03:00:03 +0100 4922486 http://www.medworm.com/index.php?rid=4876776&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21528637%26dopt%3DAbstract Authors: Ghandforoush-Sattari M, Zakeri-Milani P, Mashayekhi S, Valizadeh H The aim of the present study was to determine the concentrations of nitroglycerin (glyceryl trinitrate, GTN, CAS 55-63-0) and its two main stable metabolites; 1,2-dinitroglycerin (1,2-glyceryl dinitrate, GDN, CAS 621-65-8) and 1,3-dinitroglycerin (1,3-GDN, CAS 623-87-0) in human plasma using a capillary gas chromatography method with an electron capture detection. Using the GC conditions, linear calibrations were obtained for 1,3-GDN from 0.14 to 3 ng/mL, for 1,2-GDN from 0.06 to 6 ng/mL, and for GTN from 0.01 to 0.3 ng/mL in plasma samples by the following calibration curve equations: [y = 0.1924x - 0.0088 (r = 0.999)], [y = 0.2273x + 0.0164 (r = 0.995)], [y = 17.434x - 0.0751] for 1,3-GDN, 1,2-GDN, and GTN re... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4876776 Sun, 29 May 2011 22:45:03 +0100 4876776 http://www.medworm.com/index.php?rid=4876775&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21528638%26dopt%3DAbstract This study aims to investigate the effect of 20(S)-protopanaxatriol (PT, CAS 179799-20-3) and its epimeric derivatives (20S, 24R-epoxy-dammarane-3beta, 6alpha, 12beta, 25-tetraol, PTD1 and 20S, 24S-epoxy-dammarane-3beta, 6alpha, 12beta, 25-tetraol, PTD2) on myocardial injury induced by isoproterenol in rats. PMID: 21528638 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4876775 Sun, 29 May 2011 22:45:03 +0100 4876775 http://www.medworm.com/index.php?rid=4876774&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21528639%26dopt%3DAbstract Authors: Almeida S, Pedroso P, Filipe A, Pinho C, Neves R, Jiménez C, Sicard E, Lefebvre M Eplerenone (CAS 107724-20-9) prevents the binding of aldosterone, a key hormone in the renin-angiotensin-aldosterone-system (RAAS), which is involved in the regulation of blood pressure and the pathophysiology of cardiovascular disease and is indicated, in addition to standard therapy including beta-blockers, to reduce the risk of cardiovascular mortality and morbidity in stable patients with left ventricular dysfunction (LVEF < or = 40%) and clinical evidence of heart failure after recent myocardial infarction. PMID: 21528639 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4876774 Sun, 29 May 2011 22:45:03 +0100 4876774 http://www.medworm.com/index.php?rid=4876773&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21528640%26dopt%3DAbstract Authors: Qi W, Fan W, Benidipine (CAS 91599-74-5) has been reported as an effective antihypertensive treatment and its cardioprotective effects have been shown in several basic and clinical studies. However, the long-term efficacy and safety of benidipine remain unknown in elderly Chinese patient with hypertension. In this prospective, multicenter, open-label clinical trial, 152 eligible patients aged 60 to 75 years with mild to moderate essential hypertension (sitting systolic blood pressure (BP) > or = 140 mmHg and/or sitting diastolic BP > or = 90 mmHg) entered a 52-week study. All patients initially received benidipine 2-4 mg once a day, followed by titration to benidipine 8 mg/day to achieve the target BP (< 140/90 mmHg in non-diabetics and <130/80 mmHg in diabetics).... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4876773 Sun, 29 May 2011 22:45:03 +0100 4876773 http://www.medworm.com/index.php?rid=4876772&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21528641%26dopt%3DAbstract Authors: Huang J, Tian Y, Zhang ZJ, Li J, Cao X The pharmacokinetics and relative bioavailability/bioequivalence of two formulations of mosapride citrate (CAS 112885-42-4) were assessed in this study. The study was conducted in 20 healthy Chinese male volunteers according to an open, randomized, single-blind, 2-way crossover study design with a wash-out phase of 7 days. Blood samples for pharmacokinetic profiling were taken up to 12 h post-dose, and mosapride citrate plasma concentrations were determined by a validated liquid chromatography-tandem mass spectrometry (LC-MS/MS) method. Based on the plasma concentration-time data of each individual during two periods, pharmacokinetic parameters, Cmax, AUCo-t,, AUCo-infinity, and t1/2, were calculated by applying non-compartmental analysis... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4876772 Sun, 29 May 2011 22:45:03 +0100 4876772 http://www.medworm.com/index.php?rid=4876771&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21528642%26dopt%3DAbstract The objective of this study was to evaluate whether colchicine has any effect on EE-induced cholestasis. The effects of colchicine treatment on EE-induced cholestasis in rats for 5 consecutive days were evaluated. The serum components and enzymatic activity were assayed. In addition, the bile flow and biliary excretion were determined. Furthermore, western blot analysis was used to measure the expression of farnesoid X receptor (FXR), bile salt export pump (BSEP), multidrug resistance-associated protein 2 (MRP2), and cholesterol 7alpha-hydroxylase (CYP7A1). Colchicine not only significantly inhibited the elevation of cholestasis-related serum components and enzyme activity but also significantly attenuated the decrease of the bile flow and biliary excretion. Colchicine also remarkably incr... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4876771 Sun, 29 May 2011 22:45:03 +0100 4876771 http://www.medworm.com/index.php?rid=4876770&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21528643%26dopt%3DAbstract Authors: Deshpande SR, Pai KV, Pai RS In an attempt to develop effective and safer analgesic anti-inflammatory agents, nine compounds belonging to 4-[1-oxo-3-(substituted aryl)-2-propenyl]-3-(4-methoxyphenyl) sydnones, containing the structural features of mesoionic sydnone and styrylketone, have been designed and synthesized by condensing 4-acetyl-3-(4-methoxyphenyl) sydnone with various substituted aryl aldehydes and characterized by spectral studies. They have been tested for analgesic activity by acetic acid induced writhing in mice and for anti-inflammatory activity by carrageenan induced rat paw edema at 100 mg/kg body weight p.o. The compounds containing furyl and chloro substituents showed highly significant analgesic effect, while those with dimethylamino, chloro and nitro sub... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4876770 Sun, 29 May 2011 22:45:03 +0100 4876770 http://www.medworm.com/index.php?rid=4876769&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21528644%26dopt%3DAbstract In this study, 15 compounds bearing N,N-phthaloylacetamide structure designed by the molecular simplification approach based on thalidomide structure were synthesized and evaluated for inhibitory potencies against cyclooxgenase (COX) isoenzymes, namely COX-1 and COX-2. The results suggested that the N,N-phthaloylacetamide structure, as a primary amide, has inhibitory activity against cyclooxygenase isoenzymes with a higher COX-1 selectivity. The conversion of the primary amide to secondary or tertiary derivatives lowered the potency but favored the COX-2 selectivity thus yielding the compounds with stronger COX-2 inhibiting activity. PMID: 21528644 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4876769 Sun, 29 May 2011 22:45:03 +0100 4876769 http://www.medworm.com/index.php?rid=4876768&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21528645%26dopt%3DAbstract Authors: Imanishi Y, Matsui K, Ishida K, Ito S, Matsuura K, Deguchi T, Itoh Y The present study was designed to determine the pharmacokinetic profiles of a once-daily formulation of tacrolimus (CAS 104987-11-3; TAC-once) in patients before and after introduction of renal transplantation. Pharmacokinetic parameters for tacrolimus were almost comparable among patients receiving TAConce before, 2 weeks after and 3 weeks after renal transplantation. Among various parameters, C(trough) correlated most closely with the area under the concentration-time curve during 24 h (AUCo-24) (R2 = 0.82, P < 0.001), while no consistent correlation was observed between AUCo_24 and concentrations at 2 h or 4 h, or the dose of TAC-once. The clinical outcomes such as the incidence of acute re-jection, ren... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4876768 Sun, 29 May 2011 22:45:03 +0100 4876768 http://www.medworm.com/index.php?rid=4876767&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21528646%26dopt%3DAbstract Authors: Zhao L, Liu Y, Kou Z, Bayasi A, Cai H, Zhang C, Wang Q, Li Y, Fang Y Existing methods to determine biapenem (CAS 120410-24-4), a carbapenem, either lacked sensitivity/reproducibility or had no internal standard as a control. Here an improved reversed-phase high-performance liquid chromatographic (RP-HPLC) method was established in human plasma and urine. After adding p-aminobenzoic acid as the internal standard to plasma or urine, plasma samples were ultra-filtrated and urine samples were diluted directly. Chromatographic separations were carried out on a 4.6 mm x 150 mm column with acetonitrile-0.1 mol/l sodium acetate (2:98, v:v; pH 4.38 or 4.00) as mobile phase and UV detection at 300 nm. The extraction recovery was 91.51% for biapenem at the concentration level of 5 microg... