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. Fri, 19 Mar 2010 15:13:25 +0100 http://www.medworm.com/index.php?rid=3312413&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%3D20184221%26dopt%3DAbstract Authors: Czubak A, Nowakowska E, Burda K, Kus K, Metelska J Many patients undergoing long-term treatment of epilepsy complain of memory disorders, which entail worse quality of life. The risk factors generating memory disorders include: morphological brain damage, the duration and course of epileptic seizures (conscience disorders), the time of diagnosis (the risk is greater if epileptic seizures start early in life), drug resistance, the presence of interseizure changes in the EEG in the form of sharp-wave discharges or sharp spike-wave/ slow spike-wave complexes and improper pharmacotherapy (exceeding the admissible concentration of drugs in blood serum, polytherapy). GABAergic neurotransmission of older antiepileptic drugs (barbiturates, benzodiazepines) makes them particularly pron... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3312413 Sat, 27 Feb 2010 11:48:03 +0100 3312413 http://www.medworm.com/index.php?rid=3312412&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%3D20184222%26dopt%3DAbstract CONCLUSIONS: Retrospective evaluation of fluoxetine and norfluoxetine pharmacokinetic data demonstrated existence of both PM and EM phenotypes in the Indian population. Based on the overall data (n=144 subjects) there appeared to be 10.4% of PM phenotypes for fluoxetine and/or possibly for other polymorphic CYP2D6 substrates commonly used in this region. PMID: 20184222 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3312412 Sat, 27 Feb 2010 11:48:03 +0100 3312412 http://www.medworm.com/index.php?rid=3312411&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%3D20184223%26dopt%3DAbstract Authors: Aytemir MD, Septioğlu E, Caliş U A series of new 3-hydroxy-6-hydroxymethyl-2-substituted 4H-pyran-4-one derivatives were synthesized as potential anticonvulsant compounds. Mannich compounds were prepared by the reaction of appropriate substituted piperazine derivatives with kojic acid and formaline. The structure of the synthesized compounds was confirmed using the elementary analysis results and spectroscopic techniques such as IR, 1H-NMR and ESI-MS. Anticonvulsant activities of the synthesized compounds were examined by maximal electroshock (MES) and subcutaneous Metrazol (scMet) induced seizure tests. Neurotoxicity was determined by the rotorod toxicity test. All these tests were performed according to procedures of the Antiepileptic Drug Development (ADD) progr... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3312411 Sat, 27 Feb 2010 11:48:03 +0100 3312411 http://www.medworm.com/index.php?rid=3312410&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%3D20184224%26dopt%3DAbstract Authors: Ahmadi A, Khalili M, Mihandoust F, Barghi L Phencyclidine (1-(1-phenylcyclohexyl)piperidine, CAS 956-90-1, PCP, 1) and ketamine (2-O-chlorophenyl-2-methylaminocyclohexan, CAS 1867-66-9, II) revealed some analgesic effects. Some of their derivatives have been synthesized for biological properties studies. Utilizing 1-tetralone as a starting material, 1-[1-(3-methylphenyl)(tetralyl)]piperidine, (PCP-CH3-tetralyl, III) was synthesized and its analgesic effects were studied on rats via tail immersion (as a model of acute thermal pain) and formalin (as a model of acute chemical and chronic pain) tests and compared with those of ketamine and PCP. The results indicated a marked anti-nociception 2-25 min after ketamine injection, but this analgesic effect lasted for 40 min following P... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3312410 Sat, 27 Feb 2010 11:48:03 +0100 3312410 http://www.medworm.com/index.php?rid=3312409&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%3D20184225%26dopt%3DAbstract Authors: Izquierdo I, Borja J, Rovira S, Pelagio P, Torres F, Cebrecos J, García-Rafanell J Triflusal (CAS 322-79-2) is an antiplatelet agent that irreversibly acetylates cyclooxygenase isoform 1 (COX-1) and therefore inhibits thromboxane biosynthesis. The main metabolite of triflusal, 2-hydroxy-4-trifluoromethyl benzoic acid (HTB), possesses also antiaggregant activity. Recently a new oral 600 mg (10 ml) solution form of triflusal has been developed. The purpose of this clinical trial was to study the relative bioavailability of the new oral solution of triflusal versus the capsules formulation, both administered as a single dose. This was a randomized, two-way, cross-over, open-label, single-site phase I clinical trial, in 24 healthy volunteers who received triflusal as 600 mg o... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3312409 Sat, 27 Feb 2010 11:48:03 +0100 3312409 http://www.medworm.com/index.php?rid=3312408&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%3D20184226%26dopt%3DAbstract CONCLUSION: Biorelevant medium in both USP apparatus 2 and 3 may be used as a tool to predict in vivo disposition of formulations of pantoprazole. Furthermore, it can be argued that biowaiver can be granted for enteric coated formulations of pantoprazole on the basis of in vitro dissolution profile. PMID: 20184226 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3312408 Sat, 27 Feb 2010 11:48:03 +0100 3312408 http://www.medworm.com/index.php?rid=3312407&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%3D20184227%26dopt%3DAbstract Authors: Ghorab MM, Ragab FA, Heiba HI, Youssef HA, Galal M Several novel pyrazole (11-18) and pyrimidine (19-23) derivatives were synthesized starting from different sulfonamides and different active methylenes. The synthesized compounds were characterized by elemental analysis, IR, 1H-NMR and mass spectral data. The obtained compounds were screened as antitumor agents against human tumor cell line. Some of the tested compounds were equipotent while the others were more potent than doxorubicin (CAS 25316-40-9). The synergistic effect with gamma-radiation was also studied. PMID: 20184227 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3312407 Sat, 27 Feb 2010 11:48:03 +0100 3312407 http://www.medworm.com/index.php?rid=3100764&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%3D19998575%26dopt%3DAbstract Authors: Nowakowska E, Kus K, Czubak A, Jedrzejewska J Topiramate (TOP, CAS 97240-79-4) particularly potentiates gamma-aminobutyric acid (GABA) neuroinhibition, and GABA and glutamate receptors, which have also been implicated in memory formation. Patients' giving up treatment due to adverse effects (disorders of attention, memory, and verbal fluency) is the main problem with a therapy based on this drug. The antidepressant effect of TOP administered to rats in the dose of 15 mg/kg is observed only after 14 and 21 days of treatment. The delay in the antidepressant effect of TOP may be due to the modulation of GABA A receptors as well as due to the influence of the drug on receptors for type AMPA/KAIN excitatory amino acids. The research has also shown that long-term treatment with TOP ... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3100764 Fri, 18 Dec 2009 16:32:02 +0100 3100764 http://www.medworm.com/index.php?rid=3100762&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%3D19998576%26dopt%3DAbstract Authors: Arumugam K, Chamallamudi MR, Mallayasamy SR, Ganesan S, Shavi GV, Averineni R, Reddy R, Bhat K, Udupa N The effect of gender on the pharmacokinetics of rivastigmine (CAS 123441-03-2) was studied in male and female Wistar rats following intravenous bolus administration. The area under the plasma concentration-time curve (AUC), apparent volume of distribution (Vd), systemic clearance (CL), and terminal plasma halflife (t1/2) of rivastigmine were compared between male and female rats. Compared to male rats, female rats exhibited higher plasma rivastigmine levels showing significantly (p < 0.05) larger AUC (226.77 vs. 149.68 ng h/ml), Vd (6.70 vs. 4.13 L), t1/2 (0.84 vs. 0.34 h) and a lower CL (5.51 vs. 8.35 L/h). The male rats had a 2.5 fold greater elimination rate constant t... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3100762 Fri, 18 Dec 2009 16:32:02 +0100 3100762 http://www.medworm.com/index.php?rid=3100761&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%3D19998577%26dopt%3DAbstract This study was designed to assess whether DA-6034 (7-carboxymethyloxy-3',4',5-trimethoxy flavone monohydrate), a new synthetic derivative of eupatilin, increases secretion of mucin-like glycoprotein and some mucins species in conjunctiva and cornea, and contributes to the preservation of ocular surface integrity. Human conjunctival and corneal epithelial cells were incubated with DA-6034 (1-250 microM). To investigate mucin secreting activity more directly, isolated rat conjunctival goblet cells were also used. Corneal protection was investigated using a desiccation-induced rabbit model of dry eye syndrome. It was found that DA-6034 increased mucin-like glycoprotein levels of both conjunctival and corneal epithelial cells at concentrations above 100 microM. Using human conjunctival epithel... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3100761 Fri, 18 Dec 2009 16:32:02 +0100 3100761 http://www.medworm.com/index.php?rid=3100758&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%3D19998579%26dopt%3DAbstract Authors: Metzner JE, Frank T, Kunz I, Burger D, Riegger C Genistein (CAS 446-72-0), an isoflavone and phytoestrogen predominantly found in soy, is considered a promising natural bioactive to prevent post-menopausal bone loss. geniVida (previously Bonistein), a novel product containing of min. 98.5% synthetic genistein aglycone, was investigated in 12 healthy post-menopausal women to assess the safety and tolerability as well as to obtain pharmacokinetic data after 7 days of repeated intakes. 24 h pharmacokinetic profiles were determined after the first oral dose and after 7 days repeated intakes of 30 mg of the test formulation. Plasma genistein (aglycone) and its conjugates were determined by a standardised LC/MS analytical method using D4-genistein as the internal standard. The plasm... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3100758 Fri, 18 Dec 2009 16:32:02 +0100 3100758 http://www.medworm.com/index.php?rid=3100754&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%3D19998580%26dopt%3DAbstract This study was conducted in order to assess the bioequivalence of two different formulations containing 70 mg alendronate sodium (CAS 121268-17-5) under fasted conditions. One hundred twenty-two healthy male volunteers were enrolled in an open label, randomized, crossover design with a wash-out period of 20 days in one study center. Urine samples were collected up to 36 h post-dose, and the concentrations of alendronic acid were determined using a high performance liquid chromatographic method with pre-derivatization and fluorescence detection (HPLC/FL) method. The mean Ae(0-t) were 604.24 +/- 348.73 microg and 627.36 +/- 327.99 microg, while the mean R(max) were 193.87 +/- 114.68 microg/h and 202.00 +/- 107.83 microg/h for the test and reference formulations, respectively. The T(max) of t... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3100754 Fri, 18 Dec 2009 16:32:02 +0100 3100754 http://www.medworm.com/index.php?rid=3100751&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%3D19998581%26dopt%3DAbstract Authors: Mahjoob E, Khalaj A, Ostad SN, Azizi E, Fouladdel S, Tavajohi S, Salehi R, Dowlatabadi R Several new acenaphtho[1,2-b]quinoxaline derivatives were prepared by the reaction of o-phenylenediamines with acenaphthenequinones. The response of different carcinoid cell lines to these compounds were evaluated by MTT (3-(4,5-dimethylthiazol-2-yl)2,5-diphenyl tetrazolium bromide) assay and trypan blue exclusion tests. The cytotoxicity of 3,4-dinitroacenaphtho[1,2-b]quinoxaline (IIId) on the tested cell lines was confirmed by both tests. Furthermore, the MTT test showed a significant difference (p < 0.05) between the cytotoxicity of this compound on malignant cell lines of Caco-2, HT-29, T47D and non malignant mouse fibroblast cell line of NIH-3T3. An apoptosis inducing effect of comp... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3100751 Fri, 18 Dec 2009 16:32:02 +0100 3100751 http://www.medworm.com/index.php?rid=3100750&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%3D19998582%26dopt%3DAbstract Authors: Setiawati E, Purnomo A, Deniati SH, Yunaidi DA, Handayani LR, Harinato G, Santoso ID The bioequivalence of two capsule formulations containing 100 mg minocycline was assessed in 12 healthy adult male and female volunteers in a crossover, randomized, single-blind study. The participating volunteers were required to fast overnight and in the next morning and were given orally one capsule of the test drug (Acnez) or one capsule of the reference drug. Blood samples were drawn immediately before taking the drug (control), and at 0.33, 0.67, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, and 60 h after drug administration. One week after the first drug administration (washout period), the procedure was repeated using the alternate drug. Plasma concentrations of the drug were determined by high p... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3100750 Fri, 18 Dec 2009 16:32:02 +0100 3100750 http://www.medworm.com/index.php?rid=3100746&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%3D19998583%26dopt%3DAbstract Authors: Chachad S, Lulla A, Malhotra G, Purandare S The study was designed to compare the rate and extent of absorption of a fixed dose combination tablet of lamivudine (CAS 134678-17-4) and stavudine (CAS 3056-17-5) with the concurrent administration of lamivudine tablet and stavudine capsule in 24 healthy volunteers under fasting conditions. The volunteers were randomly assigned to the test or reference treatment, with the two treatment periods separated by a washout period of at least 7 days. Plasma samples were analyzed for both analytes lamivudine and stavudine by a validated analytical method. Since the 90% confidence intervals for the "test/reference" mean ratio of the In-transformed pharmacokinetic variables C(max) AUC(0-t) and AUC(0-infinity) were clearly within the conventio... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=3100746 Fri, 18 Dec 2009 16:32:02 +0100 3100746 http://www.medworm.com/index.php?rid=2939228&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%3D19856789%26dopt%3DAbstract CONCLUSION: Darbepoetin alfa increases the Hgb value effectively in Japanese hemodialysis patients. Although no serious adverse events were apparent in our short-term analysis, the incidence of hypertension and excessive increase of the Hgb value must be noted. PMID: 19856789 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2939228 Thu, 29 Oct 2009 16:28:02 +0100 2939228 http://www.medworm.com/index.php?rid=2939226&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%3D19856790%26dopt%3DAbstract This study shows that both formulations were well tolerated and the test formulation can be considered a pharmaceutically and therapeutically equivalent alternative to the reference formulation. PMID: 19856790 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2939226 Thu, 29 Oct 2009 16:28:02 +0100 2939226 http://www.medworm.com/index.php?rid=2939225&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%3D19856791%26dopt%3DAbstract In this study, increasing the dosage of pravastatin was investigated to determine whether it had a clearly favorable effect on the adiponectin level in hypercholesterolemic patients. A total of 26 mild hypercholesterolemic and hypertensive patients were enrolled in this study. The patients were initially treated with pravastatin 10 mg/day for 6 months or more, and then increased to pravastatin 20 mg/day. Serum adiponectin, cholesterol fractionated components, and lipoprotein components were evaluated after 6 months. Increasing the dose of pravastatin from 10 to 20 mg/day caused the low-density lipoprotein cholesterol levels to decrease (from 130 to 104 mg/dL, p < 0.001), and thereafter the serum adiponectin levels, particularly the high-molecular-weight adiponectin levels significantly ... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2939225 Thu, 29 Oct 2009 16:28:02 +0100 2939225 http://www.medworm.com/index.php?rid=2939224&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%3D19856792%26dopt%3DAbstract Authors: Sahoo BK, Das A, Agarwal S, Bhaumik U, Bose A, Ghosh D, Roy B, Pal TK The aim of the present study was to compare the pharmacokinetics of rabeprazole (CAS 117976-89-3) and itopride (CAS 122898-67-3) after oral administration of a rabeprazole (20 mg)-itopride (150 mg) fixed dose combination (FDC) in healthy human volunteers. The bioequivalence of two formulations (test and reference) was determined in 12 healthy Indian male volunteers (age: 25.25 +/- 4.69 years; weight: 60.50 +/- 5.04 kg) in a randomized, single-dose, two-period, two-treatment crossover study. Both formulations were administered orally as a single dose, with the treatments separated by a washout period of 1 week. Rabeprazole and itopride plasma levels were determined by a validated HPLC method using UV detectio... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2939224 Thu, 29 Oct 2009 16:28:02 +0100 2939224 http://www.medworm.com/index.php?rid=2939221&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%3D19856793%26dopt%3DAbstract Authors: Marzo A, Zava D, Coa K, Dal Bo L, Ismaili S, Tavazzi S, Cantoni V Isoxsuprine (1-(4-hydroxyphenyl)-2-(1-methyl-2-phenoxyethylamino)-1-propanol, CAS 395-28-8) is a peripheral vasodilator that also stimulates beta-adrenergic receptors. It causes a direct relaxation of vascular and uterine smooth muscles and produces positive inotropic and chronotropic effects. It is widely used to arrest premature labour and miscarriage. The aim of this trial was to investigate the pharmacokinetics of isoxsuprine hydrochloride administered orally to healthy young female volunteers as an extended-release formulation at the doses of 30, 60 and 90 mg compared to 10 mg by i.m. route. A randomised, crossover, four-period, multisequence, single-dose design was adopted. Plasma and urine concentrations ... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2939221 Thu, 29 Oct 2009 16:28:02 +0100 2939221 http://www.medworm.com/index.php?rid=2939219&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%3D19856794%26dopt%3DAbstract Authors: Matsui S, Imai S, Yabuki M, Komuro S AmBisome, a liposomal formulation of amphotericin B (CAS 1397-89-3, L-AMB), shows different pharmacokinetics from the conventional formulation, amphotericin B deoxycholate (D-AMB). To characterize the clearance process of L-AMB, the form in which it exists in rat plasma, pharmacokinetics in hepatic or renal failure rats, cellular distribution in rat liver, and placental and milk transfer in rat were investigated. Furthermore, to predict the drug-drug interaction, in vitro metabolism of amphotericin B (AMB) by rat, dog and human liver S9 fraction, and effects of L-AMB on drug-metabolizing enzyme systems were investigated. L-AMB was found to exist stably as a liposomal form in rat plasma without any notable transfer to milk or fetus in rats. ... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2939219 Thu, 29 Oct 2009 16:28:02 +0100 2939219 http://www.medworm.com/index.php?rid=2939218&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%3D19856795%26dopt%3DAbstract In this study, the mean AUCt, AUCinf, Cmax, and t1/2 of azithromycin from the test drug were 4967.49 ng x h x mL(-1), 5871.74 ng x h x mL(-1), 412.14 ng/mL, and 51.32 h, respectively. The mean AUCt, AUCinf, Cmax, and t1/2 of azithromycin from the reference drug were 4276.75 ng x h x mL(-1), 5578.12 ng x h x mL(-1), 419.89 ng/mL, and 51.23 h, respectively. The median tmax of he test drug and reference drug were 3.0 h and 2.0 h, respectively. The geometric mean ratios (90% CI) of the test drug/reference drug for azithromycin were 101.56% (86.61-119.08%) for AUCt, 101.27% (84.97-120.70%) for AUCinf, and 97.78% (84.50-113.16%) for Cmax. Based on this study, it was concluded that the two azithromycin tablets (test and reference drug) were bioequivalent in terms of the rate and extent of absorpt... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2939218 Thu, 29 Oct 2009 16:28:02 +0100 2939218 http://www.medworm.com/index.php?rid=2939217&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%3D19856796%26dopt%3DAbstract The objective of this article was to check the safety of the substitution of theophylline by means of a comparative evaluation of bioequivalence studies carried out on theophylline slow-release preparations. A systematic literature search was carried out in the MEDLINE database. The search terms used were combinations of the following key words: theophylline, generics, bioequivalence, substitution, brand and non-brand. In addition, a manual search was performed in the reference lists of the relevant articles. Only articles that were published between January 1, 1988 and August 30, 2008 were to be included. Five studies conformed to the inclusion and exclusion criteria. Two of the studies came to the conclusion that the preparations analysed were bioequivalent. In the remaining three studie... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2939217 Thu, 29 Oct 2009 16:28:02 +0100 2939217 http://www.medworm.com/index.php?rid=2880126&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%3D19813460%26dopt%3DAbstract Authors: Zou Q, Zhan Y, Ge Z, Wei P, Ouyang P A sensitive and selective liquid chromatographic-mass spectrometric (LC-MS) method for the determination of amlodipine (CAS 88150-42-9) in human plasma has been developed. Sample preparation was based on liquid-liquid extraction using NaOH and cyclohexane. Analytical determination was carried out on a C18 column interfaced with a single quadrupole mass spectrometer. Positive electrospray ionization was employed as the ionization source. The mobile phase was 10 mmol/L ammonium acetate solution-methanol (30:70, v/v) at the flow rate of 0.2 mL/min. The method was linear in the concentration range of 0.2-20 ng/mL. The lower limit of quantification was 0.2 ng/mL. Amlodipine was sensitive to UV light. The method was validated in terms of accuracy... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2880126 Sun, 11 Oct 2009 05:10:03 +0100 2880126 http://www.medworm.com/index.php?rid=2880125&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%3D19813461%26dopt%3DAbstract This study was conducted in order to assess the bioequivalence of a test and reference tablet formulation containing 10 mg of ramipril ((1S,5S,7S)-8-[(2S)-2-[[(1S)-1-ethoxycarbonyl-3-phenyl-propyl]amino]propanoyl]-8-azabicyclo[3.3.0] octane-7-carboxylic acid, CAS 87333-19-5). Forty healthy male and female volunteers were treated in a single-centre randomised, single-dose, open-label, 2-way crossover study, with a washout period of 35 days between treatments. Plasma samples were collected up to 168 h post-dosing for the determination of ramipril and its active metabolite, ramiprilat, by LC-MS/MS. The evaluation of bioequivalence was based on the following pharmacokinetic parameters that were calculated by standard non-compartmental methods: the area under the plasma concentration-time curve... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2880125 Sun, 11 Oct 2009 05:10:03 +0100 2880125 http://www.medworm.com/index.php?rid=2880124&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%3D19813462%26dopt%3DAbstract This study was designed to evaluate the bioequivalence of two formulations of alendronate (CAS 121268-17-5) 70 mg (test formulation, alendronate 70 mg tablets, vs. the reference formulation) in 80 healthy volunteers under fasting conditions. The trial followed an open, randomized, crossover design with a washout period of 28 days. Urine samples were collected up to 48 h post-dose, and the concentrations of alendronate were determined by HPLC. The mean Ae(0-48) was (mean +/- SD) 152.15 +/- 136.09 microg for the reference formulation and 150.37 +/- 126.20 microg for the test formulation, while the mean Rmax was 53.33 +/- 41.53 microg/h and 55.85 +/- 49.57 microg/h, respectively. No significant differences in pharmacokinetic parameters between the two formulations were found. The 90% confiden... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2880124 Sun, 11 Oct 2009 05:10:03 +0100 2880124 http://www.medworm.com/index.php?rid=2880123&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%3D19813463%26dopt%3DAbstract CONCLUSIONS: The piroxicam patch is effective in the treatment of lumbar osteoarthritis and has demonstrated to be well tolerated and it improves patients compliance. The piroxicam patch offers a comparable alternative to the marketed piroxicam cream for the treatment of lumbar osteoarthritis with the advantage of a better compliance with the once a day application of the patch compared to three daily applications for the piroxicam cream. PMID: 19813463 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2880123 Sun, 11 Oct 2009 05:10:03 +0100 2880123 http://www.medworm.com/index.php?rid=2880122&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%3D19813464%26dopt%3DAbstract In conclusion, it appears necessary to pay attention to the kind of NSAIDs reported as the cause of hypersensitivity in anamnesis, because it must be considered a successful guide in choosing the alternative drug to administer to the patient during the challenge test. PMID: 19813464 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2880122 Sun, 11 Oct 2009 05:10:03 +0100 2880122 http://www.medworm.com/index.php?rid=2880121&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%3D19813465%26dopt%3DAbstract Authors: Abadi AH, Abouel-Ella DA, Ahmed NS, Gary BD, Thaiparambil JT, Tinsley HN, Keeton AB, Piazza GA Two closely related series of novel beta-carboline derivatives, electronically similar to tadalafil (CAS 171596-29-5), were synthesized and evaluated for their inhibitory effects upon phosphodiesterase 5 (PDE5) and phosphodiesterase 11 (PDE11) and their in vitro tumor cell growth inhibitory activity versus HT29 colorectal carcinoma cell line. Interestingly, some of the synthesized compounds showed growth inhibitory properties that appear to be associated with their ability to inhibit PDE5. Moreover, the PDE5 inhibition seems relevant to the stereochemical aspects of the compounds. PMID: 19813465 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2880121 Sun, 11 Oct 2009 05:10:03 +0100 2880121 http://www.medworm.com/index.php?rid=2880120&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%3D19813466%26dopt%3DAbstract Authors: Grabowski T, Swierczewska A, Borucka B, Sawicka R, Sasinowska-Motyl M, Gumułka SW A HPLC/mass spectrometry method for the estimation of itraconazole (CAS 84625-61-6, ITR) and its active metabolite hydroxyitraconazole (CAS 112559-91-8, HOX) in human plasma was developed. Terconazole (CAS 67915-31-5) was used as an internal standard. The analytical method was fully validated according to FDA and EMEA requirements. The accuracy and precision of the developed method was satisfactory and stability studies showed an acceptable variation (below 15%) of ITR and HOX concentrations when the samples were stored frozen at -75 degrees C for 95 days. The developed method was successfully used for a comparative 2 x 2 period, crossover bioequivalence study of two preparations of ITR (It... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2880120 Sun, 11 Oct 2009 05:10:03 +0100 2880120 http://www.medworm.com/index.php?rid=2880119&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%3D19813467%26dopt%3DAbstract Authors: Zakeri-Milani P, Valizadeh H, Ghanbarzadeh S, Nemati M The aim of the present study was to compare the pharmacokinetics and bioavailability of two commercial brands of clarithromycin (CAS 81103-11-9) suspensions in healthy male Iranian volunteers. In an open label, single-dose, randomized study with a crossover design an equivalent 500-mg clarithromycin suspension was given orally to each of 24 subjects as a single dose on two treatment days. The treatment periods were separated by a one-week washout period. Blood samples were drawn at different time points and the separated plasma was kept frozen at -20 degrees C for subsequent analysis. The plasma concentrations of the drug were analyzed by a rapid and sensitive HPLC method with UV detection. Mean maximum serum concentration... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2880119 Sun, 11 Oct 2009 05:10:03 +0100 2880119 http://www.medworm.com/index.php?rid=2769075&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%3D19728559%26dopt%3DAbstract Authors: Srinivas NR A close scrutiny of deployment of the present day home medicines has shown increased indulgence of antacids as a household remedy. While such household interventions are considered innocuous, it could trigger potential drug-drug interaction(s), if the subject is taking other prescription medicine(s). Examination of the literature indicated that co-administration of antacids may have the potential to cause therapy failures due to reduced oral bioavailability of several drugs. Additionally, fortified foods and beverages with mineral supplement may also have the potential to reduce the bioavailability of oral drugs. On the basis of this review a number of drugs displayed reduced oral bioavailability in the presence of antacids. However, almost one third of the reviewe... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2769075 Sun, 06 Sep 2009 01:56:03 +0100 2769075 http://www.medworm.com/index.php?rid=2769074&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%3D19728560%26dopt%3DAbstract Authors: Borges NC, Mazuqueli A, Moreno RA, Astigarraga RB, Sverdloff CE, Galvinas PA, Sampaio MR, da Silva WM A specific, fast and sensitive high performance liquid chromatography (HPLC) coupled to atmospheric pressure photoionization (APPI) tandem mass spectrometric (LC-MS/MS) assay was developed for the determination of cyproterone (CYP) acetate (CAS 427-51-0) in human plasma. The retention times were 3.26 and 2.90 min for CYP acetate and its internal standard (I. S.) finasteride (FIN), respectively. The overall mean recovery, using liquid/liquid extraction, was found to be 109.0, 107.7 and 100.3%, for low, medium and high concentrations, respectively. Calibration curves were linear in the concentration range of 0.1-50.0 ng/ml, and the lower limit of quantification (LLOQ) was 0.1 ng... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2769074 Sun, 06 Sep 2009 01:56:03 +0100 2769074 http://www.medworm.com/index.php?rid=2769073&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%3D19728561%26dopt%3DAbstract CONCLUSION: Based on the obtained results the two fexofenadine formulations are considered to be equivalent. PMID: 19728561 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2769073 Sun, 06 Sep 2009 01:56:03 +0100 2769073 http://www.medworm.com/index.php?rid=2769072&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%3D19728562%26dopt%3DAbstract Authors: Chhabria MT, Shishoo CJ, Vaghela DK, Patel SM, Satia MC A series of 5-carbethoxy-4-chloro-6-(substituted amino)pyrimidines was designed on the basis of its good 3-dimensional structural similarity with mefenamic acid (CAS 61-68-7), a well known anti-inflammatory drug. Synthesis of some 5-carbethoxy-4-chloro-6-(substitutedamino)pyrimidines has been achieved by cyclization of N-(cyanovinyl)formamidine intermediate in the presence of dry HCl. Target compounds were evaluated for their analgesic and anti-inflammatory potential by known experimental models. Some of the compounds emerged as more potent analgesic and anti-inflammatory agents than the standard drug diclofenac sodium (CAS 15307-79-6). A very low ulcer index was observed with the most potent compound. PMID: 19728562 ... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2769072 Sun, 06 Sep 2009 01:56:03 +0100 2769072 http://www.medworm.com/index.php?rid=2769071&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%3D19728563%26dopt%3DAbstract Authors: Gökçe M, Colak MS, Küpeli E, Sahin MF For reducing gastrointestinal toxicity associated with non-steroidal anti-inflammatory drugs (NSAIDs) a variety of 6-phenyl/(4-methylphenyl)-3(2H)-pyridazinon-2-propionamide were synthesized. The structures of these new pyridazinone derivatives were confirmed by their IR, 1H-NMR spectra and elementary analysis. All the new compounds were tested in vivo for their analgesic and anti-inflammatory activities. The analgesic activity of the test compounds was determined by phenylbenzoquinone-induced writhing assay and the anti-inflammatory activity was evaluated by the carrageenan-induced rat paw edema model. 6-Phenyl-3(2H)-pyridazinon-2-yl-[4-(4-fluorophenyl)piperazinyl] propanamide IVa-3 was the most active one among the synthes... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2769071 Sun, 06 Sep 2009 01:56:03 +0100 2769071 http://www.medworm.com/index.php?rid=2769070&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%3D19728564%26dopt%3DAbstract Authors: Gul M, Mete E, Atalay M, Arik M, Gul HI 1-Aryl-3-buthylamino-1-propanone hydrochloride type mono Mannich bases were synthesized and their cytotoxicity was tested against transformed human T-lymphocytes (Jurkat cells) and rat skeletal muscle derived myoblasts (L6 cells). Aryl part was changed as phenyl in 1, 4-methylphenyl in 2, 4-chlorophenyl in 3, 4-fluorophenyl in 4, 4-bromophenyl in 5, 4-hydroxyphenyl in 6, 2-acethylthiophene in 7. Of the compounds synthesized, 2, 5, 6, and 7 are reported for the first time. Compounds 1-7 had 3.16, 3.13, 3.35, 2.87, 4.17, 2.60, and 3.04 times higher cytotoxic potency than the reference compound 5-fluorouracil (CAS 51-21-8) against Jurkat cells, respectively. Compounds 1, 3, 4, 5, 6, and 7 had 1.22, 1.46, 1.59, 2.18, 1.24, and 1.45 times hig... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2769070 Sun, 06 Sep 2009 01:56:03 +0100 2769070 http://www.medworm.com/index.php?rid=2769069&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%3D19728565%26dopt%3DAbstract CONCLUSION: Intake of AQ and AS with a high fat meal resulted in (1) a statistically significant increase in blood levels of AQ and DSA which may affect the safety and tolerability of the study drugs and (2) a decrease in AS and DHA blood levels which may affect efficacy. These results suggest that the fixed-dose combination should not be administered with a high-fat meal. PMID: 19728565 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2769069 Sun, 06 Sep 2009 01:56:03 +0100 2769069 http://www.medworm.com/index.php?rid=2769068&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%3D19728566%26dopt%3DAbstract CONCLUSION: If a reliable extrapolation is impossible, the cut MRT can be estimated only from measured concentrations. However, the cropping and the truncation maneuvers should be considered simultaneously to counterbalance the cutoff errors. PMID: 19728566 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2769068 Sun, 06 Sep 2009 01:56:03 +0100 2769068 http://www.medworm.com/index.php?rid=2654755&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%3D19634508%26dopt%3DAbstract Authors: Klotz U Acid secretion or intragastric pH play a very important role in the pathophysiology of acid-related disorders such as peptic ulcer (PU), gastrooesophageal reflux disease (GERD) or nonsteroidal anti-inflammatory drug (NSAID)-induced gastrointestinal lesions. Proton pump inhibitors (PPIs) represent the most potent/effective antisecretory drugs for these indications. For the selection among the various agents (omeprazole/esomeprazole (CAS 73590-58-6/119141-88-7), pantoprazole (CAS 102625-70-7), lansoprazole (CAS103577-45-3), rabeprazole (CAS 117976-83-3)) some features of their pharmacokinetic (PK) and pharmacodynamic (PD) properties should be considered as the clinical outcome depends on systemic drug exposure (PK) and elevation of intragastric pH about certain threshold... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2654755 Fri, 31 Jul 2009 06:16:02 +0100 2654755 http://www.medworm.com/index.php?rid=2654754&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%3D19634509%26dopt%3DAbstract In this study, analysis on a like-for-like basis of the L- and N-type calcium channel-inhibitory activity of typical dihydropyridine-type calcium-channel blockers (DHPs) was performed. Moreover, to understand the differences of N-type calcium channel inhibition among DHPs, the binding of DHPs to the channel was investigated by means of hypothetical three-dimensional pharmacophore modeling using multiple calculated low-energy conformers of the DHPs. All of the tested compounds, i.e. cilnidipine (CAS 132203-70-4), efonidipine (CAS 111011-76-8), amlodipine (CAS 111470-99-6), benidipine (CAS 85387-35-5), azelnidipine (CAS 123524-52-7) and nifedipine (CAS 21829-25-4), potently inhibited the L-type calcium channel, whereas only cilnidipine inhibited the N-type calcium channel (IC50 value: 51.2 n... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2654754 Fri, 31 Jul 2009 06:16:02 +0100 2654754 http://www.medworm.com/index.php?rid=2654753&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%3D19634510%26dopt%3DAbstract CONCLUSIONS: Measurement of CBS concentrations should not be a reliable one for the bioequivalence assessment, due to very low concentrations, very small and variable values of AUC and high intra-subject variability. Thus, bioequivalence evaluation should be based on CCA determination. In the presented study evaluation based on CCA unequivocally and with the proper power confirmed the bioequivalence between the investigated clopidogrel products. PMID: 19634510 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2654753 Fri, 31 Jul 2009 06:16:02 +0100 2654753 http://www.medworm.com/index.php?rid=2654752&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%3D19634511%26dopt%3DAbstract CONCLUSION: While both products were bioequivalent in terms of the rate and extent of absorption, the present study also confirmed a high variability for clopidogrel suggesting high volunteer numbers in bioequivalence trials. PMID: 19634511 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2654752 Fri, 31 Jul 2009 06:16:02 +0100 2654752 http://www.medworm.com/index.php?rid=2654751&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%3D19634512%26dopt%3DAbstract CONCLUSIONS: IPC supplementation for eight months yielded significant improvements in cognitive function and scholastic performance in Indian adolescents with and without iron deficiency and anemia. PMID: 19634512 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2654751 Fri, 31 Jul 2009 06:16:02 +0100 2654751 http://www.medworm.com/index.php?rid=2654750&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%3D19634513%26dopt%3DAbstract Authors: Ahlawat P, Srinivas NR Allometry has been extensively used in the modern day drug development scenario to predict the human relevant parameters (clearance, Cl, and volume of distribution at steady state, Vss) from animal data. The applicability of allometry in the prediction of human parameters for irinotecan (CAS 97682-44-5), an important topoisomerase I inhibitor, has been retrospectively investigated. Literature pharmacokinetic data has been gathered for both irinotecan and its main metabolite, SN-38 (CAS 86639-52-3), from several animal species. The corresponding human parameters were predicted using allometry (Cl and Vss for irinotecan; Cl/F for SN-38). Although irinotecan has a complex metabolism and disposition profile, it appeared that simple allometry predicted satisf... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2654750 Fri, 31 Jul 2009 06:16:02 +0100 2654750 http://www.medworm.com/index.php?rid=2654749&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%3D19634514%26dopt%3DAbstract Authors: Schneider B The repetition of animal experiments requires justification according to the German Animal Protection Act (Tierschutzgesetz). On the other hand, repetition of experiments is considered necessary for the improvement of the precision and reliability of the results. In this paper it is shown that such improvement is not achieved by a repetition of the experiment but by repeated inclusion of animals into the experiment. The more animals are included, the more precisely and reliably the results can be generalized to further situations. The number of animals necessary for a proposed precision can be determined with statistical methods. The basic ideas are explained in the paper and demonstrated with two examples. In long term experiments the precision can be improved, if... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2654749 Fri, 31 Jul 2009 06:16:02 +0100 2654749 http://www.medworm.com/index.php?rid=2531482&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%3D19402340%26dopt%3DAbstract Authors: Di Stilo A, Chegaev K, Lazzarato L, Fruttero R, Gasco A, Rastaldo R, Cappello S Nitric oxide (NO) donor antioxidants are a class of polyvalent drugs which is the focus of great interest today. They are potentially useful for the treatment of many forms of cardiovascular diseases, including the myocardial ischemia/reperfusion (I/R) damage which seems to be due to both a burst of reactive oxygen species (ROS) and a reduced release of NO during reperfusion. In this paper the results of a study on the ability of new NO-donor antioxidants containing the phenol vitamin E substructure and furoxan moiety to attenuate I/R damage are reported. The compounds under study are obtained by combining the phenol moiety (6-hydroxy-2,2,5,7,8-pentamethylchroman) present in vitamin E with differen... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2531482 Sat, 27 Jun 2009 15:25:03 +0100 2531482 http://www.medworm.com/index.php?rid=2531481&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%3D19402341%26dopt%3DAbstract Authors: Juárez Olguín H, Flores Pérez C, Ramírez Mendiola B, Barranco Garduño L, Sandoval Ramírez E, Flores Pérez J Propafenone (CAS 34183-22-7) is an effective antiarrhythmic drug used in children, although in some countries no specific pediatric formulation is available. The aim of this study is to compare the relative bioavailability of a magistral (MAG) preparation of propafenone versus its commercial (COM) presentation in a group of 16 Mexican healthy volunteers. Bioavailability was determined after crossover administration of the drugs, through a randomized two-phase trial. All volunteers had normal hepatic and renal functions, determined clinically at the beginning of the study, and received 150 mg of either COM (tablets) or MAG (suspension). ... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2531481 Sat, 27 Jun 2009 15:25:03 +0100 2531481 http://www.medworm.com/index.php?rid=2531480&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%3D19402342%26dopt%3DAbstract Authors: Sun J, Jiao H, Tian Y, Zhang Z, Chen Y A sensitive, selective and simple high performance liquid chromatographyelectrospray ionization-mass spectrometry (HPLC-ESI-MS) was developed and validated for the quantification of ticlopidine hydrochloride (CAS 53885-35-1) in human plasma using loratadine (CAS 79794-75-5) as internal standard (IS). Following liquid-liquid extraction, the analyte and the IS were extracted from plasma samples by n-hexane:isopropanol (95:5, v/v), separated by HPLC on a commercially available column (150 mm x 2.0 mm ID, 5 microm) with a mobile phase of acetonitrile: 10 mmol/L ammonium acetate buffer solution (85:15, v/v) and analyzed on a quadrupole mass spectrometer with ESI interface operating in the positive-ion mode. The correlation coefficient of the c... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2531480 Sat, 27 Jun 2009 15:25:03 +0100 2531480 http://www.medworm.com/index.php?rid=2531479&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%3D19402343%26dopt%3DAbstract In this study, 7,8-dihydroxy-3-(4-methylphenyl) coumarin (DHMPC), a new coumarin derivative, was tested for the first time to determine whether it had any antioxidant and lipid lowering effects. Hypercholesterolemia was induced by feeding rats with a high cholesterol diet for 17 days. The lipid lowering and antioxidant effects of DHMPC were compared with those of hesperidin (CAS 520-26-3) and rutin (CAS 153-18-4), which have been pharmacologically determined as potential lipid lowering and antioxidant agents. DHMPC significantly decreased total cholesterol levels but not as efficient as hesperidin. When the ratios of high density lipoprotein-cholesterol (HDL-cholesterol) to total cholesterol were evaluated, the most significant changes were observed in DHMPC and rutin treatments. The resul... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2531479 Sat, 27 Jun 2009 15:25:03 +0100 2531479 http://www.medworm.com/index.php?rid=2531478&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%3D19402344%26dopt%3DAbstract Authors: Allegrini A, Nuzzo L, Zucchelli M, Scaringi AT, Felaco S, Giangreco D, Pavone D, Toniato E, Mezzetti A, Martinotti S, Comuzio S, Di Grigoli M A fast, specific, accurate, precise and reproducible high-performance liquid chromatography (HPLC) method with diode-array detector (DAD) was developed and validated for the determination of ketoprofen (CAS 22071-15-4) in human plasma using flubiprofen (CAS 5104-49-4) as an internal standard. The chromatographic separation was achieved on an onyx monolithic C18 (100 x 4.6 mm) analytical column with an isocratic mobile phase consisting of acetonitrile/potassium dihydrogen phosphate (KH2PO4) 0.01 M, (40:60, v/v) adjusted to pH 3.5. The flow was set at 5 ml x min(-1) and the wavelength at 254 nm. The total analysis time was less than 5 min.... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2531478 Sat, 27 Jun 2009 15:25:03 +0100 2531478 http://www.medworm.com/index.php?rid=2531477&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%3D19402345%26dopt%3DAbstract In conclusion, the present observations indicated that erianin plasma concentrations were clearly dose-proportional for the dose range studied. There was no gender difference in pharmacokinetics for erianin in male and female dogs. PMID: 19402345 [PubMed - indexed for MEDLINE] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2531477 Sat, 27 Jun 2009 15:25:03 +0100 2531477 http://www.medworm.com/index.php?rid=2531476&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%3D19402346%26dopt%3DAbstract Authors: Olschläger V, Schrader A, Hockertz S Cell lines present a valuable tool for in vitro assessment of skin damage caused by application of cosmeticals or pharmaceuticals. They form a reproducible test system under controllable test conditions and, in many cases, can be used as alternatives to animal testing in order to assess the compatibility of drugs or cosmetics and human skin. Yet, it can not necessarily be assumed that the behavior of cultured cells, when treated with different substances, is exactly consistent with the behavior of cells being part of a live organism. Becoming immortal, cells exhibit changes in genotype and/or phenotype, possibly resulting in modified reactions to external influences. Therefore, to obtain results close to in vivo studies, it seems appar... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2531476 Sat, 27 Jun 2009 15:25:03 +0100 2531476 http://www.medworm.com/index.php?rid=2531475&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%3D19517891%26dopt%3DAbstract Authors: Srinivas NR In recent years, the assessment of metabolite pharmacokinetic data has been increasingly on the rise in several types of clinical pharmacology studies including bioavailability/bioequivalence assessments of drug formulations. While the importance of pharmacokinetic data of metabolite(s) are well accepted, there appears to be reluctance on the part of scientific community to use such data in a prospective manner in the establishment of bioavailability/bioequivalence of marketed products and/or drugs in development. This review highlights the current trends that suggest that metabolite(s) data are being considered with or without the parent pharmacokinetic data in bioavailability/bioequivalence studies with numerous case studies. Also, some useful considerations from... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2531475 Sat, 27 Jun 2009 15:25:03 +0100 2531475 http://www.medworm.com/index.php?rid=2531474&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%3D19517892%26dopt%3DAbstract Authors: Das A, Bhaumik U, Chakrabarty US, Sarkar AK, Ghosh A, Bose A, Chatterjee B, Pal TK An improved HPLC method was developed and validated for the determination of concentration of amisulpride (CAS 71675-85-9) in human plasma, an attempt to compare the bioavailability of two amisulpride tablet formulations (reference and test) containing 200 mg of amisulpride. Both the formulations were administered orally as a single dose, separated by washout period of 1 week. This HPLC method validated by examining the precision and accuracy for the inter-day and intra-day runs in a linear concentration range of 50-1200 ng/ml. Bioequivalence of two formulation were determined on 12 healthy Indian male volunteer in a single-dose, two-period, two-sequence, two-treatment crossover study. The conte... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2531474 Sat, 27 Jun 2009 15:25:03 +0100 2531474 http://www.medworm.com/index.php?rid=2531473&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%3D19517893%26dopt%3DAbstract Authors: Joti JJ, Nahar K, Hasan A, Azad MA, Ullah MA, Islam SM, Hasnat A Omeprazole (CAS 73590-58-6) effectively suppresses the gastric acid secretion in the parietal cells of the stomach and is a widely prescribed proton pump inhibitor in Bangladesh. The increasing number of omeprazole containing products available in the market raises questions of therapeutic equivalence and/or generic substitution which are yet to be conducted with Bangladeshi population. The aim of the study is to assess the bioequivalence and pharmacokinetic properties of two oral formulations of 20 mg omeprazole capsule, the reference product and Omep-20 as test product using serum data. The randomized, two-way crossover study was conducted on 24 healthy male subjects in compliance with the Declaration of Helsin... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2531473 Sat, 27 Jun 2009 15:25:03 +0100 2531473 http://www.medworm.com/index.php?rid=2531472&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%3D19517894%26dopt%3DAbstract This study evaluates possible differences between iron sucrose and ISS preparations on haemodynamic and oxidative stress markers in normal rats. 60 male and 60 female Sprague Dawley rats were divided into four groups and assigned to receive commercially available ISS test 1, ISS test 2, reference or isotonic saline solution (control). A single i.v. dose of iron (40 mg/kg) or saline (equivalent volume) was administered after 24 h and every 7 days for 4 weeks. Blood samples were collected for biological assessment of haemoglobin (Hb), serum iron and percentage transferrin saturation (TSAT), and urine samples were collected to investigate creatinine clearance and proteinuria. Animals were sacrificed after receiving an i.v. dose on days 1, 7 and 28, and kidney, liver, and heart homogenates wer... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2531472 Sat, 27 Jun 2009 15:25:03 +0100 2531472 http://www.medworm.com/index.php?rid=2531471&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%3D19517895%26dopt%3DAbstract CONCLUSION: These results indicate that the two formulations of dexamethasone are bioequivalent and thus may be prescribed interchangeably. PMID: 19517895 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2531471 Sat, 27 Jun 2009 15:25:03 +0100 2531471 http://www.medworm.com/index.php?rid=2531470&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%3D19517896%26dopt%3DAbstract Authors: Berk B, Erol DD, Kupeli E, Yesilada E The carboxylic acid group of the anti-inflammatory drug, (S)-2-(6-methoxynaphthalen-2-yl) propanoic acid, naproxen (CAS 22204-53-1) was reacted with the substituted ethylamine derivatives to form (S)-2-(6-methoxynaphthalen-2-yl)-N-substituted ethyl propanamides by using N,N'-dicyclohexyl carbodiimide (DCC) and 4-(dimethylamino)pyridine (DMAP). Anti-inflammatory and analgesic activities of the compounds were assessed in vivo by carrageenan-induced hind paw edema and p-benzoquinone induced abdominal contraction tests in mice, respectively. In addition, the ulcerogenic properties of the new compounds were evaluated, and compared to that of naproxen. Among the newly synthesized compounds, compound 2f showed the highest analgesic and antiinflam... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2531470 Sat, 27 Jun 2009 15:25:03 +0100 2531470 http://www.medworm.com/index.php?rid=2531469&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%3D19517897%26dopt%3DAbstract Authors: Ahmadi A, Khalili M, Abbassi S, Javadi M, Mahmoudi A, Hajikhani R Phencyclidine (1-(1-phenylcyclohexyl) piperidine; CAS 956-90-1; PCP, I) has shown analgesic effects. Some of its derivatives have been synthesized and their biological properties have been studied. In this work, new methyl and methoxy hydroxyl derivatives of phencyclidine were synthesized and the analgesic effects of this compounds [(1-[1-(4-methylphenyl) (cyclohexyl)] 4-piperidinol, II), (1-[1-(4-methoxyphenyl) (cyclohexyl)] 4-piperidinol, III)] were studied using tail immersion test on rats and compared to PCP. The results showed that, II can produce more analgesic effects in the tail immersion test (as a model of acute thermal pain) in comparison to the PCP with a marked significant increase in tail immersion... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2531469 Sat, 27 Jun 2009 15:25:03 +0100 2531469 http://www.medworm.com/index.php?rid=2531468&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%3D19517898%26dopt%3DAbstract Authors: Pardo Andreu GL, Inada NM, Pellón RF, Docampo ML, Fascio ML, D'Accorso NB, Vercesi AE An intensive effort has been directed toward finding alternative drugs for treatment of Chagas' disease, caused by Trypanosoma cruzi (T. cruzi), and prophylaxis of blood in endemic areas. The preparation and in vitro evaluation as potential anti-protozoal agent of (2E)-N-(1,3-benzothiazol-2-yl)-3-(2,5-dimethoxyphenyl)-2-propenamide (CAD-1) is presented. The results show that 0.05 mM CAD-1 induced 58.1% of T. cruzi epimastigotes death; mainly by apoptosis. The diminution in the transmembrane mitochondrial electrical potential together with the increase in the intracellular generation/accumulation of reactive oxygen species, suggest the parasites mitochondria as the main target for CAD-1-i... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2531468 Sat, 27 Jun 2009 15:25:03 +0100 2531468 http://www.medworm.com/index.php?rid=2531467&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%3D19537521%26dopt%3DAbstract Authors: Petersen KU Poor or lacking responses to the antiplatelet effect of clopidogrel (CAS 113665-84-2) and the attendant clinical consequences have been a growing concern for several years. This debate has been invigorated by reports suggesting the ability of inhibitors of the cytochrome P450 isoenzyme, CYP 2C19, to interfere with clopidogrel efficacy. In the present review, the mechanisms underlying clopidogrel failure are analyzed, based on an overview of the current perceptions of drug metabolism by the CYP superfamily of enzymes, and paying particular attention to the relevant properties of the newly introduced thienopyridine, prasugrel (CAS 150322-43-3). Convincing evidence indicates that the vulnerability of clopidogrel lies in its mode of activation. In a two-step sequence, ... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2531467 Sat, 27 Jun 2009 15:25:03 +0100 2531467 http://www.medworm.com/index.php?rid=2531466&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%3D19537522%26dopt%3DAbstract Authors: Li J, Tian Y, Zhang ZJ, Wang N, Ren X, Chen Y The aim of the present study was to compare the bioavailability of escitalopram (CAS 128196-01-0) from two escitalopram oxalate (CAS 219861-08-2) tablets (escitalopram 10 mg tablet as test preparation and 10 mg tablet commercially available original tablet of the drug as reference preparation) in 20 Chinese healthy male volunteers, aged between 19 and 27. The study was conducted according to an open, randomized, single blind, 2-way crossover study design with a wash-out phase of 14 d. Blood samples for pharmacokinetic profiling were taken up to 156 h post-dose, and escitalopram plasma concentrations were determined with a validated liquid chromatography-electrospray ionization-mass spectrometry (LC-ESI-MS) method. Maximum plasma co... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2531466 Sat, 27 Jun 2009 15:25:03 +0100 2531466 http://www.medworm.com/index.php?rid=2531465&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%3D19537523%26dopt%3DAbstract Authors: Groenewoud G, Potgieter L, Meyer B The bioavailability of two rilmenidine tablet formulations was compared in healthy male (17) and female (8) subjects, aged 18 to 36 years, during a laboratory-blind, randomized, two-treatment, two-period, cross-over study under fasting conditions. In each treatment phase subjects received a single dose of 1.544 mg rilmenidine dihydrogen phosphate (CAS 85409-38-7), equivalent to 1 mg rilmenidine (CAS 54187-04-1). Consecutive dosing was separated by a drug-free wash-out period of 7 d. Following each dosing, serial venous blood samples were collected over a period of 48 h for the determination of plasma rilmenidine concentrations by means of a validated LCMS/MS method. The most frequently reported drug-related adverse events were dizziness and h... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2531465 Sat, 27 Jun 2009 15:25:03 +0100 2531465 http://www.medworm.com/index.php?rid=2531464&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%3D19537524%26dopt%3DAbstract CONCLUSION: In this study bioequivalence could be demonstrated with respect to rate and extent of methocarbamol exposure. PMID: 19537524 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2531464 Sat, 27 Jun 2009 15:25:03 +0100 2531464 http://www.medworm.com/index.php?rid=2531463&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%3D19537525%26dopt%3DAbstract Authors: Chhabria MT, Patel VT, Rajan KS, Brahmkshatriya PS A series of 4-amino-2-(substituted)-5-(substituted)aryl-6-[(substituted)aryl)-amino]pyrimidines was designed based on the triangular pharmacophoric requirements for histamine H1-receptor antagonists. The designed molecules were synthesized by condensation of arylacetonitriles with respective arylisothiocyanates to form corresponding acrylonitriles followed by cyclocondensation with carboxamidines to afford substituted pyrimidines. All compounds were screened for their histamine H1-receptor antagonistic activity using the model "Inhibition of the isotonic contraction induced by histamine on isolated guinea pig ileum". Target compounds were also evaluated for their sedative potential as well as their anticholinergic activities a... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2531463 Sat, 27 Jun 2009 15:25:03 +0100 2531463 http://www.medworm.com/index.php?rid=2531462&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%3D19537526%26dopt%3DAbstract Authors: Yoshimatsu A, Nan-ya K, Miki I Granulocyte colony-stimulating factor (G-CSF) is known to mobilize stem cells to various organs and that it participates in tissue regeneration. Effect of the recombinant human G-CSF nartograstim (CAS 134088-74-7) was tested on elastase-induced emphysema. Porcine pancreas elastase (PPE) was administered intratracheally to male Sprague-Dawley rats to induce parenchymal destruction which was assessed by measuring the mean linear intercept (Lm) in tissue sections as an indicator of air space size. Lung alveoli were destructed and Lm value was significantly increased 2 weeks after PPE instillation. Increase in Lm was sustained for 8 weeks after PPE instillation. Two weeks after PPE instillation, 100 and 200 microg/kg of G-CSF injected for 5 d, follow... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2531462 Sat, 27 Jun 2009 15:25:03 +0100 2531462 http://www.medworm.com/index.php?rid=2531461&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%3D19537527%26dopt%3DAbstract Authors: Sharma SS, Srinivasan SK, Krishnamoorthy S, Kaushal AM, Bansal AK Safety pharmacological studies need to be performed according to ICH S7A Guidelines for finished formulations that substantially alter the pharmacokinetics and/or pharmacodynamics of the active substance in comparison to formulations previously tested (i. e. through active excipients such as penetration enhancers, liposomes, and other changes such as polymorphous system). In the present study, amorphous formulation of celecoxib (CAS 169590-42-5), a new patented formulation with altered pharmacokinetic profile was investigated in comparison with the standard crystalline celecoxib (CEL) for its undesirable pharmacodynamic effects using certain safety pharmacological studies. The effects of the new formulation on v... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2531461 Sat, 27 Jun 2009 15:25:03 +0100 2531461 http://www.medworm.com/index.php?rid=2531460&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%3D19537528%26dopt%3DAbstract Authors: Chachad S, Lulla A, Malhotra G, Purandare S The study was designed to compare the rate and extent of absorption of two fixed dose combination tablet formulations of lopinavir (CAS 192725-17-0) and ritonavir (CAS 155213-67-5). This bioequivalence study was conducted using a standard preparation as reference and a generic alternative as test in 72 adult healthy volunteers within 18-45 years of age who received a single dose of the test or reference product under fasting conditions. A washout period of 10 d was maintained between period I and period II dosing. After dosing, blood samples were collected from 0 h (pre-dose) to 72 h postdose administration. Lopinavir and ritonavir were quantified using a validated LC-MS/MS method. The data obtained for each subject was evaluated for... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2531460 Sat, 27 Jun 2009 15:25:03 +0100 2531460 http://www.medworm.com/index.php?rid=2306829&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%3D19338136%26dopt%3DAbstract Authors: Lattmann E, Lattmann P, Boonprakob Y, Airarat W, Singh H, Offel M, Sattayasai J Oxazepam (CAS 604-75-1) 4a served as building block in the synthesis of substituted 3-amino-1,4-benzodiazepines, which were subsequently tested in various CNS animal models. The hydroxy group of oxazepam was either activated as a chloride (Method A) or as a phosphor-oxy derivative (Method B) giving the desired 3-amino-1,4-benzodiapines 6a-6r in high yields with primary and secondary amines in a typical nucleophilic substitution reaction. Eighteen 3-substituted 1,4-benzodiazepines were prepared and served as new chemical entities and for lead structure discovery. The mixed cholecystokinin (CCK) antagonist 6e showed anxiolytic and antidepressant effects from 10 microg/kg in mice in the elevated x-maz... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2306829 Tue, 07 Apr 2009 13:32:38 +0100 2306829 http://www.medworm.com/index.php?rid=2306828&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%3D19338137%26dopt%3DAbstract Authors: Pinelli A, Cighetti G, Trivulzio S Morphine (CAS 57-27-2) administration or its removal induces alterations in glucose levels and oxidative status or behaviour signs, which may be hypothetically closely related; if this is correct, controlling glucose changes may lead to modifications in peroxide levels and in behaviour profile. It therefore seems important to find a drug able to control alterations of glucose metabolism, peroxide generation and behaviour symptoms in morphine or morphine withdrawal animals. This paper describes the effects of morphine or morphine plus naloxone (CAS 51481-60-8) on the plasma levels of glucose, malondialdehyde (MDA) (CAS 100683-54-3) and behavioural signs in rats treated or not with alpha-lipoic acid (CAS 1077-28-7), known to interfere with gluc... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2306828 Tue, 07 Apr 2009 13:32:38 +0100 2306828 http://www.medworm.com/index.php?rid=2306827&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%3D19338138%26dopt%3DAbstract Authors: Takashima K, Nishiyama C, Arisaka N, Takahashi T, Souma S, Tsuda M, Hayashi M, Kasahara H, Kodama H, Tamura T, Murakami M, Kuroda J, Sato F The renoprotective effect of cilnidipine ((+/-)-2-methoxyethyl 3-phenyl-2(E)-propenyl 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate, CAS 132203-70-4), a L/N-type calcium channel antagonist, on puromycin aminonucleoside (PAN)-induced nephrosis was investigated in rats. In the Experiment I, rats were given an intravenous injection of PAN (70 mg/kg). Cilnidipine (3 mg/kg/day) and enalapril (CAS 75847-73-3, 5 mg/kg/day) were administered orally from 6 days after treatment with PAN (day 6) to day 26, and urinary analysis was performed on days 9, 15, 20 and 27. In the Experiment II, nephrosis was also induced by intravenou... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2306827 Tue, 07 Apr 2009 13:32:38 +0100 2306827 http://www.medworm.com/index.php?rid=2306823&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%3D19338139%26dopt%3DAbstract Authors: Feng S, Tian Y, Zhang Z, Zhang J, Huang M, Chen Y A rapid, simple and sensitive high performance liquid chromatography with positive ion electrospray ionization tandem mass spectrometry (HPLC-ESI-MS/MS) was first developed and validated to simultaneously determine paracetamol (PAR, CAS 103-90-2), amantadine hydrochloride (ATH, CAS 665-66-7), caffeine (CAF, CAS 58-08-2) and chlorpheniramine maleate (CPM, CAS 113-92-8) in human plasma using tramadol hydrochloride (TMH, CAS 22204-88-2) as internal standard (IS). Following methanol-induced protein precipitation, the analytes were separated using a mobile phase comprised of methanol:water (0.5% formic acid) = 20:80 (v/v) on a commercially available column (150 mm x 2.1 mm I.D., 5 microm) and analyzed by electrospray ionization tand... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2306823 Tue, 07 Apr 2009 13:32:38 +0100 2306823 http://www.medworm.com/index.php?rid=2306819&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%3D19338140%26dopt%3DAbstract Authors: Ghorab MM, Ragab FA, Noaman E, Heiba HI, Aboulmagd SA Various isomeric structural purine analogues possessing the pyrazolo[3,4-d]pyrimidine nucleus bearing amino acid moieties have been synthesized. The structures of the synthesized compounds were elucidated by spectral data. Preliminary testing for in vitro anticancer activity of the synthesized compounds against Ehrlich ascites carcinoma cells was carried out. 2-(1-Phenyl-1H-pyrazolo [3,4-d]pyrimidin-4-ylamino)-propanoic acid (3 d), 4-methyl-2-(1-phenyl-1H-pyrazolo [3,4-d] pyrimidin-4-ylamino)-pentanoic acid (3 d), 4-methylthlo-2-(1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-ylamino)-butanoic acid (3e) and phenyl-2-(1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-ylamino)propanoic acid (3f) were the most active compounds. Moreover, compoun... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2306819 Tue, 07 Apr 2009 13:32:38 +0100 2306819 http://www.medworm.com/index.php?rid=2306816&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%3D19338141%26dopt%3DAbstract Authors: Monif T, Reyar S, Tiwari HK, Tippabhotla SK, Khuroo A, Thudi NR, Ahmed S, Raghuvanshi R Lamivudine (CAS 134678-17-4) is a synthetic nucleoside analogue with activity against HIV-1 and HBV. Stavudine (CAS 3056-17-5) is a synthetic thymidine nucleoside analogue, active against the human immunodeficiency virus (HIV). Lamivudine and stavudine in combination with other antiretroviral (ARV) agents are indicated for the treatment of HIV infection. As there are no suitable pediatric ARVs, adult fixed-dose ARVs are commonly used in children. This practice poses concerns about dose inaccuracy, which may lead to resistance or toxicity. A new fixed-dose combination (FDC) tablet for oral suspension, containing lamivudine 40 mg and stavudine 10 mg has been developed. An open-label, balanced... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=2306816 Tue, 07 Apr 2009 13:32:38 +0100 2306816 http://www.medworm.com/index.php?rid=1993278&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%3D19025056%26dopt%3DAbstract Authors: Manosroi A, Thathang K, Werner RG, Schubert R, Peschka-Süss R, Manosroi J Cationic liposomes with high stability and low cytotoxicity for gene therapy have been developed. Luciferase plasmid DNA (pLuc) was used as a model gene. The empty liposomes and niosomes were prepared by freeze dried empty liposomes (FDEL) method. The entrapment of pLuc in the liposomes was by reconstitution of the lyophilized dried vesicles with the plasmid solution. The morphology of the vesicles showing multilamellar structure was characterized by transmission electron microscope (TEM) and cryo-TEM. Cytotoxicity of the vesicular formulations was investigated on mouse melanoma cell lines (B16F10) by MTT assay. Cationic lposomes and niosomes containing the cationic lipid DDAB were less cytotoxic th... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1993278 Thu, 27 Nov 2008 17:38:57 +0100 1993278 http://www.medworm.com/index.php?rid=1993277&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%3D19025057%26dopt%3DAbstract Authors: Osman MY, Osman HM Acetylcholine (CAS 60-31-1, ACh), which is similar in its chemical structure to the carbamate aldicarb, was found to inhibit brain monoamine oxidase isoenzymes, namely MAO-A and B. The effect of ACh on both isoenzymes extracted from the whole brain of male albino rats and its different parts (frontal cortex, basal ganglia, cerebellum, pons and medulla oblongata) was studied. The results indicated that ACh inhibited MAO-A from the cerebellum and MAO-B from the basal ganglia more than MAO iso-enzymes from other brain parts. The inhibition was of the competitive type. It was also found that the enzyme inhibitor dissociation constants (Ki) and the affinity constants (Ki/Km) of MAO-A were higher than those of MAO-B. PMID: 19025057 [PubMed - in process] (Sourc... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1993277 Thu, 27 Nov 2008 17:38:57 +0100 1993277 http://www.medworm.com/index.php?rid=1993276&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%3D19025058%26dopt%3DAbstract Authors: Tian Y, Zhang JJ, Feng SD, Zhang ZJ, Chen Y The pharmacokinetics of aniracetam (CAS 72432-10-1) in Chinese healthy male volunteers was investigated for the first time. Twenty male volunteers were enrolled into this open, randomized, single blind two-sequence, two-period crossover study. Under fasting conditions, each subject received a single oral dose of 400 mg (2 x 200 mg/capsule) aniracetam as a test or reference formulation with a 3-day washout period between the two preparations. The plasma concentrations of aniracetam were analyzed by a sensitive liquid chromatography-tandem mass spectrometry (LC-MS/MS) method. The pharmacokinetic parameters of the test and reference formulations were estimated as follows: The maximum plasma concentrations (Cmax) were 8.75 +/- 7.82 and 8... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1993276 Thu, 27 Nov 2008 17:38:57 +0100 1993276 http://www.medworm.com/index.php?rid=1993275&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%3D19025059%26dopt%3DAbstract CONCLUSION: These results indicate that two formulations of estazolam are bioequivalent and, thus, may be prescribed interchangeably. PMID: 19025059 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1993275 Thu, 27 Nov 2008 17:38:57 +0100 1993275 http://www.medworm.com/index.php?rid=1993274&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%3D19025060%26dopt%3DAbstract CONCLUSION: Benidipine was welltolerated and effective in elderly Chinese patients with essential hypertension. PMID: 19025060 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1993274 Thu, 27 Nov 2008 17:38:57 +0100 1993274 http://www.medworm.com/index.php?rid=1993273&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%3D19025061%26dopt%3DAbstract Authors: Koksal M, Bilge SS, Bozkurt A, Sahin ZS, Isik S, Erol DD Several 5-(3,4-dichlorophenyl)-2-(aroylmethyl)thio-1,3,4-oxadiazoles were synthesized and characterized by elemental analyses, IR and nuclear magnetic resonance spectra. All compounds were evaluated for anti-inflammatory activity by determining their ability to provide protection against carregeenan-induced edema in rat paw. In addition, ulcerogenic activity was determined. The anti-inflammatory data scoring showed that compounds 5e, 5f and 5g, at the dose of 100 mg/kg, exhibited anti-inflammatory activity, which for compound 5f was comparable to that of the reference drug indometacin (CAS 53-86-1). PMID: 19025061 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1993273 Thu, 27 Nov 2008 17:38:57 +0100 1993273 http://www.medworm.com/index.php?rid=1993272&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%3D19025062%26dopt%3DAbstract Authors: Bolakatti GS, Maddi VS, Mamledesai SN, Ronad PM, Palkar MB, Swamy S A novel series of coumarinyl Mannich bases (3a-1) have been synthesized by reacting 3-acetyl coumarin (1) with various substituted secondary amines (2a-1) in presence of paraformaldehyde. The structures of the newly synthesized compounds were characterized by IR, 1H NMR, 13C NMR and HRMS (high resolution mass spectral) data. Title compounds were screened for in vivo acute anti-inflammatory activity using the carrageenan-induced rat paw edema assay model. Among the compounds tested, 3-[3-(diethylamino)propanoyl]-2H-chromen-2-one (3a)and 3-[3-(piperidine-1-yl) propanoyl]-2H-chromen-2-one (3c) showed 63.1 and 66.7% inhibition, respectively, as compared to the standard drug diclofenac (CAS 15307-86-5, 68.8%). Thes... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1993272 Thu, 27 Nov 2008 17:38:57 +0100 1993272 http://www.medworm.com/index.php?rid=1993271&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%3D19025063%26dopt%3DAbstract Authors: Becan L, Wagner E A series of new derivatives of 3-phenylthiazolo[4,5-d]pyrimidine-2-thiones were synthesized by the cyclization of 4-amino-5-alkyl(aryl) carboxamido-2,3-dihydrothiazolo-2-thione with aromatic aldehydes. Amine moieties were substituted in position 7 of the obtained bicyclic compounds. The synthesized compounds were characterized by elemental analysis, IR, 1H-NMR, and 13C-NMR spectral data. Some of the newly synthesized compounds were selected by the U.S. National Cancer Institute for in vitro antitumor screening. The two compounds 3d 7-chloro-5-(4-fluorophenyl)-3-phenyl-4,5-dihydro-3H-thiazolo[4,5-d]pyrinimidine-2-thione and 4i 5-(2-chlorophenyl)-7-(4-fluorobenzylaxnlno)-3-phenyl-4,5-dihydro-3H-thiazolo[4,5-dipyrhflldlfle-2thione proved to be the most active in... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1993271 Thu, 27 Nov 2008 17:38:57 +0100 1993271 http://www.medworm.com/index.php?rid=1993270&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%3D19025064%26dopt%3DAbstract Authors: Qin Y, Song QG, Zhang ZR, Liu J, Fu Y, He Q, Liu J Recent studies indicate that luteinizing hormone-releasing hormone (LHRH) analogues (LHRHa), like LHRH, are able to specifically bind to LHRH receptors which are highly expressed on the extracellular membrane of ovarian tumor cells. As a targeting moiety, LHRHa can mediate the ovarian tumor targeting of docetaxel-loaded liposomes. In our study, synthesized negatively charged cholesterol succinimide (CHS) was employed for the preparation of negatively charged docetaxel-loaded liposomes, with which the positively charged LHRHa is linked via electrostatic absorption. An HPLC-based assay for determination of docetaxel (CAS 114977-28-5, Doc) in vivo and the model of ovarian cancer xenograft were established to investigat the biodis... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1993270 Thu, 27 Nov 2008 17:38:57 +0100 1993270 http://www.medworm.com/index.php?rid=1925491&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%3D18972871%26dopt%3DAbstract Authors: Zou J, Dai L, Wang GJ, Zhu Y, Fan H, Xiao da W A sensitive liquid chromatography-tandem mass spectrometry (LC/MS/MS) method was developed and validated for the determination of trimetazidine (CAS 13171-25-0) in human plasma, using pseudoephedrine as internal standard (IS). Plasma samples were simply pretreated with methanol for deproteinization. The chromatographic separation was performed on a C18 column with a mobile phase of 3 mmol/L ammonium acetate solution-methanol (15:85, v/v) at a flow rate of 0.3 mL/min. The chromatographic separation was achieved in less than 3.2 min. The linearity was established over the concentration range of 1-100 ng/mL. Both intra- and inter-batch standard deviations were less than 9.5%. The method was successfully applied to study the relative ... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1925491 Sat, 01 Nov 2008 16:53:12 +0100 1925491 http://www.medworm.com/index.php?rid=1925490&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%3D18972872%26dopt%3DAbstract CONCLUSION: This study demonstrated that benidipine prevents the occurrence of cardiovascular events in patients with AP, suggesting that benidipine contributes to a favorable long-term prognosis of such patients. PMID: 18972872 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1925490 Sat, 01 Nov 2008 16:53:12 +0100 1925490 http://www.medworm.com/index.php?rid=1925489&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%3D18972873%26dopt%3DAbstract Authors: Zarghi A, Shafaati A, Foroutan SM, Movahed H, Khoddam A A rapid, sensitive and reproducible HPLC method was developed and validated for the analysis of pantoprazole (CAS 102625-70-7) in human plasma. The separation was achieved on a monolithic silica column using acetonitrile-potassium dihydrogen phosphate buffer (25:75,v/v), pH 3.0, as the mobile phase at a flow rate of 1.5 ml min(-1). The wavelength was set at 290 nm. The assay enables the measurement of pantoprazole for therapeutic drug monitoring with a minimum quantification limit of 20 ng ml(-1). The method involves a simple protein precipitation procedure. Analyticil recovery was complete. The calibration curve was linear over the concentration range 20-3500 ng ml(-1) The coefficients of variation forthe inter-day and i... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1925489 Sat, 01 Nov 2008 16:53:12 +0100 1925489 http://www.medworm.com/index.php?rid=1925488&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%3D18972874%26dopt%3DAbstract Authors: Wang X, Wang Z, Sun H, Lv H, Guan H, Meng X, Sun H, Zhang G, Cao H High performance liquid chromatography (HPLC) coupled with the solid phase extraction method was developed for determining cimifugin (a coumarin derivative; one of Saposhnikovia divaricatae's constituents) in rat plasma after oral administration of Saposhnikovia divaricatae extract (SDE), and the pharmacokinetics of cimifugin either in SDE or as a single compound was investigated. The HPLC analysis was performed on a commercially available column (4.6 mm x 200 mm, 5 pm) with the isocratic elution of solvent A (Methanol) and solvent B (Water) (A:B=60:40) and the detection wavelength was set at 250 nm. The calibration curve was linear over the range of 0.100-10.040 microg/mL. The limit of detection was 30 ng/mL. ... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1925488 Sat, 01 Nov 2008 16:53:12 +0100 1925488 http://www.medworm.com/index.php?rid=1925487&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%3D18972875%26dopt%3DAbstract This study was conducted in order to assess the bioequivalence of two enteric-coated formulations of 40 mg pantoprazole (CAS 102625-70-7), under fed conditions. Seventy-four healthy subjects, age ranging from 24 to 55 years, were enrolled in a two-centre, randomised, single-dose, open-label, 2-way crossover study, with a minimum washout period of 7 days. Plasma samples were collected up to 30.0 h post-dosing. Pantoprazole levels were determined by reverse liquid chromatography and detected by tandem mass spectrometry detection (LC-MS/ MS). Pharmacokinetic parameters used for bioequivalence assessment were the AUClast (area under the concentration-time curve from time zero to time of last observed non-zero concentration), AUCinf (area under the concentration-time curve from time zero to inf... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1925487 Sat, 01 Nov 2008 16:53:12 +0100 1925487 http://www.medworm.com/index.php?rid=1925486&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%3D18972876%26dopt%3DAbstract Authors: Alafeefy AM A series of fenamate quinazolinyl analogues, viz acids 6a-d, esters 6e-h, carbohydrazides 7a-d, arylidenes 8a-d, oxadiazol-2-ones 13a-d and oxadiazol-2-thiones 14a-d, have been prepared and screened for their analgesic (acetic acid-induced writhing), anti-inflammatory (carrageenan-induced rat paw edema) activities as well as their ulcerogenic effects. All the final compounds except 7a-d and 8a-d showed good dual activities. Compounds 6a, 6b, 6e, 6f, 13a and 14a showed activities comparable to that of mefenamic acid (CAS 61-68-7) in the acetic acid-induced writhing model as well as in the carrageenan-induced rat paw edema test at a dose level of 100 mg/ kg.Compounds 6a and 6b were highly ulcerogenic, while compounds 6e, 6f, 13a and 14a exhibited the lowest ulcerogen... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1925486 Sat, 01 Nov 2008 16:53:12 +0100 1925486 http://www.medworm.com/index.php?rid=1925485&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%3D18972877%26dopt%3DAbstract In this study, 3-alkyl and 3-aryl esters of hexahydroquinoline derivatives were screened for their ability to decrease bacterial resistance to ciprofloxacin (CAS 85721-33-1), which is extensively used to treat bacterial infections. A group of 3-alkyl and 3-aryl esters of hexahydroquinoline derivatives in which 2-aryl thiazole is substituted at 4-position were synthesized. The enhancement of the antibacterial activity of ciprofloxacin by these new synthetic compounds was evaluated against a resistant clinical strain of Staphylococcus aureus. The agar disk diffusion method was used to determine the antibacterial activity of different synthetic compounds in the absence and presence of ciprofloxacin. These results indicate that the antibacterial effect of ciprofloxacin is enhanced by two 3-alk... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1925485 Sat, 01 Nov 2008 16:53:12 +0100 1925485 http://www.medworm.com/index.php?rid=1925484&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%3D18972878%26dopt%3DAbstract Authors: Kiep L, Burkhardt J, Seifert K Previous investigations have shown that an ex vivo model on the basis of the incubated hen's egg represents a potential alternative to animal experimentation for xenobiotic metabolism studies. This model is characterized by administration of the xenobiotic into the yolk sac and identification of metabolites in the allantoic fluid. In the present study, gentisic acid (2,5-dihydroxybenzoic acid, 2,5-DHBA, CAS 490-79-9) was used as a test substance. The oxidative fate of this salicylate metabolite in human and animal species could not be completely elucidated until now. Inoculation of 2,5-DHBA into the incubated hen's egg in concentrations up to 8 mg/egg did not affect embryo viability. For the metabolism studies a dose of 2 mg/egg was chosen and 2,... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1925484 Sat, 01 Nov 2008 16:53:12 +0100 1925484 http://www.medworm.com/index.php?rid=1925483&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%3D18972879%26dopt%3DAbstract Authors: Wink K To prove the efficacy of drugs in patients with chronic systolic heart failure, taking into consideration certain criteria is necessary for the planning and performance of the clinical investigation of medicinal products. For the different stages and the collective of patients those criteria include the definition of the corresponding endpoints, adequate study design, appropriate randomisation, blinding, the choice of an appropriate dose, valid methods of examination, the correct sample size estimation and analysis. If these criteria will b e used, the besttherapy for the different stages can be ascertained. PMID: 18972879 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1925483 Sat, 01 Nov 2008 16:53:12 +0100 1925483 http://www.medworm.com/index.php?rid=1830549&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%3D18807576%26dopt%3DAbstract Authors: Neves R, Almeida S, Filipe A, Spínola AC, Abolfathi Z, Yritia M, Ortuño J The study was conducted in order to assess the bioequivalence of two film-coated formulations containing 100 mg of losartan (CAS 124750-99-8) and 12.5 mg of hydrochlorothiazide (CAS 58-93-5). Seventy-three healthy subjects were enrolled in a randomised, single-dose, open-label, two-way crossover study, with a minimum washout period of 7 days. A total of 21 blood samples were collected up to 36 h post-dosing. Losartan, losartan carboxy acid and hydrochlorothiazide levels were determined by liquid chromatography with tandem mass detection (lower limit of quantification: 1.01 ng/mL for hydrochlorothiazide, 2.02 ng/mL for losartan and 2.51 ng/mL for losartan carboxy acid). Pharmacokinetic parameter... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1830549 Fri, 26 Sep 2008 19:50:55 +0100 1830549 http://www.medworm.com/index.php?rid=1830548&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%3D18807577%26dopt%3DAbstract In conclusion, D-003 (5-20 mg/d) given as doses titrated every 15 days (5-20 mg/d) inhibited AA- and collagen-induced platelet aggregation in hypercholesterolemic patients and was well tolerated. PMID: 18807577 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1830548 Fri, 26 Sep 2008 19:50:55 +0100 1830548 http://www.medworm.com/index.php?rid=1830547&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%3D18807578%26dopt%3DAbstract Authors: Allegrini A, Nuzzo L, Scaringi AT, Felaco S, Pavone D, Toniato E, Mezzetti A, Martinotti S, Lenotti G The study was conducted in order to assess the bioequivalence of two capsule formulations (test and reference) containing 20 mg of omeprazole (5-methoxy-2-[[4-methoxy-3,5-dimethyl-2-pyridinyl) methyl]sulfinyl]-1H-benzimidazole, CAS 73590-58-6). Fifty healthy male and female volunteers were treated in a single-centre, randomised, repeated-dose (once daily for six consecutive days), open-label, two-way crossover study, with a washout period of at least 9 days between treatments. Plasma samples were collected up to 12 h post-dosing for the determination of omeprazole by HPLC with photodiode array detector (DAD). The evaluation of bioequivalence was based on the following pharmaco... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1830547 Fri, 26 Sep 2008 19:50:55 +0100 1830547 http://www.medworm.com/index.php?rid=1830546&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%3D18807579%26dopt%3DAbstract CONCLUSIONS: IPC supplementation improved the iron status of adolescents with and without iron deficiency and anemia. These data provide evidence that IPC is an easy-to-administer and well tolerated compound which can improve and normalize the iron status of iron deficient and anemic patients. PMID: 18807579 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1830546 Fri, 26 Sep 2008 19:50:55 +0100 1830546 http://www.medworm.com/index.php?rid=1830545&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%3D18807580%26dopt%3DAbstract Authors: Koksal M, Kelekci NG, Mercanoglu GO, Erdogan H A new series of 6-acyl-3-alkyl-5-methyl-2(3H)-benzoxazolones have been obtained starting from 5-methyl-2(3H)-benzoxazolone. All the compounds have been characterized by IR, 1H-NMR and mass spectroscopy. The new compounds were screened for analgesic and anti-inflammatory activities and ulcerogenic effect. The in vitro antioxidant capacity of the synthesized compounds were tested by the nitric oxide radical scavenging assay. Most of the compounds showed antiinflammatory activity. Among them, 3-[4-(4-fluorophenyl)piperazinomethyl] -6-(3-chlorobenzoyl)-5-methyl-2(3H)-benzoxazolone (3j) was found more potent than the reference drug indometacin (CAS 53-86-1) with 41.66% decrease in edema. Compared with the control, some of the compounds... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1830545 Fri, 26 Sep 2008 19:50:55 +0100 1830545 http://www.medworm.com/index.php?rid=1830544&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%3D18807581%26dopt%3DAbstract This study presents the results of a two-way, two-period, two-treatment crossover investigation in 12 healthy Indian male subjects to assess the bioequivalence of two oral formulations containing 50 mg of diacerein (CAS 13739-02-1). Both formulations were administered orally as a single dose separated by a one-week washout period. The content of diacerein 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 this study indicated that there were no statistically significant diffe... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1830544 Fri, 26 Sep 2008 19:50:55 +0100 1830544 http://www.medworm.com/index.php?rid=1830543&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%3D18807582%26dopt%3DAbstract Authors: Lal J, Tripathi RP, Gupta RC A sensitive and reproducible high performance liquid chromatography (HPLC)-UV method for the determination of the novel anti-tuberculosis compound 1,2:5,6-di-O-isopropylidene-3-O-(phenyl cyclopropyl methanonyl)-alpha-D-glucofuranose (S-001-14) has been developed and validated in rat serum, urine and feces. Following extraction with hexane at alkaline pH, samples were separated on a reverse phase C18 column and quantified using UV detection at 267 nm. The mobile phase was 70% acetonitrile in ammonium acetate buffer (10 mmol/L, pH 6.0) with a flow rate of 1.0 ml/min. The method was used to determine the pharmacokinetics and excretion of S-001-14 after oral doses in rats. Linearity was satisfactory over the concentration range of 5-500 ng/ml (r2, >... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1830543 Fri, 26 Sep 2008 19:50:55 +0100 1830543 http://www.medworm.com/index.php?rid=1830542&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%3D18807583%26dopt%3DAbstract Authors: Filipe A, Almeida S, Spínola AC, Trabelsi F, Ortuño J The study was conducted in order to compare the bioavailability of two tablet formulations containing letrozole 2.5 mg (CAS 112809-51-5). Twenty healthy subjects were enrolled in a single-centre, bioequivalence, randomised, single-dose, open-label, two-way crossover study, performed under fasting conditions with a minimum washout period of 21 days. Plasma samples were collected up to 240 h post-dosing. Letrozole levels were determined by reverse liquid chromatography and detected by tandem mass spectrometry detection, LC/MS/MS method. Pharmacokinetic parameters used for bioequivalence assessment, area under the concentration-time curve from time zero to time of last non-zero concentration (AUC(0-t)) and from time ... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1830542 Fri, 26 Sep 2008 19:50:55 +0100 1830542 http://www.medworm.com/index.php?rid=1830541&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%3D18807584%26dopt%3DAbstract Authors: Leedman B PMID: 18807584 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1830541 Fri, 26 Sep 2008 19:50:55 +0100 1830541 http://www.medworm.com/index.php?rid=1744190&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%3D18751496%26dopt%3DAbstract CONCLUSION: The CVR in cortical structures recovered sooner than that in subcortical gray matter. Although the number of stroke patients included in this study was small, it is concluded that this phenomenon may be attributable to the earlier vasoreactivity increase in the cortical vessels than the subcortical perforators. PMID: 18751496 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1744190 Sat, 30 Aug 2008 14:56:54 +0100 1744190 http://www.medworm.com/index.php?rid=1744189&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%3D18751497%26dopt%3DAbstract The objective of this study was to compare the pharmacokinetics and to establish bioequivalence of two formulations of amlodipine. The study was performed at the Clinical Pharmacology Unit, Hospital de Clínicas, Medical School of Buenos Aires University. This randomized, single blind, two-period, two-sequence, comparative crossover study was conducted in 24 Caucasian healthy volunteers. A single oral 10 mg dose of amlodipine besylate (CAS 111470-99-6) test formulation and reference formulation were administered to the volunteers separated by a 3-week washout period in a crossover manner. Blood samples for pharmacokinetic analysis were collected over a period of 144 h after drug administration. Amlodipine was measured in plasma samples using a validated HPLC method with LC-MS-MS detect... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1744189 Sat, 30 Aug 2008 14:56:54 +0100 1744189 http://www.medworm.com/index.php?rid=1744188&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%3D18751498%26dopt%3DAbstract Authors: Nordling J, van Ophoven A Effectiveness, safety, and tolerability of instillation therapy with chondroitin sulphate (CAS 9082-07-9, Gepan instill) was investigated in a non-interventional study. 286 patients with clinically diagnosed chronic forms of cystitis, such as bladder pain syndromelinterstitial cystitis, radiation cystitis, overactive bladder syndrome and chronically-recurring cystitis were included. The course of symptoms was documented over 8 instillations at maximum, covering a period of approximately three months. All main symptoms of chronic cystitis declined consistently and statistically significantly (p < 0.0001). Both daytime and nighttime micturition frequencies as well as the score levels of urgency and pain declined significantly during the course of tre... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1744188 Sat, 30 Aug 2008 14:56:54 +0100 1744188 http://www.medworm.com/index.php?rid=1744187&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%3D18751499%26dopt%3DAbstract Authors: Wang X, Lv H, Sun H, Sun W, Liu L, Wang P, Cao H A method for the rapid and simultaneous determination of 6,7-dimethylesculetin (CAS 120-08-1) and geniposide (CAS 24512-63-8) in rat plasma has been developed, using validated high performance liquid chromatography (HPLC) with solid phase extraction (SPE). The HPLC analysis was performed on a commercially available column (200 mm x 4.6 mm, 5 microm) with acetonitrile-methanol-0.1% aqueous formic acid as mobile phase and the UV detection at 343 nm and 238 nm for 6,7-dimethylesculetin and geniposide, respectively. The calibration curves for 6,7-dimethylesculetin and geniposide were linear over the range 0.4-25.6 microg/mL and 1.12-71.68 microg/mL, respectively. The lower limits of quantitation were 0.40 microg/ mL and 1.12 microg/... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1744187 Sat, 30 Aug 2008 14:56:54 +0100 1744187 http://www.medworm.com/index.php?rid=1744186&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%3D18751500%26dopt%3DAbstract CONCLUSION: Thus, these findings clearly indicate that the two formulations are bioequivalent in terms of rate and extent of drug absorption. Both preparations were well tolerated with no adverse reactions observed throughout the study. PMID: 18751500 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1744186 Sat, 30 Aug 2008 14:56:54 +0100 1744186 http://www.medworm.com/index.php?rid=1744185&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%3D18751501%26dopt%3DAbstract Authors: Zhang W, Xiang BR, Zhang J A sensitive and selective high-performance liquid chromatographic-ultraviolet (HPLC-UV) method for the determination of mycophenolic acid (MPA, CAS 24280-93-1) in human plasma has been developed. Sample treatment was based on protein precipitation with a trichloroacetic acid-water (10:90, w/v) solution. The analytical determination was carried out by HPLC with ultraviolet detection at 254 nm. Chromatographic separation was achieved on a C18 column by isocratic elution with acetonitrile-water (pH 4.4) (50:50, v/v) at a flow rate of 1.0 mL/min. The method was linear in the concentration range of 0.2-50.0 microg/mL. The lower limit of quantification (LLOQ) was 0.2 microg/ mL. The intra-day and inter-day relative standard deviations across three validati... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1744185 Sat, 30 Aug 2008 14:56:54 +0100 1744185 http://www.medworm.com/index.php?rid=1744184&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%3D18751502%26dopt%3DAbstract Authors: Juszczak M, Matysiak J, Brzana W, Niewiadomy A, Rzeski W Two 2-(monohalogenophenylamino)-5-(2,4-dihydroxyphenyl)-1,3,4-thiadiazoles were synthesized by reaction of sulfinyl bis(2,4-dihydroxythiobenzoyl) with 4-substituted 3-thiosemicarbazides and evaluated for their antiproliferative activity in tumor cells and for cytotoxicity in normal cells. Both derivatives in micromolar concentrations elicited a prominent antiproliferative effect in tumor cells derived from cancers of the nervous system (rhabdomyosarcoma/medulloblastoma, glioma) and peripheral cancers, including breast adenocarcinoma and lung carcinoma. The anticancer effect was attributed to decreased DNA synthesis and was not connected with apoptosis induction. Both compounds were not toxic to normal human skin fibrobla... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1744184 Sat, 30 Aug 2008 14:56:54 +0100 1744184 http://www.medworm.com/index.php?rid=1744183&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%3D18751503%26dopt%3DAbstract Authors: Li J, Wang N, Zhang ZJ, Tian Y, Tang W, Chen Y The aim of the present study was to compare the bioavailability of clindamycin (CAS 18323-44-9) from three clindamycin hydrochloride (CAS 21 462-39-5) capsules (clindamycin 75 mg capsule as test 1 preparation, 150 mg capsule as test 2 preparation and a commercially available original 150 mg capsule of the drug as reference preparation) in 24 Chinese healthy male volunteers, aged between 22 and 28. The study was conducted according to a randomized, double-blind, 3-period, 3-treatment, 3-sequence, single-dose, crossover design with a wash-out phase of 7 days. Blood samples for pharmacokinetic profiling were taken up to 14 h post-dose, and clindamycin plasma concentrations were determined with a validated liquid chromatography-electr... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1744183 Sat, 30 Aug 2008 14:56:54 +0100 1744183 http://www.medworm.com/index.php?rid=1744182&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%3D18751504%26dopt%3DAbstract This study shows that the test formulation is bioequivalent to the reference formulation of terbinafine. PMID: 18751504 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1744182 Sat, 30 Aug 2008 14:56:54 +0100 1744182 http://www.medworm.com/index.php?rid=1684183&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%3D18677966%26dopt%3DAbstract Authors: Lippert TH, Ruoff HJ, Volm M Drug resistance is the major reason for failure in cancer chemotherapy. Resistance may be either pre-existent (intrinsic resistance), or induced by drugs (acquired resistance), So far, no strategy has been found to overcome resistance, which is based on highly complex and individually variable biological mechanisms. In present clinical practice, drug resistance can only be recognized during treatment, after long lag times. Thus diagnostic tests are re quired, indicating resistance at an earlier stage, in order to avoid unnecessary medication, frequently associated with toxic side-effects. A number of new anti-cancer drugs are now available. In contrast to the unspecifically acting cytostatic chemotherapy, these compounds have targeted actions. Howe... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1684183 Wed, 06 Aug 2008 19:26:41 +0100 1684183 http://www.medworm.com/index.php?rid=1684182&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%3D18677967%26dopt%3DAbstract Authors: Vloeberghs E, Coen K, Van Dam D, De Deyn PP Valid animal models are indispensable in the drug discovery pipeline for dementia. Transgenic APP23 mice model Alzheimer's disease patients' memory deficits and additionally present with various behavioural disturbances, such as aggressive behaviour. The present study investigated and confirmed significant sensitivity of the model to the aggression-lowering ability of the antipsychotic agent risperidone (CAS 106266-06-2). The sensitivity for such anti-aggressive action contributes to the therapeutic predictive validity of the APP23 model of Alzheimer's disease, which can be used as a pre-clinical screening tool for the identification of novel anti-aggressive agents. PMID: 18677967 [PubMed - in process] (Source: Arzneimittel-Forsc... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1684182 Wed, 06 Aug 2008 19:26:41 +0100 1684182 http://www.medworm.com/index.php?rid=1684181&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%3D18677968%26dopt%3DAbstract CONCLUSION: These results showed that in an open-field setting buspirone appears to have a dual effect. The reduced activity and increase in time spent in the center areas are indicative of both an anxiogenic and an anxiolytic effect, respectively. This was found in both open-field settings, suggesting that the effects of buspirone are independent of the anxiety level. PMID: 18677968 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1684181 Wed, 06 Aug 2008 19:26:41 +0100 1684181 http://www.medworm.com/index.php?rid=1684180&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%3D18677969%26dopt%3DAbstract CONCLUSION: In patients treated with ibudilast, the amelioration of dizziness and depression was accompanied by a CBF increase in the right frontal and occipital cortices. These findings suggest that the right frontal and occipital cortices may be related to their dizziness and depression. PMID: 18677969 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1684180 Wed, 06 Aug 2008 19:26:41 +0100 1684180 http://www.medworm.com/index.php?rid=1684179&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%3D18677970%26dopt%3DAbstract Authors: Quetglas EG, Campanero MA, Sádaba B, Escolar M, Azanza JR Triflusal (CAS 322-79-2) is an antiplatelet agent related to salicylates used in several European and Latin American countries in the treatment of cardiovascular diseases. The aim of this paper was to evaluate the bioequivalence of triflusal derived from two preparations using both parent drug and metabolite pharmacokinetic data. The bioavailabolity was measured in 24 healthy male Caucasian volunteers following a single oral dose (600 mg) of the test or reference products in the fasting state. Blood samples were collected for 120 h. Plasma concentrations of triflusal and its metabolite 3-hydroxy-4-trifluoromethylbenzoic acid (HTB) were analyzed by high-performance liquid chromatography with UV and fluorescence dete... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1684179 Wed, 06 Aug 2008 19:26:41 +0100 1684179 http://www.medworm.com/index.php?rid=1684178&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%3D18677971%26dopt%3DAbstract Authors: Varanasi VS, Veeraraghavan S, Potharaju S, Thappali RS, Raghavan R, Vakkalanka VS A high performance liquid chromatographic (HPLC) method for simultaneous determination of rosiglitazone, CAS 122320-73-4, RSG), cilostazol (CAS 73963-72-1, CLZ) and its active metabolite 3, 4-dehydro-cilostazol (DCLZ), using pioglitazone (PIO) as internal standard (IS), in rat plasma is described. The plasma was extracted with methyl t-butyl ether, the dry extract was reconstituted in mobile phase and the aliquot was injected. The eluent drugs were detected by UV at dual wavelength of 226 nm (RSG and DCLZ) and 257 nm (CLZ). The mobile phase consisting of acetonitrile:potassium di-hydrogen phosphate buffer (35:65 v/v) was used at the flow rate of 1.2 ml/min on a reverse phase C18 column. The absol... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1684178 Wed, 06 Aug 2008 19:26:41 +0100 1684178 http://www.medworm.com/index.php?rid=1684177&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%3D18677972%26dopt%3DAbstract CONCLUSIONS: Th2 cytokines may increase the airway cough reflex sensitivity in patients with atopic cough. Oral administration of suplatast tosilate may be a novel therapy for atopic cough. PMID: 18677972 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1684177 Wed, 06 Aug 2008 19:26:41 +0100 1684177 http://www.medworm.com/index.php?rid=1684176&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%3D18677973%26dopt%3DAbstract CONCLUSIONS: Inhalation of DSCG/REP before exercise provides significantly better protection against EIA than three days treatment with MON. PMID: 18677973 [PubMed - in process] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1684176 Wed, 06 Aug 2008 19:26:41 +0100 1684176 http://www.medworm.com/index.php?rid=1684175&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%3D18677974%26dopt%3DAbstract Authors: Vargas-Estrada D, Gutiérrez L, Juarez-Rodríguez I, Sumano H Doxycycline hyclate (CAS 24390-14-5, doxycycline-h), an antibacterial with time-dependent action, was formulated as a non-irritating long-acting parenteral formulation based on a beta-cyclodextrin: poloxamer-based matrix (doxycycline-h-LA). Tissue and serum concentrations vs time profile were investigated after its subcutaneous injection to Wistar rats. Serum concentration profiles and key pharmacokinetic (PK) variables of doxycycline-h-LA were compared to the corresponding profiles and PK values obtained with an aqueous formulation of doxycycline-h administered either intramuscularly, orally or intravenously to Wistar rats. In all groups, the dose was 10 mg/kg. Doxycycline-h-LA showed outstanding bioavailab... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1684175 Wed, 06 Aug 2008 19:26:41 +0100 1684175 http://www.medworm.com/index.php?rid=1588446&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%3D18368944%26dopt%3DAbstract Authors: Hardeland R, Poeggeler B, Srinivasan V, Trakht I, Pandi-Perumal SR, Cardinali DP Melatonin (CAS 73-31-4) has both hypnotic and sleep/wake rhythm regulating properties. These sleep promoting actions, which are already demonstrable in healthy humans, have been found useful in subjects suffering from circadian rhythm sleep disorders (CRSD) like delayed sleep phase syndrome (DSPS), jet lag and shift-work sleep disorder. Low nocturnal melatonin production and secretion have been documented in elderly insomniacs, and exogenous melatonin has been shown to be beneficial in treating sleep disturbances of these patients. In comparison to a number of sleep-promoting compounds that are usually prescribed, such as benzodiazepines and z-drugs (zolpidem and zopiclon belonging to the latter o... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1588446 Mon, 07 Jul 2008 18:03:49 +0100 1588446 http://www.medworm.com/index.php?rid=1588445&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%3D18368945%26dopt%3DAbstract Authors: Shin MC, Kim JK, Kim CK The bioequivalence of a test formulation (Nanopril, "test") and a reference formulation ("reference") of lisinopril (CAS 83915-83-7) was demonstrated by in vivo and in vitro tests. The in vivo bioequivalence study in 26 healthy volunteers was designed as a single dose, randomized, double-blind trial with a 2-week washout period between the doses. Prior to the in vivo study, an in vitro comparative dissolution test was performed by the paddle method following the bioequivalence guidance of the Korea Food and Drug Administration (KFDA). By the results of the dissolution test it was demonstrated from the similar and rapidly dissolving patterns of the two lisinopril tablets that the two formulations were pharmaceutically equivalent. However, the in vivo bio... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1588445 Mon, 07 Jul 2008 18:03:49 +0100 1588445 http://www.medworm.com/index.php?rid=1588444&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%3D18368946%26dopt%3DAbstract CONCLUSION: Our research suggested the efficacy of pemirolast potassium in glomerulonephritis. A well-controlled study is considered necessary to validate pemirolast potassium as a therapeutic drug for glomerulonephritis. PMID: 18368946 [PubMed - indexed for MEDLINE] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1588444 Mon, 07 Jul 2008 18:03:49 +0100 1588444 http://www.medworm.com/index.php?rid=1588443&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%3D18368947%26dopt%3DAbstract Authors: Shioya T, Satake M, Sato K, Sano MA, Sugawara K, Takahashi H, Honma M The present study was undertaken to evaluate the long-term effect of procaterol hydrochloride (CAS 62929-91-3, Meptin), a third generation beta2-receptor agonist on lung function, exercise capacity, health-related quality of life (HRQOL) and activities of daily living (ALDs) in patients with stable chronic obstructive pulmonary disease (COPD). Twenty patients were randomly assigned to the procaterol group or to the control group, who received oxitropium bromide (CAS 30286-75-0), an anticholinergic agent. Procaterol was inhaled three times a day at a dose of 20 pg, while oxitropium was inhaled three times a day at a dose of 200 microg. The subjects were evaluated based on spirometry, exercise capacity, the Bo... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1588443 Mon, 07 Jul 2008 18:03:49 +0100 1588443 http://www.medworm.com/index.php?rid=1588442&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%3D18368948%26dopt%3DAbstract Authors: Dahiya R, Kaur K In present study, a natural phenylalanine-rich cycloheptapeptide segetalin C (compound VIII) was synthesized by coupling and cyclization of peptide units Boc-gly-L-leu-L-his-OH and L-Phe-L-alaL-phe-L-pro-OMe and examined for different bioactivities. The structure of compound VIII was elucidated by IR, 1H NMR, 13C NMR, mass spectral data and elemental analysis. It was demonstrated that the newly synthesized cyclopeptide has good activity against pathogenic fungi Candida albicans and dermatophytes, in addition to high cytotoxicityagainst Dalton's lymphoma ascites (DLA) and Ehrlich's ascites carcinoma (EAC) cell lines with CTC50 values of 3.35 and 5.72 micromol/L. PMID: 18368948 [PubMed - indexed for MEDLINE] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1588442 Mon, 07 Jul 2008 18:03:49 +0100 1588442 http://www.medworm.com/index.php?rid=1588441&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%3D18368949%26dopt%3DAbstract Authors: Ghorab MM, Ragab FA, Noaman E, Heiba HI, El-Hossary EM The present work reports the possible utility of 4-(5,5-dimethyl-3-oxo-cyclohex-1-enylamino)benzenesulfonamide in the synthesis of some novel 4-(quinolin-1-yl) benzenesulfonamide derivatives (6a-o). Structures of the newly synthesized compounds were confirmed by elemental analyses and spectral data. All the newly synthesized compounds were evaluated for their in vitro anticancer activity. Compounds 6k, 6j and 6m showed interesting cytotoxic activity compared with doxorubicin (CAS 23214-922-8) as a reference drug. Additionally, compound 6c exhibited in vivo radioprotective activity, against gamma-irradiation, in mice. PMID: 18368949 [PubMed - indexed for MEDLINE] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1588441 Mon, 07 Jul 2008 18:03:49 +0100 1588441 http://www.medworm.com/index.php?rid=1588440&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%3D18368950%26dopt%3DAbstract Authors: Kano EK, Porta V, Koono EE, Schramm SG, Serra CH Two different cefadroxil (CAS 50370-12-2) formulations were evaluated for their relative bioavailability in 24 healthy volunteers who received a single 500 mg oral dose of each preparation. An open, randomized clinical trial designed as a two-period crossover study with a 7-day washout period between doses was employed. Plasma samples for assessments of their cefadroxil concentration by HPLC-UV were obtained over 8 h after administration. Values of 48.94 +/- 10.18 pg x h/ml for test, and 48.51 +/- 9.02 microg x h/ml for the reference preparation AUC(0-t) demonstrate a nearly identical extend of drug absorption. Maximum plasma concentration Cmax of 16.04 +/- 4.94 microg/ml and 16.01 + 4.02 microg/ml achieved for the test and refe... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1588440 Mon, 07 Jul 2008 18:03:49 +0100 1588440 http://www.medworm.com/index.php?rid=1588439&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%3D18368951%26dopt%3DAbstract Authors: PMID: 18368951 [PubMed - indexed for MEDLINE] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1588439 Mon, 07 Jul 2008 18:03:49 +0100 1588439 http://www.medworm.com/index.php?rid=1588431&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%3D18412018%26dopt%3DAbstract Authors: Meza-Toledo SE, Bowery NG The phenyl alcohol amides, DL-2-hydroxy-2-phenyl butyramide (CAS 52839-87-9), DL-3-hydroxy-3-phenyl pentanamide (CAS 131802-69-2, DL-HEPP) and DL-4-hydroxy-4-phenyl hexanamide (CAS 67880-30-2) and their fluorine and chlorine analogs, at a concentration of 100 micromol/L, did not displace [3H]-gamma-aminobutyric acid ([3H]-GABA, CAS 108158-36-7) from GABAA receptors and only weakly displaced [3H]-GABA and [3H]-CGP62349 (CAS 186986-97-0), a GABAB receptor antagonist, from GABAB receptors in rat brain crude synaptic membranes. The electrically and potassium chloride (15 mmol/L) evoked [3H]-GABA release in the presence of DL-HEPP, GABA and GABAB receptor ligands from rat brain substantia nigra (SN) slices was studied. R-Baclofen (CAS 69308-37-8) (10 micro... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1588431 Mon, 07 Jul 2008 18:03:49 +0100 1588431 http://www.medworm.com/index.php?rid=1588430&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%3D18412019%26dopt%3DAbstract Authors: Lal J, Gupta RC CDRI-93/478 (1- [4-(4-fluorophenyl) piperazine-1-yl]-3-(2-oxopyrrolidin-1-yl) propane hydrochloride, an arylpiperazine derivative, is a potent anti-ischemic and anti-hypertensive agent and is in advanced stage of preclinical trials. In order to develop CDRI-93/478 into a clinical agent, the absorption, protein binding, pharmacokinetics, and excretion of the compound were investigated in male Sprague-Dawley rats. Oral absorption was evaluated in situ and in vivo, using the portal-venous concentration difference method. The compound showed negligible absorption (ka = 0.01 h(-1)) at pH 2.6. However, the rate of absorption of the compound at pH 7.4 was 0.6 h(-1) and was comparable to that observed in the in vivo study (ka, >0.58 h(-1)) in rats after a single 2 m... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1588430 Mon, 07 Jul 2008 18:03:49 +0100 1588430 http://www.medworm.com/index.php?rid=1588429&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%3D18412020%26dopt%3DAbstract Conclusion: Nitric oxide-independent activation of sGC might be an innovative therapeutic approach for the treatment of liver fibrosis of necro-inflammatory and immunological origin. PMID: 18412020 [PubMed - indexed for MEDLINE] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1588429 Mon, 07 Jul 2008 18:03:49 +0100 1588429 http://www.medworm.com/index.php?rid=1588428&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%3D18412021%26dopt%3DAbstract In conclusion, tamsulosin (0.05 and 0.1 mg/kg) and D-004 (400-800 mg/kg) dose-dependently inhibited the VM reduction induced with PHE, their combined therapy producing the greater effects. PMID: 18412021 [PubMed - indexed for MEDLINE] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1588428 Mon, 07 Jul 2008 18:03:49 +0100 1588428 http://www.medworm.com/index.php?rid=1588427&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%3D18412022%26dopt%3DAbstract Authors: Colombo D, Ferraboschi P, Franchini L, Nishino H, Takayasu J, Tokuda H The aim of this study was to evaluate the cancer chemopreventive potential of the widely prescribed drug tibolone (17alpha-ethynyl-7alpha-methyl-5(10)-estren-3-one, CAS 5630-53-5) and its main metabolites, 17alpha-ethynyl-7alpha-methyl-4-estren-3-one (CAS 1162-60-3), 17alpha-ethynyl-7alpha-methyl-5(10)-estrene-3alpha,17beta-diol (CAS 100239-44-9) and 17alpha-ethynyl-7alpha-methyl-5(10)-estrene-3beta,17beta-diol (CAS 100239-45-0), by studying their anti-tumor-promoting activity. To this aim the test compounds were submitted to the short term in vitro assay for the inhibition of Epstein-Barr virus early antigen (EBV-EA) activation induced by the tumor promoter 12-O-tetradecanoylphorbol-13-acetate (TPA) as a p... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1588427 Mon, 07 Jul 2008 18:03:49 +0100 1588427 http://www.medworm.com/index.php?rid=1588426&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%3D18412023%26dopt%3DAbstract Authors: Gonçalves TM, Bedor DC, de Abreu LR, de Sousa CE, Rolim CM, de Santana DP A simple, fast, sensitive and selective solid-phase extraction-liquid chromatography-tandem mass spectrometry (SPE-LC-MS/MS) method for the quantitative analysis of ampicillin (CAS 69-53-4) in human plasma was developed using amoxicillin as internal standard, and sample extraction by solid-phase extraction (SPE). Extracts were separated by reversed-phase C18 with aqueous mobile phase (acetonitrile, 80:20, v/v) with 0.1% formic acid. The method was validated and successfully applied in a bioequivalence study of capsules 500 mg of ampicillin. Using a short running time of 2.5 min, the lower limit of quantification (LLOQ) for obtained ampicillin was 0.1 microg/ml for a plasma sample of 250 microl and a... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1588426 Mon, 07 Jul 2008 18:03:49 +0100 1588426 http://www.medworm.com/index.php?rid=1588425&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%3D18412024%26dopt%3DAbstract Authors: Zakeri-Milani P, Valizadeh H, Islambulchilar Z The bioavailability of a new cefixime ((6R,7R)-7-[(Z)-2-(2-amino-4-thiazolyl)-2-(carboxymethoxyimino) acetamido]-8-oxo-3-vinyl-5-thia-1-azabicyclo-[4,2,0]-oct-2-ene-2-carboxylic acid, CAS 79350-37-1) tablet preparation (Loprax) was compared with that of a reference preparation of the drug in 24 healthy male volunteers. The trial was designed as an open, randomized, single-blind, two-sequence, two-period crossover study. Under fasting conditions, each subject received a single oral dose of 400 mg cefixime tablet as a test or reference formulation on 2 treatment days. The treatment periods were separated by a one-week washout period. The plasma concentrations of the drug were analyzed by a rapid and sensitive HPLC method with UV det... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1588425 Mon, 07 Jul 2008 18:03:49 +0100 1588425 http://www.medworm.com/index.php?rid=1588424&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%3D18488805%26dopt%3DAbstract Authors: Meza-Toledo SE, Yasutake-Kimoto L, Alcalá-Rentería M, Domínguez-Rodríguez MA, Jaime-Rodríguez R, Nava-Arzaluz MG, Gutiérrez-Laflor G, Peralta-Cruz J, Carvajal-Sandoval G The anticonvulsant activity of some DL-hydroxybenzenamides is described. The following compounds from this series were prepared and tested: DL-2-hydroxy-2-(3'-bromophenyl)butyramide (4, CAS 620950-12-1), DL-2-hydroxy-2-(4'-bromophenyl)butyramide (5, CAS 620950-13-2), DL-2-hydroxy-2-(3'-nitrophenyl)butyramide (6, CAS 620950-14-3), DL-2-hydroxy-2-phenyl hexanamide (7, CAS 63002-05-1), DL-2-hydroxy-2-(3',4'-dichlorophenyl)hexanamide (8, CAS 863976-06-1), DL-3-hydroxy-3-(4'-bromophenyl)pentanamide (9, CAS 620950-16-5), DL-3-hydroxy-3-phenyl-heptanamide (10, CAS 863976-08-3) and DL-4-h... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1588424 Mon, 07 Jul 2008 18:03:49 +0100 1588424 http://www.medworm.com/index.php?rid=1588423&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%3D18488806%26dopt%3DAbstract Authors: Liu Y, Xul FG, Zhang ZJ, Song R, Tian Y, Chen Y A sensitive and highly selective liquid chromatography-mass spectrometry (LCMS) method was developed to determine nitrendipine (4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3, 5-pyridinedicarboxylic acid ethyl methyl ester, CAS 39562-70-4) in human plasma. The analyte and the internal standard nimodipine (CAS 66085-59-4) were extracted from plasma samples by n-hexane-isopropanol (95:5, v/v), and analyzed on a commercially available column Interfaced with a mass spectrometer. Positive atmospheric pressure chemical ionization (APCI) was empolyed as the ionization source. The samples were detected by the use of selected ion monitoring (SIM) mode. The mobile phase consisted of methanol-water (75:25, v/v). The method has a limit of detect... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1588423 Mon, 07 Jul 2008 18:03:49 +0100 1588423 http://www.medworm.com/index.php?rid=1588422&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%3D18488807%26dopt%3DAbstract This study shows that the test formulation is bioequivalent to the reference formulation for spironolactone and its main active metabolite canrenone. PMID: 18488807 [PubMed - indexed for MEDLINE] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1588422 Mon, 07 Jul 2008 18:03:49 +0100 1588422 http://www.medworm.com/index.php?rid=1588421&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%3D18488808%26dopt%3DAbstract This study was conducted in order to assess the bioequivalence of two tablet formulations containing 100 mg sildenafil (1-[4-ethoxy-3-(6,7-dihydro-1-,ethyl-7-oxo-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-5-yl)phenylsulphonyl] -4-methyl piperazine, CAS 139755-83-2). Twenty-eight healthy subjects were enrolled in a single-centre, randomised, single-dose, open-label, 2-way crossover study, with a minimum washout period of 7 days. Plasma samples were collected up to 18.0 h postdosing. Sildenafil levels were determined by reverse liquid chromatography coupled with tandem mass spectrometry detection (LC-MS/MS). Pharmacokinetic parameters used for bioequivalence assessment [area under the concentration-time curve from time zero to time of last non-zero concentration (AUC(last)) and maximum observed co... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1588421 Mon, 07 Jul 2008 18:03:49 +0100 1588421 http://www.medworm.com/index.php?rid=1588420&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%3D18488809%26dopt%3DAbstract CONCLUSIONS: D-003 (5-250 mg/kg) orally administered for 4 weeks was more effective than policosanol for lowering all the lipid peroxidation markers assessed, like plasma MDA and total peroxides, and MDA concentrations generated by the enzymatic and non-enzymatic oxidant systems of liver homogenates. The inhibitions with D-003 were marked and dose-dependent. Neither D-003 nor policosanol modified the activity of enzymes involved in the endogenic antioxidant defensive system. PMID: 18488809 [PubMed - indexed for MEDLINE] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1588420 Mon, 07 Jul 2008 18:03:49 +0100 1588420 http://www.medworm.com/index.php?rid=1588419&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%3D18488810%26dopt%3DAbstract In this study, a series of thiazolyl-2,4-thiazolidinediones (VIa-f, VIHa-f and VIIa-f) was prepared by Knoevenagel reaction of substituted phenacyl-2,4-thiazolidinediones (IVa-f)/substituted benzyl-2,4-thiazolidinediones (Va-f) with chlorothiazolecarbaldehydes (II, III).The prepared compounds were tested for their insulinotropic activities in INS-1 cells. A significant insulinotropic effect was seen with compounds VIa, VIb, VIe, VIIa, VIIb and VIIId. Introducing a 2-[(phenylethyl)thio] group into the thiazole ring increased the biological effect, whereas NO2 groups in phenylacyl or benzyl groups diminished the effects. PMID: 18488810 [PubMed - indexed for MEDLINE] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1588419 Mon, 07 Jul 2008 18:03:49 +0100 1588419 http://www.medworm.com/index.php?rid=1588418&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%3D18488811%26dopt%3DAbstract Authors: Di Loreto VE, Roma SM, Menoyo I, Rigalli A Clinical course of pancreatitis depends partially on the proteinases-antiproteinases balance. Monofluorophosphate (CAS 10163-15-2, MFP) binds to plasmatic antiproteinase alpha-macroglobulin (AM), modifies its homeostasis and, as a consequence, has potential effects on the progression of pancreatitis and other inflammatory processes. The progress of incomplete closed duodenal loop induced pancreatitis was studied in rats with AM homeostasis perturbed by the oral administration of MFP. Twelve rats received 80 micromol MFP/day orally for one month before the induction of pancreatitis. Controls did not receive MFP. Plasmatic amylase activity and AM levels were measured. The day of death was recorded and histopathology of pancreas was perf... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1588418 Mon, 07 Jul 2008 18:03:49 +0100 1588418 http://www.medworm.com/index.php?rid=1588417&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%3D18488812%26dopt%3DAbstract CONCLUSION: Since the 90% CI for AUC(last) and C(max) ratios were within the 80-125% interval proposed by the US FDA, it was concluded that pantoprazole 40 mg DR tablet (test formulation) with and without food was bioequivalent to the reference 40 mg DR tablet for both the rate and extent of absorption. PMID: 18488812 [PubMed - indexed for MEDLINE] (Source: Arzneimittel-Forschung) Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1588417 Mon, 07 Jul 2008 18:03:49 +0100 1588417 http://www.medworm.com/index.php?rid=1588416&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%3D18488813%26dopt%3DAbstract Authors: Zaid AN, Alhaique F, Kort J, Sweileh W The aim of this study was to compare the bioavailability, after oral administration, of the generic "Adcef Suspension" (test) (125 mg/5 ml cefdinir; CAS 91832-40-5), with that of a commercially available original preparation (reference) (125 mg/ 5 ml cefdinir). For this purpose a randomized, two-way, crossover, bioequivalence study was performed in 24 healthy, male volunteers. The Middle Eastern selected volunteers were divided into two groups of 12 subjects. One group was treated with the reference standard and the other one with the test, with a crossover after the drug washout period of 7 days. Blood samples were collected at fixed time intervals and cefdinir concentrations were determined by a validated HPLC assay method. The pharmaco... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1588416 Mon, 07 Jul 2008 18:03:49 +0100 1588416 http://www.medworm.com/index.php?rid=1588415&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%3D18540476%26dopt%3DAbstract Authors: Meza-Toledo SE, Lira-Zárate F, Robles-Martínez EL, Peralta-Alvarez B, Cabrera-Cedillo F, Peralta-Cruz J, Cruz-Peinado C, Miñón-López H DL-2-Hydroxy-2-phenyl butyramide (1, CAS 52839-87-9), DL-3-hydroxy-3-phenyl pentanamide (2, CAS 131802-69-2) and DL-4-hydroxy-4-phenyl hexanamide (3, CAS 67880-30-2) are anticonvulsants. Searching for more active compounds, some DL-fluorobenzenamides were prepared and tested: DL-2-hydroxy-2-(3'-trifluoromethylphenyl)butyramide (4), DL-2-Hydroxy-2-4'-trifluoromethylphenyl) butyramide (5, CAS 620950-10-9), DL-2-hydroxy-2-[3',5'-bis(trifluoromethyl)phenyl]butyramide (6, CAS 620950-09-6), DL-3-hydroxy-3-(3'-trifluoromethylphenyl) pentanamide (7), DL-3-hydroxy-3-(4'-trifluoromethylphenyl)pentanamide (8), and DL-3-hydroxy-3-[... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1588415 Mon, 07 Jul 2008 18:03:49 +0100 1588415 http://www.medworm.com/index.php?rid=1588414&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%3D18540477%26dopt%3DAbstract Authors: Seif-El-Nasr M, Atia AS, Abdelsalam RM An increasing number of reports suggest the involvement of oxidative stress in neurodegenerative diseases where the increased formation of reactive oxygen species (ROS) leads to neuronal damage and cell death. Dopamine may contribute to neurodegenerative disorders such as Parkinson's disease and ischemia/reperfusion-induced damage. Monoamine oxidase (MAO) enzyme (particularly MAO-B) is responsible for metabolizing dopamine and plays an important role in oxidative stress through altering the redox state of neuronal and glial cells. MAO participates in the generation of hydroxyl radicals during ischemia/reperfusion. This suggests the possible use of MAO inhibitors as neuroprotective agents for treating ischemic injury. The protective effect... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1588414 Mon, 07 Jul 2008 18:03:49 +0100 1588414 http://www.medworm.com/index.php?rid=1588413&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%3D18540478%26dopt%3DAbstract The objective of this post-marketing surveillance (PMS) was the evaluation of efficacy, tolerability, and acceptance of the advanced formoterol (CAS 73573-87-2) multidose dry powder inhaler (MDPI) Formatris 6 microg/12 microg Novolizer (FN) in asthmatic patients (n = 5219) in a real-life setting. A total of 2727 patients (52%) received concomitant anti-inflammatory treatment exclusively via a budesonide Novolizer (BN). Efficacy of the FN was assessed by measurement of peak expiratory flow (PEF) and forced expiratory volume in one second (FEV1) before and after 4 weeks of therapy. The severity of cough, wheezing, diurnal dyspnea, nocturnal dyspnea and dyspnea on physical effort were assessed on a four-point scale, and a severity sum score was calculated. The patients' satisfaction with the ... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1588413 Mon, 07 Jul 2008 18:03:49 +0100 1588413 http://www.medworm.com/index.php?rid=1588412&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%3D18540479%26dopt%3DAbstract Authors: Alagarsamy V, Solomon VR, Murugesan S A variety of novel 3-(2-methylphenyl)-2-substituted amino-quinazolin-4(3H)-ones were synthesized by reacting the amino group of 2-hydrazino-3-(2-methylphenyl)-quinazolin-4(3H)-one with a variety of aldehydes and ketones. The starting material 2-hydrazino-3-(2-methylphenyl)-quinazolin-4(3H)-one was synthesized from 2-methyl aniline. The title compounds were investigated for analgesic, anti-inflammatory and ulcerogenic index activities. Among these, the compound 2-(1-ethylpropylidene)-hydrazino-3-(2-methylphenyl)-quinazolin-4(3H)-one emerged as the most active compound for analgesic activity, while the compound 2-(1-methylbutylidene)-hydrazino-3-(2-methylphenyl)-quinazolin-4(3H)-one showed most potent anti-inflamma-tory activity of the serie... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1588412 Mon, 07 Jul 2008 18:03:49 +0100 1588412 http://www.medworm.com/index.php?rid=1588411&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%3D18540480%26dopt%3DAbstract Authors: Canudas N, Figueroa L, Zamora D, Villamizar JE, Guedez A, Fuentes JM, Castelli C, Taddei A The photobiological properties of 4-acetylaminophenylacetic acid (Actarit, ACT, MS-932, CAS 18699-02-0) were studied using in vitro phototoxicity assays: photohemolysis, photoperoxidation of linoleic acid and Candida sp phototoxicity test. ACT reduced nitro blue tetrazolium (NBT) when irradiated with lambda > or = 300 nm in deoxygenated aqueous buffer solution (pH 7.4). The photohemolysis rate and photoperoxidation of linoleic acid were inhibited significantly by reduced glutathione. ACT was phototoxic to Candida sp. The isolation and identification of the photodegradation products of ACT in phosphate buffered saline solution (pH 7.4) and methanol were studied under aerobic conditions... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1588411 Mon, 07 Jul 2008 18:03:49 +0100 1588411 http://www.medworm.com/index.php?rid=1588410&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%3D18540481%26dopt%3DAbstract Authors: Zakeri-Milani P, Valizadeh H, Islambulchilar Z, Damani S, Mehtari M The primary endpoint of this study was to determine the intestinal permeability of ciclosporin (cyclosporine A, CsA, CAS 59865-13-3) using the single-pass intestinal perfusion technique (SPIP) and a range of concentrations in rats. The second objective was to assess the quantitative contribution of P-glycoprotein (P-gp)-mediated efflux in limiting the oral bioavailability of CsA using erythromycin (Ery, CAS 114-07-8) as an inhibitor of P-gp efflux transporter. A solution containing CsA and phenol red either in the presence or in the absence of Ery as a P-gp inhibitor was perfused through a cannulated jejunal segment in rats. Outlet samples were collected every 10 min in micro tubes up to 90 min. Samples were a... Arzneimittel-Forschung journals http://www.medworm.com/rss/comments.php?id=1588410 Mon, 07 Jul 2008 18:03:49 +0100 1588410