Arzneimittel-ForschungThis is an RSS file. You can use it to subscribe to this data in your favourite RSS reader, such as GoogleReader, or to display this data on your own website or blog. Subscribe to this data using MyMedWorm.Subscribe to this data using GoogleReader.Subscribe to this data using Bloglines.Subscribe to this data using MyYahoo.

This page shows you the latest items in this publication.

Pages: 1 2 3 4 5

205 records returned

Effect of darbepoetin alfa on renal anemia in Japanese hemodialysis patients.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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)
Source: Arzneimittel-Forschung - October 29, 2009 Category: Drugs & Pharmacology Authors: Kusaba T, Ishida R, Nakayama M, Kato H, Uchiyama H, Sato K, Mori Y, Matsubara H, Kajita Y Tags: Arzneimittelforschung Source Type: journals

Pharmacokinetics and bioequivalence study of two cetirizine hydrochloride formulations in healthy Chinese male volunteers.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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)
Source: Arzneimittel-Forschung - October 29, 2009 Category: Drugs & Pharmacology Authors: Xu FG, Liu Y, Zhang ZJ, Tian Y, Chen Y Tags: Arzneimittelforschung Source Type: journals

Effects of increasing the dose of pravastatin on serum adiponectin level in Japanese mild hypercholesterolemic and hypertensive patients.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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 level...
Source: Arzneimittel-Forschung - October 29, 2009 Category: Drugs & Pharmacology Authors: Kai T, Kanamasa K Tags: Arzneimittelforschung Source Type: journals

Pharmacokinetics and bioequivalence study of a fixed dose combination of rabeprazole and itopride in healthy Indian volunteers.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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. Rabepraz...
Source: Arzneimittel-Forschung - October 29, 2009 Category: Drugs & Pharmacology Authors: Sahoo BK, Das A, Agarwal S, Bhaumik U, Bose A, Ghosh D, Roy B, Pal TK Tags: Arzneimittelforschung Source Type: journals

Pharmacokinetics of isoxsuprine hydrochloride administered orally and intramuscularly to female healthy volunteers.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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, crossove...
Source: Arzneimittel-Forschung - October 29, 2009 Category: Drugs & Pharmacology Authors: Marzo A, Zava D, Coa K, Dal Bo L, Ismaili S, Tavazzi S, Cantoni V Tags: Arzneimittelforschung Source Type: journals

Pharmacokinetics characterization of liposomal amphotericin B: investigation of clearance process and drug interaction potential.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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 investigate...
Source: Arzneimittel-Forschung - October 29, 2009 Category: Drugs & Pharmacology Authors: Matsui S, Imai S, Yabuki M, Komuro S Tags: Arzneimittelforschung Source Type: journals

Bioequivalence study of two azithromycin formulations in healthy subjects.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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%)...
Source: Arzneimittel-Forschung - October 29, 2009 Category: Drugs & Pharmacology Authors: Setiawati E, Deniati SH, Yunaidi DA, Handayani LR, Harinanto G, Santoso ID, Sari AP, Rimainar A Tags: Arzneimittelforschung Source Type: journals

Substitution of theophylline slow-release formulations according to the rebate contracts in the German statutory health insurance.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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 con...
Source: Arzneimittel-Forschung - October 29, 2009 Category: Drugs & Pharmacology Authors: Weissenfeld J, Lüngen M, Stock S, Drabik A, Gerber A Tags: Arzneimittelforschung Source Type: journals

Liquid chromatography-mass spectrometry method for the determination of amlodipine in human plasma and its application in a bioequivalence study.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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 lowe...
Source: Arzneimittel-Forschung - October 11, 2009 Category: Drugs & Pharmacology Authors: Zou Q, Zhan Y, Ge Z, Wei P, Ouyang P Tags: Arzneimittelforschung Source Type: journals