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4876767 Sun, 29 May 2011 22:45:03 +0100 4876767 http://www.medworm.com/index.php?rid=4665549&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21428240%26dopt%3DAbstract Authors: Cánovas M, Torres F, Domenech G, Cebrecos J, Pelagio P, Manríquez M, Martínez G, Arcabell M, Cabré F Two bioequivalence studies were carried out in healthy volunteers in order to compare the rate and extent of absorption of two dosage forms (film-coated tablet and orodispersible tablet) of oral olanzapine (CAS 132539-06-1) 10 mg test formulations and the respective brand formulations as reference. Twenty and twenty-six subjects were administered olanzapine film-coated tablet or orodispersible tablet of test and reference formulations in an open-label, randomised, fasting, two-period, two-sequence, crossover study. Blood samples were taken before and within 240 h after drug administration. Plasma concentrations were determined by LC/MS/MS. Log-transformed AUC and Cmax value... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4665549 Fri, 01 Apr 2011 19:15:15 +0100 4665549 http://www.medworm.com/index.php?rid=4665548&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21428241%26dopt%3DAbstract Authors: Nandi U, Bhaumik U, Chakrabarty US, Das A, Pal TK A randomized, two-treatment and two-way crossover study on twelve healthy Indian male subjects was conducted to assess the bioequivalence of two tablet formulations containing 20 mg of rimonabant (CAS 158681-13-1). Both of the formulations were administered orally as a single dose with a 45-day washout period between two dosing sessions. The content of rimonabant in plasma was determined by a validated HPLC method with UV detection. The formulations were compared using the parameters area under the plasma concentration-time curve (AUC(0-t)), area under the plasma concentration-time curve from zero to infinity (AUC(0-infinity)), peak plasma concentration (Cmax), and time to reach peak plasma concentration (tmax). The results of ... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4665548 Fri, 01 Apr 2011 19:15:15 +0100 4665548 http://www.medworm.com/index.php?rid=4665547&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21428242%26dopt%3DAbstract Authors: Kumokawa T, Hirata K, Sato K, Kano S Dermal absorption of mucopolysaccharide polysulfate (MPS, the active ingredient of Hirudoid") in human and minipig was investigated by using 14C-labeled MPS. Three types of human and minipig skin samples were used: intact, dried and tape-stripped. At 24 h after application of 14C-MPS to intact human skin on a Franz cell in vitro, the radioactivity was detected in 0.98, 1.34, and 0.08% of the applied dose in stratum corneum, epidermal-dermal skin, and receptor fluid, respectively. In dried human skin, the amount of radioactivity detected was similar to that in intact human skin. By contrast, in tape-stripped human skin, higher radioactivity was detected in epidermal-dermal skin and receptor fluid (2.85 and 0.33% of the applied dose, respecti... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4665547 Fri, 01 Apr 2011 19:15:15 +0100 4665547 http://www.medworm.com/index.php?rid=4665546&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21428243%26dopt%3DAbstract Authors: Ahmadi A, Khalili M, Hajikhani R, Naserbakht M Phencyclidine (1-(1-phenylcyclohexyl)piperidine, CAS 77-10-1, PCP, I) and many of its analogues have been synthesized and their pharmacological properties studied. In this research, new methyl morpholine derivative of phencyclidine (1-[1-(4-methylphenyl) (cyclohexyl)]morpholine, Methyl-PCM, III) was synthesized and the acute and chronic pain activities were studied using tail immersion and formalin tests on rats and compared to PCP and PCM (1-(1-phenylcyclohexyl)morpholine, CAS 2201-40-3, PCP-morpholine, II). The results Indicated that Methyl-PCM (III, 6 mg/kg, i.p) produces more analgesic effects in tail immersion test (as a model of acute thermal pain) in comparison with the PCP, PCM and control groups. Meanwhile, this analgesic... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4665546 Fri, 01 Apr 2011 19:15:15 +0100 4665546 http://www.medworm.com/index.php?rid=4665545&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21428244%26dopt%3DAbstract Authors: Liu L, Jiang Z, Huang X, Liu J, Zhang J, Xiao J, Bao Q, Wen J, Zhang S, Zhu D, Zhang P, Zhang L Triptolide (CAS 38748-32-2), a major active component of Tripterygium wilfordii Hook F (TWHF), was reported to be sex-dependently metabolized mainly due to sex-related expression of CYP3A2. Sexual dimorphism in the expression of CYP isoforms is affected by sex difference in daily rhythm of growth hormone (GH) secretion. Neonatal administration of monosodium glutamate (MSG) can produce latent developmental defects in GH secretion and associated sex-dependent hepatic enzymes. In the present study, the triptolide metabolism, CYP3A2 expression and CYP3A-dependent activity were evaluated in Sprague-Dawley rats treated neonatally with MSG (4 mg/g) or saline (control) on postnatal days 1, ... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4665545 Fri, 01 Apr 2011 19:15:15 +0100 4665545 http://www.medworm.com/index.php?rid=4665544&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21428245%26dopt%3DAbstract Authors: Ringe JD, Schacht E, Dukas L, Mazor Z This is a preplanned subgroup analysis on 318 patients with glucocorticoid-induced osteoporosis (GIOP) from an open, prospective, multi-centered, uncontrolled study on a large cohort of elderly patients with a high risk of falls and fractures. The entire group of 2579 patients was recruited by 818 practicing physicians and treated for three months with a new combination package containing 4 or 12 self-explanatory one-week blisters, each with one tablet of 70 mg alendronate (CAS 260055-05-8) and 7 capsules of 1 pg alfacalcidol (CAS 41294-56-8) (Tevabone"). The average age of the GIOP patients was 71 years and the mean body mass index 26.7 kg/m2. 58% had a diagnosis of increased risk of falls, prevalent vertebral and non-vertebral fractures ... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4665544 Fri, 01 Apr 2011 19:15:15 +0100 4665544 http://www.medworm.com/index.php?rid=4665543&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21428246%26dopt%3DAbstract This report describes physicochemical and toxicological studies into a new iron sucrose generic preparation, "Iron Sucrose Azad (ISA)", using the original iron sucrose product as reference. It could be demonstrated that the specifications and physicochemical characteristics of ISA reflect those of the reference product. Furthermore, in a rat model previously shown to identify possible toxicological effects of "unsimilar" iron sucrose preparations, ISA was found to have the same properties as the reference product, with both being well tolerated. PMID: 21428246 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4665543 Fri, 01 Apr 2011 19:15:15 +0100 4665543 http://www.medworm.com/index.php?rid=4665542&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21428247%26dopt%3DAbstract Authors: Singh RP, Sabarinath S, Gautam N, Gupta RC, Singh SK The present study has been designed to investigate the pharmacokinetic parameters of the novel trioxane antimalarial 97-78 (US Patent 6316493 B1, 2001) in male and female rats after single oral and intravenous administration. The pharmacokinetic profile of 97-78 was investigated in the form of its completely converted metabolite 97-63 after dose administration. Quantification of metabolite 97-63 in rat plasma was achieved using a simple and rapid LC-MS/MS method. The LC-MS/MS method has been validated in terms of accuracy, precision, sensitivity and recovery for metabolite 97-63 in rat plasma. The intra- and interday accuracy (% bias) and precision (% RSD) values of the assay were less than 10% for metabolite 97-63. The chro... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4665542 Fri, 01 Apr 2011 19:15:15 +0100 4665542 http://www.medworm.com/index.php?rid=4665540&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21428248%26dopt%3DAbstract This study compared the efficacy of a thymol + eugenol vaginal douche (SD) (CAS nr. thymol: 89-83-8 and eugenol: 97-53-0), with econazole (CAS 27220-47-9) in VC and metronidazole (CAS 443-48-1) in BV, as suppository reference therapies. Thymol and eugenol are natural antibacterial and antimycotic active ingredients extracted from plants. PMID: 21428248 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4665540 Fri, 01 Apr 2011 19:15:15 +0100 4665540 http://www.medworm.com/index.php?rid=4665509&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21428249%26dopt%3DAbstract Authors: Cheng Y, Zhang ZJ, Tian Y, Li WJ, Wei W A sensitive and specific liquid chromatography-electrospray ionization mass spectrometry (LC-ESI-MS) method was developed and validated for the identification and quantification of voriconazole (VRC, CAS 137234-62-9) in human plasma. Following liquid-liquid extraction, VRC and loratadine (internal standard, CAS 79794-75-5) were separated using a mobile phase comprised of methanol: water (0.1% formic acid) = 75:25 v/v on a Shimadzu Shim-pack VP-ODS C18 (150 x 2.0 mm ID, 5 microm) column and analyzed by electrospray ionization mass spectrometry. The chromatographic separation was achieved in less than 6 min. The standard curves were linear (r = 0.9994) over the concentration range of 2-2000 ng/mL for VRC and had good accuracy and precision... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4665509 Fri, 01 Apr 2011 19:15:15 +0100 4665509 http://www.medworm.com/index.php?rid=4543759&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21355440%26dopt%3DAbstract In this study thirteen 6-substituted-3(2H)-pyridazinone-2-acetyl-2-(substituted/nonsubstituted benzal)hydrazone V derivatives were synthesized as acetylcholinesterase and butyrylcholinesterase inhibitors. Ten of the synthesized compounds were synthesized for the first time in this study and the rest of them had been synthesized in a previous study. The structures of compounds V were elucidated by IR, 1H-NMR and MASS spectra. The acetylcholinesterase (AChE) and butyrylcholinesterase (BChe) inhibitory activities of V derivatives were measured using Ellman's method. While some of the 6-substituted-3(2H)-pyridazinone-2-propyl-3-(substituted/-nonsubstituted benzal)hydrazone V derivatives exhibited significant AChE inhibitory activity, none of the compoundsshowed BChE inhibitory activity. Theser... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4543759 Fri, 04 Mar 2011 01:00:08 +0100 4543759 http://www.medworm.com/index.php?rid=4543752&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21355441%26dopt%3DAbstract Authors: Satake M, Takahashi H, Sugawara K, Kawagoshi A, Tamaki A, Homma M, Morita R, Sato K, Sano M, Shioya T The purpose of this study was to evaluate the inhibitory effect of procaterol (procaterol hydrochloride, CAS 62929-91-3) on exercise dynamic lung hyperinflation during the 6-min walk test (6MWT) in stable chronic obstructive disease (COPD) patients. Fourteen patients with stable COPD who were referred to our clinic between July 2008 and October 2009 were evaluated in this study. After the inhalation of procaterol, values for the lung function test, including vital capacity, inspiratory capacity, forced vital capacity, and FEV1/FEV1pred showed a significant improvement. Compared to the baseline assessment, the 6-min walk distance increased by a mean of 20.5 m when measured afte... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4543752 Fri, 04 Mar 2011 01:00:08 +0100 4543752 http://www.medworm.com/index.php?rid=4543745&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21355442%26dopt%3DAbstract Authors: Jelvehgari M, Milani PZ, Siahi-Shadbad MR, Monajjemzadeh F, Nokhodchi A, Azari Z, Valizadeh H The aim of this study was to investigate the applicability of microspheres containing protease inhibitor for oral delivery of insulin (CAS 9004-10-8). Microspheres of insulin were prepared by water-in-oil-in-oil (w/o1/o2) double emulsion solvent evaporation method. Formulations with different drug/polymer ratios were prepared and characterized by drug loading, loading efficiency, yield, particle size, scanning electron microscopy (SEM), Fourier Transform Infrared spectroscopy (FTIR). The in vitro release studies were performed in pH 1.2 and 7.4. In vivo studies on rats were conducted in order to investigate the bioavailability and performance of oral microspheres. The best polymer to ... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4543745 Fri, 04 Mar 2011 01:00:08 +0100 4543745 http://www.medworm.com/index.php?rid=4543739&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21355443%26dopt%3DAbstract Authors: Musmade PB, Talole KB, Deshpande PB, Karthik A, Pathak SM, Pandey S, Udupa N The need for a reliable bioanalytical method is of primary importance during preclinical studies. The aim of the present study was simultaneous determination of pioglitazone (CAS 111025-46-8) (PIO) and glimepiride (CAS 93479-97-1) (GLM) in plasma of rats. A high-performance liquid chromatographic method has been developed and validated using C18 column and UV detector. A mobile phase composed of acetonitrile and ammonium acetate buffer pH 4.5 in the ratio of 55:45%. The plasma samples clean-up was carried out using solid phase cartridges. The method was in the linear range of 50-8000 ng/mL for PIO and 50-2000 ng/mL for GLM. The coefficient of regression was found to be > or = 0.99. Precision and ac... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4543739 Fri, 04 Mar 2011 01:00:08 +0100 4543739 http://www.medworm.com/index.php?rid=4543733&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21355444%26dopt%3DAbstract Authors: Almeida S, Filipe A, Neves R, Pinho C, Pedroso P, Castillo A, Trabelsi F Pioglitazone (CAS 112529-15-4 for the HCl form) is an oral antidiabetic agent that is a member of the group of drugs known as thiazolidinediones. It is indicated for the treatment of type 2 diabetes mellitus. PMID: 21355444 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4543733 Fri, 04 Mar 2011 01:00:08 +0100 4543733 http://www.medworm.com/index.php?rid=4543724&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21355445%26dopt%3DAbstract Authors: Schacht E, Ringe JD Efficacy and safety of a new combination package containing 4 or 12 self-explanatory one-week blisters, each with one tablet of 70 mg alendronate (CAS 260055-05-8) and 7 capsules of 1 microg alfacalcidol (CAS 41294-56-8) (Tevabone) on muscle power, muscle function, balance and back pain was investigated in an open, multi-centered, uncontrolled, prospective study on a cohort of elderly patients with a high risk of falls and fractures. 818 practicing physicians all over Germany recruited 2579 patients for a 3-month observational trial being treated with the above combination package. 92.4% were women [89.7% of the women had postmenopausal osteoporosis (PMO)]. Their average age was 74.1 years and the mean body mass index 26.4 kg/m2. 55.4% had a history of fall... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4543724 Fri, 04 Mar 2011 01:00:08 +0100 4543724 http://www.medworm.com/index.php?rid=4543713&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21355446%26dopt%3DAbstract The objective of this study was to compare the rate and extent of absorption and to assess the bioequivalence between a new pharmaceutical equivalent tablet formulation containing 300 mg of TDF and the innovator product. A randomized, single-center, open-label, single-dose, two-way crossover bioequivalence study in 40 healthy adult subjects was conducted. Dosing was separated by a wash-out period of 14 days. Blood samples were collected over 48 h and plasma levels of tenofovir (TFV) were determined by a validated HPLC assay. Rate and extent of absorption were similar between products. The 90% confidence interval (CI) of the ratio of the geometric means for log-transformed C(max), AUC(last) and AUC(inf) values were used to assess bioequivalence between the two formulations using the equival... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4543713 Fri, 04 Mar 2011 01:00:08 +0100 4543713 http://www.medworm.com/index.php?rid=4543680&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21355447%26dopt%3DAbstract Authors: Das A, Mukherjee J, Dey G, Sarkar AK, Sahoo BK, Chakrabarty US, Nandi U, Pal TK An improved HPLC method was developed and validated for the determination of concentration of levofloxacin (CAS 100986-85-4) in human plasma. This paper is an attempt to compare the bioavailability of two levofloxacin tablet formulations (reference and test) containing 500 mg of levofloxacin. Both the formulations were administered orally as a single dose, separated by a washout period of 1 week. The HPLC method was validated by examining the precision and accuracy for the inter-day and intra-day runs in a linear concentration range of 0.10-10.00 microg/ml. Bioequivalence of two formulations were determined in 12 healthy, Indian, male volunteers in a single-dose, two-period, two-sequence, two-treat... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4543680 Fri, 04 Mar 2011 01:00:08 +0100 4543680 http://www.medworm.com/index.php?rid=4543672&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21355448%26dopt%3DAbstract Authors: Leban J, Vitt D Dihydroorotate dehydrogenase (DHODH), a novel and recently discovered enzyme, is involved in the biosynthesis of uridine. Leflunomide (CAS 75706-12-6), a drug approved for the treatment of treat rheumatoid arthritis (RA), was identified as an inhibitor of DHODH. Structure based drug design using the leflunomide/DHODH X-ray structure yielded novel inhibitors with improved pharmacological properties. Such drug candidates are in clinical trials against various autoimmune diseases. PMID: 21355448 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4543672 Fri, 04 Mar 2011 01:00:08 +0100 4543672 http://www.medworm.com/index.php?rid=4286163&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21175036%26dopt%3DAbstract Authors: Said SA, El-Agamy DS The present study was designed to examine the potential preventive effect of curcumin (CMN; CAS 458-37-7), rosiglitazone (RGN; CAS 155141-29-0), N-acetylcysteine (NAC; CAS 616-91-1), resveratrol (RSV; CAS 501-36-0), and losartan (LOS; CAS 114798-26-4) on sodium valproate-induced hepatotoxicity. Sodium valproate (SVP; CAS 1069-66-5) was given at a dose of 250 mg/kg i. p. 3 times daily for one week. The tested compounds were given simultaneously with SVP for one week. The results demonstrate that CMN, RGN and NAC treatment can confer protection from SVP-induced hepatotoxicity. The second part of the study includes an evaluation of the effect of CMN, RGN and NAC on the anticonvulsant activity of SVP against pentetrazole-induced seizures in mice. The results d... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4286163 Fri, 24 Dec 2010 17:00:06 +0100 4286163 http://www.medworm.com/index.php?rid=4286162&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21175037%26dopt%3DAbstract The objective of the present investigation is to develop and validate a simple, economical and reliable high performance liquid chromatography method for the quantification of quetiapine (CAS 111974-72-2) in human plasma with a quantification limit sufficiently low to support pharmacokinetic studies. Imipramine hydrochloride (CAS 113-52-0) was used as internal standard. The validated method allows quantification of quetiapine in 15-1000 ng/mL. The method was shown to be precise (< 7% coefficient of variation, CV) and accurate (< or = 10% relative error, RE). The correlation coefficient for quetiapine was > 0.9970. The simplicity of the assay and rapid liquid-liquid extraction make it an attractive procedure in high-throughput bioanalysis of quetiapine. PMID: 21175037 [PubMed -... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4286162 Fri, 24 Dec 2010 17:00:06 +0100 4286162 http://www.medworm.com/index.php?rid=4286161&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21175038%26dopt%3DAbstract Authors: He T, Zou Q, Feng Z, Zhang Z A rapid and sensitive method based on liquid chromatography/tandem mass spectrometry (LC-MS/MS) has been developed and fully validated for the quantitative determination of sodium tanshinone IIA sulfonate (STS, sodium (1,6,6-trimethyl-10,11-dioxo-7,8,9-trihydrophenanthro[1,2-b]furan)-yl-2-sulfonate) in rat biosamples including plasma and different tissues using sodium tanshinone I sulfonate (sodium (1,6-dimethyl-10,11-dioxo-phenanthro[1,2-b]furan)-yl-2-sulfonate) as internal standard. Simple protein precipitation by acetonitrile was utilized for extracting STS from the rat biosamples. Chromatographic separation of the sample matrix from the analyte and the internal standard was performed using a commercially available analytical column with a mobil... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4286161 Fri, 24 Dec 2010 17:00:06 +0100 4286161 http://www.medworm.com/index.php?rid=4286160&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21175039%26dopt%3DAbstract Authors: Hotha KK, Dasari VB, Shaik AN, Syed M, Shivva V, Lakshmanarao RK, Korlakunta JN, Mullangi R Tolmetin (TMT, CAS 26171-23-3) is a non-steroidal anti-inflammatory drug (NSAID) indicated for the relief of signs and symptoms of osteoarthritis, rheumatoid arthritis and juvenile rheumatoid arthritis. As TMT causes gastro-intestinal side effects like other NSAIDs, its nonacidic prodrug amtolmetin guacil (AMG, CAS 87344-06-7) was synthesized. AMG has similar NSAID properties like TMT with additional gastroprotective property. The aim of this study was to investigate whether TMT and AMG are differentially metabolised in rat and human plasma (fresh and acidified) and liver microsomes. TMT was found to be stable in all the matrices tested viz., rat and human plasma (fresh and acidified) a... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4286160 Fri, 24 Dec 2010 17:00:06 +0100 4286160 http://www.medworm.com/index.php?rid=4286159&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21175040%26dopt%3DAbstract Authors: Braga PC, Dal Sasso M, Culici M, Spallino A Bacterial vaginosis (BV) is the most frequent diagnosis made in women with lower genital tract symptoms. It has recently been observed that 90 % of subjects with BV show the growth of bacteria in the form of biofilms as against only 10% without BV, and that Gardnerella vaginalis was the predominant species. The propensity of G. vaginalis to form biofilm is clinically relevant because this form of growth allows it to tolerate higher concentrations of certain antibiotics, thus increasing the possibilty of recurrent BV even after apparently curative therapy. The aim of this study was to investigate whether thymol (CAS 89-83-8), a molecule present in thyme essential oil, that is credited with having a series of pharmacological properties... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4286159 Fri, 24 Dec 2010 17:00:06 +0100 4286159 http://www.medworm.com/index.php?rid=4286158&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21175041%26dopt%3DAbstract Authors: Helena KJ, N'Da DD, Johansson CC, Breytenbach JC, Ashton M The purpose of this study was to synthesize a series of delta-amide derivatives of the antitrypanosomal drug eflornithine (2,5-diamino-2-(difluoromethyl)pentanoic acid hydrochloride, DMFO, CAS 70052-12-9), to determine their physicochemical properties and to assess whether they convert to eflornithine in vivo and if so, whether higher systemic exposure to eflornithine could be achieved by increase intestinal absorption, suggesting an oral treatment to be possible. The derivatives were synthesized by amidation of eflornithine on its delta-amino group using acyl chlorides. The partition coefficients (log D, pH = 7.4) were found to be between -0.78 +/- 1.07 and -0.07 +/- 1.08 while the aqueous solubility (Sw), which as de... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4286158 Fri, 24 Dec 2010 17:00:06 +0100 4286158 http://www.medworm.com/index.php?rid=4258748&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21125807%26dopt%3DAbstract Authors: Deng XQ, Wei CX, Song MX, Quan ZS The present study describes the chemical synthesis and pharmacological evaluation of a series of 9-alkoxy-7H-furo[3,2-g]-chromen-7-ones. The pharmacological results of these compounds show that nine of them, given orally, reduced the immobility time in the forced swimming test. The results of the open-field test further confirmed that these compounds possessed an antidepressant-like effect. In the 5-hydroxytryptophan induced head-twitch test, 9-(3-chlorobenzyloxy)-7H-furo[3,2-g]chromen-7-one (3 m, 40 mg/kg p. o.) significantly increased the cumulative numberof head twitches. This finding suggested that the antidepressant-like profile seems to involve the serotonergic system as underlying mechanism. PMID: 21125807 [PubMed - in process] (Sou... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4258748 Wed, 15 Dec 2010 01:50:10 +0100 4258748 http://www.medworm.com/index.php?rid=4258743&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21125808%26dopt%3DAbstract Authors: Tarikogullari AH, Kilic FS, Erol K, Pabuccuoglu V A group of N-phenylacetamide, N-phenylpropanamide and N-benzylamide derivatives bearing 5-membered heterocyclic rings such as pyrazole, 1,2,4-triazole and imidazole rings at omega position were synthesized and their anticonvulsant activity was evaluated in the maximal electroshock test. The results indicated that the 1,2,4-triazole ring leads to superior activity than the pyrazole ring and inserting a CH2 group into the anilide structure leading to N-benzyl derivatives did not change the anticonvulsant activity, but caused a noticeable decrease in duration of action. The most active compound was 2-(1H-1,2,4-triazole-1-yl)-N-(2,6-dimethylphenyl)acetamide. PMID: 21125808 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4258743 Wed, 15 Dec 2010 01:50:10 +0100 4258743 http://www.medworm.com/index.php?rid=4258741&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21125809%26dopt%3DAbstract Authors: Mallayasamy SR, Arumugamn K, Jain T, Rajakannan T, Bhat K, Gurumadhavrao P, Devarakonda R A sensitive and selective high performance liquid chromatographic (HPLC) method was developed and validated for estimation of lamotrigine (CAS 84057-84-1) in human plasma and saliva. The chromatographic separation was achieved with a reversed phase column and a mobile phase consisting of acetonitrile and 20 mM ammonium acetate buffer pH 6.5 (30:70) with a flow rate of 1 mL/min. The calibration curve was linear within the working range for both plasma and saliva. The validated method has been successfully applied for a study of lamotrigine in human plasma and saliva to establish the correlation between these two matrices. A scatter plot of plasma versus salivary lamotrigine concentrations ... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4258741 Wed, 15 Dec 2010 01:50:10 +0100 4258741 http://www.medworm.com/index.php?rid=4258734&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21125810%26dopt%3DAbstract Authors: Valizadeh H, Nemati M, Hallaj-Nezhadi S, Ansarin M, Zakeri-Milani P The purpose of the present study was to compare the bioavailability of a new methyldopa (CAS 555-30-6) tablet formulation with that of a reference formulation in 12 healthy male subjects using a modified HPLC method. PMID: 21125810 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4258734 Wed, 15 Dec 2010 01:50:10 +0100 4258734 http://www.medworm.com/index.php?rid=4258730&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21125811%26dopt%3DAbstract Authors: Sato K, Dohi Y, Kojima M, Takase H, Suzuki S, Ito S Some thiazide diuretics seem to exert antioxidant effects, which may be beneficial in the management of hypertension. Although many large-scale clinical trials on hypertension have proved that thiazide diuretics confer significant reductions in stroke and cardiovascular events, most of these trials preferentially used chlortalidone. Therefore, the difference in antioxidant effects between chlortalidone (CAS 77-36-1; 12.5 mg/day) and another thiazide diuretic, trichlormethiazide (CAS 133-67-5; 1 mg/day) was studied. Forty patients with refractory hypertension even after treatment with a combination of a calcium channel blocker and an angiotensin II receptor blocker were randomly assigned to additionally receive either chlortal... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4258730 Wed, 15 Dec 2010 01:50:10 +0100 4258730 http://www.medworm.com/index.php?rid=4258726&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21125812%26dopt%3DAbstract In this study, besides the 4-hydroxy substituent phenyl and p-methylphenyl derivatives were synthesized and confirmed on the basis of their spectral data. 3-Amino-4-hydroxy coumarin, 5,7-dihydroxy-4-phenyl coumarin and 7,8-dihydroxy-3-(4-methylphenyl)coumarin were tested in rats to determine whether they had any effect on vitamin K inhibition by investigating the prothrombin time (PT). PT values of coumarin derivatives were compared with those of warfarin (CAS 81-81-2), which is the most commonly used anticoagulant. 7,8-Dihydroxy-3-(4-methylphenyl)coumarin increased PT when compared to saline treated control group and other coumarins synthesized, 3-amino-4-hydroxy coumarin and 5,7-dihydroxy-4-phenyl coumarin. PMID: 21125812 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4258726 Wed, 15 Dec 2010 01:50:10 +0100 4258726 http://www.medworm.com/index.php?rid=4258721&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21125813%26dopt%3DAbstract Authors: Chattopadhyay P, Wahi AK Folate is necessary for the production and maintenance of new cells and important during periods of rapid cell division and growth. Tumor necrosis factor-alpha (TNF-alpha) is known as a stimulant of apoptotic cell death. The present study was aimed to evaluate the efficacy of folic acid (CAS 59-30-3) in prevention of apoptosis by inhibiting TNF-alpha action in ischemia-reperfusion (I/R) induced liver injury. Eighteen Wistar rats were subjected to 1 h of hepatic ischemia followed by 3 h reperfusion and were divided into sham-operated control Group (I) (n = 6), ischemia and reperfusion group administered 0.9% saline (5 ml/kg, p.o.) for 7 days (II) (n = 6), folic acid treated group (1 mg/kg body weight/treated daily by oral route for 7 days before induced... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4258721 Wed, 15 Dec 2010 01:50:10 +0100 4258721 http://www.medworm.com/index.php?rid=4258689&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21125814%26dopt%3DAbstract Authors: N'Da DD, Breytenbach JC, Smith PJ, Lategan C Series of 4-aminoquinolines bearing an amino side chain linked to the ferrocene moiety through an amide bond were synthesized and evaluated for their antimalarial activity against both chloroquine-sensitive (D10, CQ-S) and chloroquine-resistant (Dd2, CQ-R) strains of Plasmodium falciparum. They were also tested for cytotoxicity against Chinese Hamster Ovarian (CHO) cells. Amide 12 featuring propyl side chain linked to the ferrocene ring was the most active of all tested compounds. With an IC50 value of 0.08 microg/mL, this amide showed 1.5-fold higher activity than chloroquine diphosphate (IC50 = 0.12 microg/mL) against the resistant strain, with a selectivity index of 550 indicating its high selectivity towards the parasite. Deriva... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4258689 Wed, 15 Dec 2010 01:50:10 +0100 4258689 http://www.medworm.com/index.php?rid=4258675&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21125815%26dopt%3DAbstract Authors: Gandia P, Trancart S, Nicot F, Barange K, Alric L, Izopet J, Séraissol P, Lavit M, Houin G Ribavirin (CAS 66510-90-5) associated to peginterferon (CAS 99210-65-8) is the current standard treatment for chronic hepatitis C. Exposure to ribavirin influences the virological response and anemia. Therefore monitoring plasma concentration of ribavirin is a useful tool for individualizing ribavirin dosing regimens. Ribavirin is a substrate of several nucleoside transporters that play a role in its distribution in erythrocytes. After blood sampling, it is essential to limit this mechanism. The aim of this study was to evaluate the influence of temperature and time on ribavirin plasma concentrations. Two blood samples, collected in EDTA tubes, were taken at the same time from 23 patien... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4258675 Wed, 15 Dec 2010 01:50:10 +0100 4258675 http://www.medworm.com/index.php?rid=4258666&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21125816%26dopt%3DAbstract Authors: Zhang QH, Yang J, He Y, Liu F, Wang JP, Davey AK The aim of the present study was to assess the effect of food on the pharmacokinetics of entecavir (CAS 142217-69-4) from dispersible tablets. PMID: 21125816 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4258666 Wed, 15 Dec 2010 01:50:10 +0100 4258666 http://www.medworm.com/index.php?rid=4224390&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21117496%26dopt%3DAbstract Authors: Burda K, Czubak A, Nowakowska E, Kus K, Metelska J, Nowakowska A Cognitive disorders in the course of mental illnesses are one of the most important and most difficult therapeutic problems related to those illnesses and they regard attention, memory, learning and sensory modulation. The limited number of nicotinic receptors (subtypes alpha7 and alpha4beta2) seems to cause the incidence and exacerbation of cognitive deficits in such patients. In patients with schizophrenia, the impairment of cognitive processes is also a side-effect of neuroleptics. The characteristics and intensity of the negative effect of antipsychotics on cognitive functions depends on the pharmacological action of those drugs and on the effect on dopamine and serotoninergic receptors in particular. Cogniti... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4224390 Fri, 03 Dec 2010 12:50:04 +0100 4224390 http://www.medworm.com/index.php?rid=4224375&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21117497%26dopt%3DAbstract Authors: Enzensperger C, Lehmann J, von Schroetter K, Riyazi A, Verspohl EJ Specific serotonin receptor agonists and antagonists are marketed with respect to various diseases, most prominently severe emesis. To identify new chemical classes with affinity for the serotonin 5-HT3 channel, several compounds were synthesized which can be structurally classified as arylalkylamines, azecines, quinolizines and beta-carbolines. These were tested in three models: (1) direct effect on ileum (overall model for contracting or relaxant effect), (2) antiserotoninergic effects on rat ileum (crude serotonin model), (3) inhibitory effect on the 5-HT, receptor channel complex expressed in N1E-115 cells (serotonin-induced [14C]guanidinium influx (specific model)). Key findings and conclusion: Several aze... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4224375 Fri, 03 Dec 2010 12:50:04 +0100 4224375 http://www.medworm.com/index.php?rid=4224366&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21117498%26dopt%3DAbstract Authors: Homsek I, Parojcić J, Dacević M, Petrović L, Jovanović D The Biopharmaceutics Classification System (BCS) represents the framework for predicting the intestinal drug absorption based on its solubility and intestinal permeability. Recent research has lead to the use of in vitro tests to waive additional in vivo bioequivalence studies for some pharmaceutical products (i.e., biowaiver). The current regulations permit waivers for BCS Class I (highly soluble/highly permeable) drug substances, which represent up to 25% of the drugs. Efforts in both the science and regulatory bodies are being made to extend biowaivers to certain Class II and III products, which would represent more than 50% of all drugs coming to the market. The aim of this study was to investigate the influence ... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4224366 Fri, 03 Dec 2010 12:50:04 +0100 4224366 http://www.medworm.com/index.php?rid=4224345&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21117499%26dopt%3DAbstract The objective of this study was to evaluate the pharmacokinetics of fenofibric acid, the main metabolite of fenofibrate (CAS 49562-28-9), and to assess the average bioequivalence of two immediate release formulations of 200 mg fenofibrate capsules in 24 healthy volunteers. The relative bioavailability of the test (generic) product Lipivim with respect to the reference product was determined in a single dose, randomized, crossover study. Only the concentrations of fenofibric acid could be used for bioequivalence determination, because the concentrations of the parent drug were too low to be accurately measured in the biological matrix. The mean values for the Cmax were 3.08 (+/- 1.69) microg/ml for the test and 3.05 (+/- 1.79) microg/ml for the reference product. The mean values for the AUC... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4224345 Fri, 03 Dec 2010 12:50:04 +0100 4224345 http://www.medworm.com/index.php?rid=4224326&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21117500%26dopt%3DAbstract Authors: Asaka N, Kakuo H, Ohmori K, Sasaki E, Togawa M, Yamada S, Oka T, Kiniwa M TAS-203 (2-[3-(cyclopropylmethoxy)-4-methoxyphenyl]-5-(1H-1,2,4-triazol-1-yl)-1H-benzimidazole, CAS 223909-92-0) is a novel phosphodiesterase 4 (PDE4) inhibitor that has been found to have good anti-inflammatory effects and low emetogenic activity in vivo. In the present studies, the anti-inflammatory profile of TAS-203 was examined and compared with that of cilomilast (CAS 153259-65-5), the most advanced PDE4 inhibitor. TAS-203 inhibited the activity of purified human PDE4 with an IC50 value of 88 nM and also the recombinant PDE4 subtypes (4A, 4B, 4C and 4D) with respective IC50 values of 47, 35, 227 and 43 nM. In the experiments using inflammatory cells, TAS-203 concentration-dependently inhibited plat... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4224326 Fri, 03 Dec 2010 12:50:04 +0100 4224326 http://www.medworm.com/index.php?rid=4224219&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21117501%26dopt%3DAbstract Authors: Chen X, Sun X, Ren K, Zhang X, Zhang Z, Gong T To increase the aqueous solubility and poor bioavailability of capsaicin (CAS 404-86-4), in this paper, the effects of hydroxypropyl-beta-cyclodextrin (HP-beta-CD) on the aqueous solubility and the pharmacokinetic characteristics of capsaicin were investigated. The corresponding inclusion complex of capsaicin/HP-beta-CD at the molar ratio of 1:1 was obtained by the method of saturated aqueous solution and characterized by differential scanning calorimetry and X-ray diffractometry. The dissolution rate of capsaicin was significantly increased by the complexation with HP-beta-CD, due to its solubilizing activity. The absorption behavior and bioavailability of capsaicin and its complexation were evaluated after their subcutaneous (s.... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4224219 Fri, 03 Dec 2010 12:50:04 +0100 4224219 http://www.medworm.com/index.php?rid=4224213&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21117502%26dopt%3DAbstract Authors: N'Da DD, Breytenbach JC, Breytenbach JW In continuation of studies focusing on the transdermal delivery of antiretroviral (ARV) drugs, the skin permeation ability of synthesized homologous series of both oligomeric and polymeric ethylene glycol (PEG) carbonates of zidovudine (3'-azido-3'-deoxythymidine, AZT, CAS 30516-87-1) and stavudine (2',3'-dideoxy-2',3'-didehydrothymine, d4T, CAS 3056-17-5) was evaluated in vitro through excised human skin in phosphate buffered solution (PBS) (0.01 M, pH 7.4) at 37 degrees C by using Franz cell diffusion methodology. The results revealed that all the derivatives permeated the skin regardless of the series. However, the derivative having three ethylene glycol repeating units was the most effective permeant in each series. The skin permeati... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4224213 Fri, 03 Dec 2010 12:50:04 +0100 4224213 http://www.medworm.com/index.php?rid=4001550&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20863002%26dopt%3DAbstract Authors: Kus K, Burda K, Nowakowska E, Czubak A, Metelska J, Łancucki M, Brodowska K, Nowakowska A Deficits of cognitive functions are perceived as an important pathogenic factor of many neurological and psychiatric diseases. Such symptoms can be a result of a disease process or appear due to applied medication. Epilepsy is a disease in which cognitive deficits can occur before first seizures, during seizures and remissions. Valproic acid (VAL, CAS 77372-61-3) is a medicine applied in order to control epileptic seizures and mood stabilizing in bipolar disorders and mania. Its activity is related to the effect on neurotransmission of many systems. The present study was conducted to investigate whether enriched environment (EE) conditions affect learning and memory, and influence the ... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4001550 Sun, 26 Sep 2010 00:39:03 +0100 4001550 http://www.medworm.com/index.php?rid=4001549&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20863003%26dopt%3DAbstract Authors: Wu JF, Xiang BR, Li KX A randomized, two-way, crossover, bioequivalence study in 6 beagle dogs was conducted to compare the bioavailability of two peppermint oil formulations, soft capsule and hard capsule. The drug was given in a single dose of two capsules (total, 200 mg), and blood samples were withdrawn during the 12 h after drug administration. Menthol (CAS 2216-51-5) as the main component of peppermint oil was determined by a gas chromatography-tandem mass spectrometry (GC-MS/I MS) method after cleavage with beta-glucuronidase. The following pharmacokinetic variables were computed for the two formulations: maximum concentration (Cmax), time to maximum concentration (Tmax), half-life of elimination (t1/2), mean residence time (MRT), and areas under the plasma concentratio... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4001549 Sun, 26 Sep 2010 00:39:03 +0100 4001549 http://www.medworm.com/index.php?rid=4001548&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20863004%26dopt%3DAbstract In conclusion, it cannot be ruled out that a relevant pharmacodynamic interaction between diazepam and esomeprazole may occur when both drugs are concomitantly administered. Pantoprazole may provide a higher safety profile. PMID: 20863004 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4001548 Sun, 26 Sep 2010 00:39:03 +0100 4001548 http://www.medworm.com/index.php?rid=4001547&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20863005%26dopt%3DAbstract Authors: Ahmadi A, Solati J, Hajikhani R, Onagh M, Javadi M Phencyclidine (1-(1-phenylcyclohexyl) piperidine, CAS 956-90-1, PCP, I) and its derivatives have shown many analgesic effects. In this research, a new derivative of PCP (1-[1-(2-methylphenyl) (cyclohexyl)l3-piperidinol, PD, II) was synthesized and its analgesic (acute and chronic pains) effects were examined on rats using tail immersion (as a model of acute thermal pain) and formalin (as a model of acute and chronic chemical pain) tests and the results are compared to PCP and control groups. The results indicated that II produces higher analgesic effects in the tail immersion test compared to the PCP and control groups, with a marked and significant increase in tail immersion latency for the doses 1, 5 and 10 mg/kg. The formal... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4001547 Sun, 26 Sep 2010 00:39:03 +0100 4001547 http://www.medworm.com/index.php?rid=4001546&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20863006%26dopt%3DAbstract Authors: Ergün BC, Nuñez MT, Labeaga L, Ledo F, Darlington J, Bain G, Cakir B, Banoglu E A set of 25 derivatives of 3-[1-(6-substituted-pyridazin-3-yl)-5-(4-substituted-phenyl)-1H-pyrazol-3-yl]propanoic acids has been synthesized and evaluated for their in vitro cyclooxygenase-1/2 (COX-1/ 2) inhibitory activity using assays with purified COX-1 and COX-2 enzymes as well as for their 5-lipoxygenase (5-LO)-mediated LTB4 formation inhibitory activity using an assay with activated human polymorphonuclear leukocytes (PMNL). Among the synthesized compounds, especially 4g showed COX-1 (IC50 = 1.5 microM) and COX-2 (IC50 = 1.6 microM) inhibitory activity, whereas compounds 4 b and 4 f resulted in the inhibition of 5-LO-mediated LTB4 formation at 14 microM and 12 microM IC50 values, respec... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4001546 Sun, 26 Sep 2010 00:39:03 +0100 4001546 http://www.medworm.com/index.php?rid=4001545&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20863007%26dopt%3DAbstract Authors: Mukherjee J, Das A, Chakrabarty US, Sahoo B, Sengupta P, Chatterjee B, Roy B, Pal TK The pharmacokinetics of rabeprazole (CAS 117976-89-3) and diclofenac sodium (CAS 15307-79-6) has been extensively evaluated in adult human volunteers individually after oral administration of tablet formulation. However, no published data is available regarding the combined pharmacokinetics and bioavailability of this particular fixed dose combination. In light of the above, a clinical study was designed to evaluate the bioequivalence of two fixed dose combination (FDC) products (reference and test) of two manufacturers containing rabeprazole 20 mg and diclofenac sodium 100 mg slow release (SR) tablet in healthy Indian male volunteers. Each subject received a test FDC and a reference FDC in a ... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4001545 Sun, 26 Sep 2010 00:39:03 +0100 4001545 http://www.medworm.com/index.php?rid=4001544&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20863008%26dopt%3DAbstract Authors: Marzo A, Coa K, Fontana E, Tavazzi S, Bo LD, Ismaili S, Zava D, Cantoni V, Bertolini A Ritodrine hydrochloride ((R,S)-4-hydroxy-alpha-[1-[2-((4-hydroxyphenyl)ethyl]amino)ethyl]benzenemethanol, CAS 26652-09-5) is a direct-acting sympathomimetic agent with a predominant beta-adrenergic activity and a selective action on beta2-receptors. A clinical trial was carried out to investigate the pharmacokinetics, pharmacodynamics and safety of ritodrine hydrochloride administered at the doses of 10, 20 and 30 mg p.o. and 10 mg by i. m. route. A four-way randomised crossover design was adopted on 12 healthy female volunteers with a wash-out of at least 14 days. Concentrations of ritodrine and of the pool of ritodrine in plasma and concentrations of the pool of ritodrine in urine of volun... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4001544 Sun, 26 Sep 2010 00:39:03 +0100 4001544 http://www.medworm.com/index.php?rid=4001543&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20863009%26dopt%3DAbstract CONCLUSIONS: Treatment with alfacalcidol increases muscle power and balance as measured with three different muscle power and balance tests and leads to a highly significant decrease in the number of fallers and falls. PMID: 20863009 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=4001543 Sun, 26 Sep 2010 00:39:03 +0100 4001543 http://www.medworm.com/index.php?rid=3886324&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20712130%26dopt%3DAbstract Authors: Giorgino FL, Egan CG The aim of this systematic review was to evaluate the efficacy of isoxsuprine (1-(4-hydroxyphenyl)-2-(1-methyl-2-phe-noxyethylamino)-1-propanol, CAS 395-28-8), a tocolytic agent used in both preterm labour and risk of abortion. Two analyses were conducted on data reporting the use of isoxsuprine in the prevention of preterm delivery. The first analysis examined two double-blind studies to determine the effect of isoxsuprine compared to placebo. The second analysis reviewed data from 25 publications containing individual and general patient data. Main outcome measures included delay of pregnancy and patient outcome. Analysis of double-blind studies demonstrated a positive outcome with isoxsuprine in 92% of cases compared to placebo control (44.4%, p < 0.... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3886324 Sat, 21 Aug 2010 01:36:02 +0100 3886324 http://www.medworm.com/index.php?rid=3886323&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20712131%26dopt%3DAbstract CONCLUSION: OAC greatly reduces gastrointestinal absorption of LTG and especially that of OXC, and it accelerates the elimination of LTG and MHD. The use of OAC is hence strongly favoured in the treatment of overdose with these drugs. PMID: 20712131 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3886323 Sat, 21 Aug 2010 01:36:02 +0100 3886323 http://www.medworm.com/index.php?rid=3886322&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20712132%26dopt%3DAbstract Authors: Mösges R, Kaatz V, Schmalz P, Meiser P, Eschmann K Inflammations of the external auditory canal number among the most frequently occurring ear-nose-throat diseases. For local treatment, substances from various groups of active ingredients are used as combinations and as single-agent drugs, e.g. antibiotics, glucocorticoids or analgesics [1]. In the case of acute otitis externa, treatment measures focus on the reduction of pain and swelling. The study described here investigates the efficacy and safety of glycerol lidocaine eardrops for the treatment of acute abacterial otitis externa (CAS No. for glycerol: 56-81-5, lidocaine-HCl: 73-78-9). In this double-blind, three-arm study, 105 patients diagnosed with acute abacterial otitis externa were included and randomized to recei... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3886322 Sat, 21 Aug 2010 01:36:02 +0100 3886322 http://www.medworm.com/index.php?rid=3886321&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20712133%26dopt%3DAbstract Authors: Zhao L, Gu S, Xu R, Cui X, Gan F, Chen H The aim of this study was to compare two methods which were based on liquid chromatography with ultraviolet detection (LC-UV) and liquid chromatography-tandem mass spectrometry (LC-MS/MS), respectively, to determine indapamide (CAS 26807-65-8) and to apply them to bioequivalence studies. The universal parameters, including selectivity, linearity, precision, and quantification limit, served as gold standard for the comparison of the two methods. As a result, the two methods were both very consistent and reliable. Furthermore, the LC-MS/MS method required only one-fifth the blood volume needed by the other method and was approximately 25 times more sensitive than the other method. The total run time of the LC-MS/MS method was 3.5 min per ... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3886321 Sat, 21 Aug 2010 01:36:02 +0100 3886321 http://www.medworm.com/index.php?rid=3886320&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20712134%26dopt%3DAbstract CONCLUSION: Since the 90% CI for Cmax and AUCs ratios were all within the 80-125% interval proposed by the US Food and Drug Administration Agency, it was concluded that the test formulation is bioequivalent to the reference for both the rate and the extent of absorption. PMID: 20712134 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3886320 Sat, 21 Aug 2010 01:36:02 +0100 3886320 http://www.medworm.com/index.php?rid=3886318&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20712135%26dopt%3DAbstract Authors: Nishikawa T, Matsuzawa Y, Suematsu S, Saito J, Omura M, Kino T Nephropathy is a major complication of diabetes mellitus, thus development of rational therapeutic means is critical for improving public health. It was previously reported that human mesangial cells locally produced aldosterone, a steroid hormone that plays an important role in the development of diabetic nephropathy. The present experiments clarified the effect of glucose, LDL and angiotensin II, the molecules frequently elevated in patients with diabetic nephropathy, on aldosterone production in human primary mesangial cells. These cells expressed the CYP11B2 mRNA, a rate-limiting enzyme in the aldosterone biosynthesis. LDL and angiotensin II stimulated CYP11B2 mRNA expression in these cells, while a high concen... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3886318 Sat, 21 Aug 2010 01:36:02 +0100 3886318 http://www.medworm.com/index.php?rid=3886317&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20712136%26dopt%3DAbstract Authors: Ozçelik AB, Gökçe M, Orhan I, Kaynak F, Sahin MF In the current study, some novel ethyl 6- [(substituted-phenylpiperazine]-3(2H)-pyridazinone-2-yl propionate III and 6-[(substituted-phenylpiperazine]-3(2H)-pyridazinone-2-yl propionohydrazide IV derivatives were synthesized as acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitors. The structures of these new pyridazinone derivatives were confirmed by their IR, 1H-NMR spectra and elementary analysis. 6-Substituted-3(2H)-pyridazinone-2-yl propionate IIIa-e derivatives showed significant inhibitory activity against AChE and BChE. 6-[4-(3-Trifluoromethylphenyl)piperazine]-3(2H)-pyridazinone-2-yl propionate IIIe has been found to be the most active compound in terms of inhibition of either AChE or BChE. Co... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3886317 Sat, 21 Aug 2010 01:36:02 +0100 3886317 http://www.medworm.com/index.php?rid=3886313&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20712137%26dopt%3DAbstract In conclusion, ferric gluconate showed the highest increase in intracellular ROS-production in HepG2 cells and the highest amount of redox-active iron in buffer in the in vitro assays. In contrast to the other i.v. iron preparations, redox-active iron from ferric gluconate was rendered completely redox-inactive by serum, indicating that redox-active iron in the various preparations has different chemical properties. PMID: 20712137 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3886313 Sat, 21 Aug 2010 01:36:02 +0100 3886313 http://www.medworm.com/index.php?rid=3781059&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20648916%26dopt%3DAbstract Authors: Sun XY, Wei CX, Deng XQ, Sun ZG, Quan ZS A new series of 6-alkyoxyl-tetrazolo[5,1-a] phthalazine derivatives (4 a-4 o) were synthesized as potential anticonvulsant agents. Anticonvulsant activity was evaluated by the maximal electroshock (MES) test. Neurotoxicity was evaluated by the rotarod neurotoxicity test. The pharmacological results showed that 6-(4-chlorophenyoxyl)-tetrazolo[5,1-a]phthalazine (4 m) was the most potent agent, with a median effective dose (ED50) of 6.8 mg/kg and a median neurotoxic dose (TD50) of 456.4 mg/kg. The protective index (PI = TD50/ED50) for compound 4 m was 67.1, which was significantly higher than that for the reference drug carbamazepine (PI = 6.4). PMID: 20648916 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3781059 Fri, 23 Jul 2010 16:06:03 +0100 3781059 http://www.medworm.com/index.php?rid=3781058&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20648917%26dopt%3DAbstract Authors: Appenroth D, Fleck C The influence of age on (1) cognition and (2) scopolamine (CAS 51-34-3) induced memory impairment in female rats was measured in the radial maze paradigm (RAM). (1) First training trials were done with 3 and 12 months old rats. Rats were trained to find all eight food baits in the RAM without errors and within 1 min. Both 3- and 12-month old rats need about 15 trials for the first-time learning of the RAM task. After intervals of 3 6 months, respectively, initially young rats were re-trained with an age of 6 and 12 months. Surprisingly, re-trained rats successfully completed the maze runs already after one re-training trial. Thus the phenomenon of preserved spatial memory was approved for female rats. (2) Memory impairment by scopolamine in the RAM was tes... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3781058 Fri, 23 Jul 2010 16:06:03 +0100 3781058 http://www.medworm.com/index.php?rid=3781057&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20648918%26dopt%3DAbstract Authors: Fleck C, Appenroth D, Fang L, Schott Y, Lehmann J, Decker M Two tacrine-ferulic acid hybrids (1 A, 1 B) and three beta-carboline derivatives (BCs; 2A, 2B, 2C) were tested in vivo on 3-month-old female rats as multi-potent anti-Alzheimer drug candidates. In vitro, the two tacrine-ferulic acid hybrids show higher acetylcholinesterase (AChE) inhibitory activity and comparable butyrylcholinesterase (BChE) inhibitory activity compared to tacrine (CAS 1684-40-8). However, in vivo both substances have no beneficial effect on scopolamine (CAS 51-34-3) induced cognition impairment. On the contrary, 1B even worsen the scopolamine induced cognition impairment. The beta-carboline derivatives 2A, 2B, and 2 C, the inhibitory potency of which at AChE reaching tacrine activity does not antago... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3781057 Fri, 23 Jul 2010 16:06:03 +0100 3781057 http://www.medworm.com/index.php?rid=3781056&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20648919%26dopt%3DAbstract Authors: Nowakowska E, Czubak A, Kus K, Metelska J, Burda K, Nowakowska A Epileptic patients are at risk of experiencing cognitive deficits as a result of pharmacotherapy as well as etiology of epilepsy. Antiepileptic drugs increase inhibitory neurotransmission and reduce the responsiveness of neurons, and thereby may have a negative impact on memory. The enriched environment intensifies exploration of the new area behavior, which may have a positive impact on spatial memory in rats. Depression is among the most common affective disorders in epileptic patients, and using antidepressant drugs together with antiepileptics brings about the risk of interactions and intensifying side effects, The aim of the study was to assess the effects of lamotrigine (CAS 84057-84-1, LTG) (10 mg/kg i.p.)... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3781056 Fri, 23 Jul 2010 16:06:03 +0100 3781056 http://www.medworm.com/index.php?rid=3781055&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20648920%26dopt%3DAbstract In conclusion, in vitro exposure to LPS desensitized vascular smooth muscle cells to endogenous and exogenous NO by overproduction of muscular iNOS-derived NO, and an iNOS inhibitor and iNOS induction inhibitors prevented the LPS-induced desensitization. PMID: 20648920 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3781055 Fri, 23 Jul 2010 16:06:03 +0100 3781055 http://www.medworm.com/index.php?rid=3781054&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20648921%26dopt%3DAbstract Authors: Lanovský M, Dolezal T, Procháizková M, Slíva J, Krsiak M The aim of the present study was to evaluate and compare the analgesic activity and serum levels of meloxicam (CAS 71125-38-7) after administration of meloxicam associated with beta-cyclodextrin (BCD, CAS 7585-39-9) and unmodified meloxicam. The analgesic activity was measured using the plantar test (rats) and the writhing test (mice). In the plantar test, BCD-meloxicam (3 mg/kg and 10 mg/kg orally) showed higher analgesic activity than corresponding doses of meloxicam alone; in the writhing test BCD-meloxicam (7 mg/kg and 15 mg/kg orally) showed stronger analgesic activity than unmodified meloxicam. Serum levels of meloxicam were significantly higher, at 0.5 h and 1 h after administration of BCD-meloxicam or... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3781054 Fri, 23 Jul 2010 16:06:03 +0100 3781054 http://www.medworm.com/index.php?rid=3781053&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20648922%26dopt%3DAbstract Authors: Bessler WG, vor dem Esche U, Zgaga-Griesz A, Ataullakhanov R The therapeutic agent OM-89 (Uro-Vaxom) contains lyophilized immunostimulating fractions from 18 Escherichia coil strains. It has been shown to provide protection against recurrent urinary tract infections in humans and against bacterial infections in mice. Here the immunostimulatory properties of OM-89 were investigated by in vitro and in vivo assays. In vitro the activation of murine spleen cells by the AlamarBlue assay was determined. OM-89 was effective in stimulating the metabolism of spleen cells within a concentration range of 0.625-2.5 mg/ml. The activation of murine bone marrow-derived macrophages by OM-89 was shown by the induction of NO production; OM-89 was a most effective stimulant at concentrations aro... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3781053 Fri, 23 Jul 2010 16:06:03 +0100 3781053 http://www.medworm.com/index.php?rid=3781052&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20648923%26dopt%3DAbstract Authors: Bonaterra GA, Kelber O, Weiser D, Metz J, Kinscherf R The well-known anti-inflammatory and analgesic effects of the phytopharmacon willow bark extract have been attributed to the content of salicin; however, pharmacological studies have shown that salicin alone, despite being involved in its therapeutic action, cannot fully explain its clinical efficacy. In addition to reducing inflammation and pain, acetylsalicylic acid (ASA, CAS 50-78-2), like other synthetic non-steroidal anti-inflammatory drugs (NSAIDs), has been shown to exert anti-proliferative effects and to induce apoptosis in a variety of cell lines, e.g., colon, stomach, and prostate cancer cells. To investigate the mechanism of action and possible anti-proliferative and proapoptotic effects of willow bark, a water e... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3781052 Fri, 23 Jul 2010 16:06:03 +0100 3781052 http://www.medworm.com/index.php?rid=3781051&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20648924%26dopt%3DAbstract The objective of this study was to develop a rapid and simplified, reliable high-performance liquid chromatography (HPLC) method for quantification of cefpirome (CAS 98753-19-6) in plasma. After precipitation of the plasma containing the internal standard, hydrochlorothiazide, with 5% trichloroacetic acid (TCA), the analysis of the cefpirome level in the plasma samples was carried out using a reverse-phase C18 column with the ultraviolet detector set at a wavelength of 258 nm. The chromatographic separation was accomplished with an isocratic mobile phase consisting of acetonitrile-acetate buffer pH 5. The proposed method was specific and sensitive with a lower limit of quantitation (LLOQ) of 0.5 microg/ml. This HPLC method was validated by examining the precision and accuracy for inter- an... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3781051 Fri, 23 Jul 2010 16:06:03 +0100 3781051 http://www.medworm.com/index.php?rid=3781050&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20648925%26dopt%3DAbstract Authors: Marx JJ PMID: 20648925 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3781050 Fri, 23 Jul 2010 16:06:03 +0100 3781050 http://www.medworm.com/index.php?rid=3781049&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20648926%26dopt%3DAbstract In conclusion, FCM has many of the characteristics of an ideal intravenous iron preparation. PMID: 20648926 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3781049 Fri, 23 Jul 2010 16:06:03 +0100 3781049 http://www.medworm.com/index.php?rid=3781048&cid=s_37558_13_f&fid=37558&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20648927%26dopt%3DAbstract Authors: Malek A An in vitro perfusion model of human placenta was used to study the transplacental passage of iron applied in the form of the drug compound ferric carboxymaltose (FCM) which had been radio-labelled with 59Fe. In four placental perfusion experiments, two simulated circuits for the maternal and fetal sides of the placenta were set up with two experimental phases each lasting 3 h. FCM was added to the maternal circuit at the beginning of each phase to a final iron concentration of 11 mM, which is at least 10 times higher than the maximal predicted level in blood after an administration of 200 mg iron as FCM. The effects of adding transferrin at a physiological concentration of 1.67 mg/ ml were also tested. The concentration profiles of 59Fe showed a 10% decrease within th... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3781048 Fri, 23 Jul 2010 16:06:03 +0100 3781048