Bioequivalence study of two tablet formulations of ramipril in healthy volunteers.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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 bioequiva...
Source: Arzneimittel-Forschung - October 11, 2009 Category: Drugs & Pharmacology Authors: Allegrini A, Nuzzo L, Zucchelli M, Tavella-Scaringi A, Bucci M, Pavone D, Toniato E, Mezzetti A, Martinotti S, Bonani S Tags: Arzneimittelforschung Source Type: journals

Truncated area under the urinary excretion rate curve in the evaluation of alendronate bioequivalence after a single dose in healthy volunteers.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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....
Source: Arzneimittel-Forschung - October 11, 2009 Category: Drugs & Pharmacology Authors: Portolés A, Prieto E, Calvo A, Laredo L, Fernández N, Vargas E Tags: Arzneimittelforschung Source Type: journals

Efficacy and safety of piroxicam patch versus piroxicam cream in patients with lumbar osteoarthritis. A randomized, placebo-controlled study.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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)
Source: Arzneimittel-Forschung - October 11, 2009 Category: Drugs & Pharmacology Authors: Allegrini A, Nuzzo L, Pavone D, Tavella-Scaringi A, Giangreco D, Bucci M, Toniato E, Mezzetti A, Martinotti S, Comuzio S, Di Grigoli M, Bonani S Tags: Arzneimittelforschung Source Type: journals

Possible link between history of hypersensitivity to a specific non-steroidal anti-inflammatory drug (NSAID) and positive results following challenge test to alternative NSAIDS.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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)
Source: Arzneimittel-Forschung - October 11, 2009 Category: Drugs & Pharmacology Authors: Trombetta D, Imbesi S, Vita G, Isola S, Minciullo PL, Saija A, Gangemi S Tags: Arzneimittelforschung Source Type: journals

Synthesis of novel tadalafil analogues and their evaluation as phosphodiesterase inhibitors and anticancer agents.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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 proces...
Source: Arzneimittel-Forschung - October 11, 2009 Category: Drugs & Pharmacology Authors: Abadi AH, Abouel-Ella DA, Ahmed NS, Gary BD, Thaiparambil JT, Tinsley HN, Keeton AB, Piazza GA Tags: Arzneimittelforschung Source Type: journals

Chromatographic/mass spectrometric method for the estimation of itraconazole and its metabolite in human plasma. Application to a bioequivalence study.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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 ...
Source: Arzneimittel-Forschung - October 11, 2009 Category: Drugs & Pharmacology Authors: Grabowski T, Swierczewska A, Borucka B, Sawicka R, Sasinowska-Motyl M, Gumułka SW Tags: Arzneimittelforschung Source Type: journals

Pharmacokinetics and comparative bioavailability study of two clarithromycin suspensions following administration of a single oral dose to healthy volunteers.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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 d...
Source: Arzneimittel-Forschung - October 11, 2009 Category: Drugs & Pharmacology Authors: Zakeri-Milani P, Valizadeh H, Ghanbarzadeh S, Nemati M Tags: Arzneimittelforschung Source Type: journals

Antacid use and reduced bioavailability of oral drugs. Case studies, overview and perspectives.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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 th...
Source: Arzneimittel-Forschung - September 6, 2009 Category: Drugs & Pharmacology Authors: Srinivas NR Tags: Arzneimittelforschung Source Type: journals

Cyproterone acetate quantification in human plasma by high-performance liquid chromatography coupled to atmospheric pressure photoionization tandem mass spectrometry. Application to a comparative pharmacokinetics study.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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/...
Source: Arzneimittel-Forschung - September 6, 2009 Category: Drugs & Pharmacology Authors: Borges NC, Mazuqueli A, Moreno RA, Astigarraga RB, Sverdloff CE, Galvinas PA, Sampaio MR, da Silva WM Tags: Arzneimittelforschung Source Type: journals

Bioequivalence of fexofenadine tablet formulations assessed in healthy Iranian volunteers.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
CONCLUSION: Based on the obtained results the two fexofenadine formulations are considered to be equivalent. PMID: 19728561 [PubMed - in process] (Source: Arzneimittel-Forschung)
Source: Arzneimittel-Forschung - September 6, 2009 Category: Drugs & Pharmacology Authors: Valizadeh H, Barghi L, Jalilian H, Islambulchilar Z, Zakeri-Milani P Tags: Arzneimittelforschung Source Type: journals

Design, synthesis and pharmacological evaluation of a series of 5-carbethoxy-4-chloro-6-(substituted amino)pyrimidines as potential analgesic and anti-flammatory agents with very low ulcerogenic potential.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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...
Source: Arzneimittel-Forschung - September 6, 2009 Category: Drugs & Pharmacology Authors: Chhabria MT, Shishoo CJ, Vaghela DK, Patel SM, Satia MC Tags: Arzneimittelforschung Source Type: journals

Synthesis and analgesic and anti-inflammatory activity of 6-phenyl/(4-methylphenyl)-3(2H)-pyridazinon-2-propionamide derivatives.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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)-...
Source: Arzneimittel-Forschung - September 6, 2009 Category: Drugs & Pharmacology Authors: Gökçe M, Colak MS, Küpeli E, Sahin MF Tags: Arzneimittelforschung Source Type: journals

Cytotoxicity of 1-aryl-3-buthylamino-1-propanone hydrochlorides against Jurkat and L6 cells.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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...
Source: Arzneimittel-Forschung - September 6, 2009 Category: Drugs & Pharmacology Authors: Gul M, Mete E, Atalay M, Arik M, Gul HI Tags: Arzneimittelforschung Source Type: journals

Bioavailability of a co-formulated combination of amodiaquine and artesunate under fed and fasted conditions. A randomised, open-label crossover study.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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)
Source: Arzneimittel-Forschung - September 6, 2009 Category: Drugs & Pharmacology Authors: Fitoussi S, Thang C, Lesauvage E, Barré J, Charron B, Filali-Ansary A, Lameyre V Tags: Arzneimittelforschung Source Type: journals

Mean residence time as estimated from cropped and truncated moments.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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)
Source: Arzneimittel-Forschung - September 6, 2009 Category: Drugs & Pharmacology Authors: Keller F, Hartmann B, Czock D Tags: Arzneimittelforschung Source Type: journals

Proton pump inhibitors--their pharmacological impact on the clinical management of acid-related disorders.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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...
Source: Arzneimittel-Forschung - July 31, 2009 Category: Drugs & Pharmacology Authors: Klotz U Tags: Arzneimittelforschung Source Type: journals

Evaluation of the inhibitory effect of dihydropyridines on N-type calcium channel by virtual three-dimensional pharmacophore modeling.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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 1235...
Source: Arzneimittel-Forschung - July 31, 2009 Category: Drugs & Pharmacology Authors: Ogihara T, Kano T, Kakinuma C Tags: Arzneimittelforschung Source Type: journals

Usefulness of the parent compound determination in bioequivalence evaluation of clopidogrel generic products.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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)
Source: Arzneimittel-Forschung - July 31, 2009 Category: Drugs & Pharmacology Authors: Pawłowska M, Duda J, Tejchman-Małecka B, Bogiel M, Marzec A, Sieradzki E Tags: Arzneimittelforschung Source Type: journals

Bioequivalence study of two different clopidogrel bisulfate film-coated tablets.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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)
Source: Arzneimittel-Forschung - July 31, 2009 Category: Drugs & Pharmacology Authors: Richter W, Erenmemisoglu A, Van der Meer MJ, Emritte N, Tuncay E, Koytchev R Tags: Arzneimittelforschung Source Type: journals

Effects of oral iron(III) hydroxide polymaltose complex supplementation on hemoglobin increase, cognitive function, affective behavior and scholastic performance of adolescents with varying iron status: a single centre prospective placebo controlled study.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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)
Source: Arzneimittel-Forschung - July 31, 2009 Category: Drugs & Pharmacology Authors: Devaki PB, Chandra RK, Geisser P Tags: Arzneimittelforschung Source Type: journals

Allometric scaling of a metabolically complex camptothecin analog: differences in scaling of irinotecan and its active metabolite, SN-38.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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;...
Source: Arzneimittel-Forschung - July 31, 2009 Category: Drugs & Pharmacology Authors: Ahlawat P, Srinivas NR Tags: Arzneimittelforschung Source Type: journals

[Justification of repeated animal experiments and determination of the required number of animals according to the German Animal Protection Act]Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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 statistic...
Source: Arzneimittel-Forschung - July 31, 2009 Category: Drugs & Pharmacology Authors: Schneider B Tags: Arzneimittelforschung Source Type: journals

Effects of nitric oxide donor antioxidants containing the phenol vitamin E substructure and a furoxan moiety on ischemia/reperfusion injury.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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 m...
Source: Arzneimittel-Forschung - June 27, 2009 Category: Drugs & Pharmacology Authors: Di Stilo A, Chegaev K, Lazzarato L, Fruttero R, Gasco A, Rastaldo R, Cappello S Tags: Arzneimittelforschung Source Type: journals

Comparative bioavailability of propafenone after administration of a magistral suspension vs. commercial tablets in healthy volunteers.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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 ...
Source: Arzneimittel-Forschung - June 27, 2009 Category: Drugs & Pharmacology Authors: Juárez Olguín H, Flores Pérez C, Ramírez Mendiola B, Barranco Garduño L, Sandoval Ramírez E, Flores Pérez J Tags: Arzneimittelforschung Source Type: journals

Quantitative determination of ticlopidine hydrochloride in human plasma by high-performance liquid chromatography-electronspray ionization mass spectrometry.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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 ...
Source: Arzneimittel-Forschung - June 27, 2009 Category: Drugs & Pharmacology Authors: Sun J, Jiao H, Tian Y, Zhang Z, Chen Y Tags: Arzneimittelforschung Source Type: journals

Antioxidative and lipid lowering effects of 7,8-dihydroxy-3- (4-methylphenyl) coumarin in hyperlipidemic rats.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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 ...
Source: Arzneimittel-Forschung - June 27, 2009 Category: Drugs & Pharmacology Authors: Yuce B, Danis O, Ogan A, Sener G, Bulut M, Yarat A Tags: Arzneimittelforschung Source Type: journals

Fast HPLC method for the determination of ketoprofen in human plasma using a monolithic column and its application to a comparative bioavailability study in man.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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 w...
Source: Arzneimittel-Forschung - June 27, 2009 Category: Drugs & Pharmacology 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 Tags: Arzneimittelforschung Source Type: journals

Liquid chromatographic-mass spectrometry analysis and pharmacokinetic studies of erianin for intravenous injection in dogs.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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)
Source: Arzneimittel-Forschung - June 27, 2009 Category: Drugs & Pharmacology Authors: Zhou H, Yang B, Hong M, Ma R, Sheng L Tags: Arzneimittelforschung Source Type: journals

Comparison of primary human fibroblasts and keratinocytes with immortalized cell lines regarding their sensitivity to sodium dodecyl sulfate in a neutral red uptake cytotoxicity assay.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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 result...
Source: Arzneimittel-Forschung - June 27, 2009 Category: Drugs & Pharmacology Authors: Olschläger V, Schrader A, Hockertz S Tags: Arzneimittelforschung Source Type: journals

Considerations for metabolite pharmacokinetic data in bioavailability/bioequivalence assessments. Overview of the recent trends.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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 o...
Source: Arzneimittel-Forschung - June 27, 2009 Category: Drugs & Pharmacology Authors: Srinivas NR Tags: Arzneimittelforschung Source Type: journals

Comparative bioavailability study of amisulpride tablets in healthy Indian volunteers.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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 s...
Source: Arzneimittel-Forschung - June 27, 2009 Category: Drugs & Pharmacology Authors: Das A, Bhaumik U, Chakrabarty US, Sarkar AK, Ghosh A, Bose A, Chatterjee B, Pal TK Tags: Arzneimittelforschung Source Type: journals

Bioequivalence and pharmacokinetic study of two different omeprazole capsule formulations in healthy Bangladeshi volunteers.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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 crosso...
Source: Arzneimittel-Forschung - June 27, 2009 Category: Drugs & Pharmacology Authors: Joti JJ, Nahar K, Hasan A, Azad MA, Ullah MA, Islam SM, Hasnat A Tags: Arzneimittelforschung Source Type: journals

Differences between original intravenous iron sucrose and iron sucrose similar preparations.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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 t...
Source: Arzneimittel-Forschung - June 27, 2009 Category: Drugs & Pharmacology Authors: Toblli JE, Cao G, Oliveri L, Angerosa M Tags: Arzneimittelforschung Source Type: journals

Comparative bioavailability of two dexamethasone tablet formulations in Indonesian healthy volunteers.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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)
Source: Arzneimittel-Forschung - June 27, 2009 Category: Drugs & Pharmacology Authors: Harahap Y, Sasongko L, Prasaja B, Indriati E, Lusthom W, Lipin Tags: Arzneimittelforschung Source Type: journals

Design and synthesis of some (S)-2-(6-methoxynaphthalen-2-yl)-N-substituted ethyl propanamide derivatives as potent non-ulcerogenic anti-inflammatory and analgesic agents.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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 c...
Source: Arzneimittel-Forschung - June 27, 2009 Category: Drugs & Pharmacology Authors: Berk B, Erol DD, Kupeli E, Yesilada E Tags: Arzneimittelforschung Source Type: journals

Synthesis and study on analgesic effects of 1-[1-(4-methylphenyl) (cyclohexyl)] 4-piperidinol and 1-[1-(4-methoxyphenyl) (cyclohexyl)] 4-piperidinol as two new phencyclidine derivatives.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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 ac...
Source: Arzneimittel-Forschung - June 27, 2009 Category: Drugs & Pharmacology Authors: Ahmadi A, Khalili M, Abbassi S, Javadi M, Mahmoudi A, Hajikhani R Tags: Arzneimittelforschung Source Type: journals

In vitro effect of a new cinnamic acid derivative against the epimastigote form of Trypanosoma cruzi.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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 spec...
Source: Arzneimittel-Forschung - June 27, 2009 Category: Drugs & Pharmacology Authors: Pardo Andreu GL, Inada NM, Pellón RF, Docampo ML, Fascio ML, D'Accorso NB, Vercesi AE Tags: Arzneimittelforschung Source Type: journals

Relevance of metabolic activation pathways: the example of clopidogrel and prasugrel.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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, pras...
Source: Arzneimittel-Forschung - June 27, 2009 Category: Drugs & Pharmacology Authors: Petersen KU Tags: Arzneimittelforschung Source Type: journals

Pharmacokinetics and bioequivalence study of escitalopram oxalate formulations after single-dose administration in healthy Chinese male volunteers.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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 wit...
Source: Arzneimittel-Forschung - June 27, 2009 Category: Drugs & Pharmacology Authors: Li J, Tian Y, Zhang ZJ, Wang N, Ren X, Chen Y Tags: Arzneimittelforschung Source Type: journals

Bioequivalence evaluation of rilmenidine in healthy volunteers.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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 concen...
Source: Arzneimittel-Forschung - June 27, 2009 Category: Drugs & Pharmacology Authors: Groenewoud G, Potgieter L, Meyer B Tags: Arzneimittelforschung Source Type: journals

Bioequivalence study with two different oral formulations of methocarbamol in healthy subjects. A mono-centre, comparative, randomized, open-label, single-dose, 2-way crossover study.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
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)
Source: Arzneimittel-Forschung - June 27, 2009 Category: Drugs & Pharmacology Authors: Schlegelmilch R, Eydeler AU, Barkworth M, Radeke A Tags: Arzneimittelforschung Source Type: journals