Protein Binding and Stability of Drug Candidates: The Achilles’ Heel in In Vitro Potency AssaysEuropean Journal of Drug Metabolism and Pharmacokinetics - Tập 45 - Trang 427-432 - 2020
Ranjeet P. Dash, Jennifer A. Thomas, Clint Rosenfeld, Nuggehally R. Srinivas
In the present scenario of drug discovery, several screening filters ensure a rigorous nomination of clinical candidates. One of these screens is the determination of IC50, the concentration of drug at half-maximal inhibitory concentration, also known as a potency assay. However, various nuances pertaining to the design, execution, and interpretation of in vitro potency results suggest a sizeable ...... hiện toàn bộ
An attempt to predict daily erythrocyte lithium fluctuationsEuropean Journal of Drug Metabolism and Pharmacokinetics - - 1995
Ö. Sögüt, C. Yalçinkaya, R. Saygili, I. Tuglular, A. Kayali
Erythrocyte lithium concentration, which is a better predictor of brain lithium levels than plasma lithium concentrations, possesses the disadvantage of precise hourly determination following the last intake. The variability in RBC lithium accumulation increases as the extracellular lithium concentration increases. This increase is also time dependent and it would be very useful if the pharmacokin...... hiện toàn bộ
Assessment and modulation of phillyrin absorption by P-gp using Caco-2 cells and MDR1-MDCKII cellsEuropean Journal of Drug Metabolism and Pharmacokinetics - Tập 36 - Trang 41-47 - 2011
Yun-Xia Li, Liang-Hong Ye, Xue-Hua Jiang, Cheng Peng
The study was to investigate the absorption mechanism and transport modulation of phillyrin by P-gp in Caco-2 cells and MDR1-MDCKII cells. Three concentrations of phillyrin were tested in transport studies. The absorptive transports of phillyrin in the two cell models were not concentration-dependent which indicated passive diffusion as the dominating process in the test concentrations. The absorp...... hiện toàn bộ
Pharmacokinetics and hepatic uptake of gliquidone affected by Huangqi injectionEuropean Journal of Drug Metabolism and Pharmacokinetics - Tập 39 - Trang 255-261 - 2013
Fan Zhang, Yuhui Wei, Yan Zhou, Dan Wang, Liting Zhou, Jianping Zhang, Xinan Wu
The root of Astragalus membranaceus also known as Huang Qi in China is a common traditional Chinese herb with extensive pharmacological activities. Huangqi injection (HI), a common preparation of Huang Qi, was wildly co-administered with gliquidone to treat diabetes mellitus and diabetic nephropathy in clinic of China. The aim of the study was to investigate the effect of HI on the pharmacokineti...... hiện toàn bộ
Single- and multiple-dose pharmacokinetics of inhaled indacaterol in healthy Chinese volunteersEuropean Journal of Drug Metabolism and Pharmacokinetics - Tập 40 - Trang 203-208 - 2014
Ji Jiang, Lilly Li, Hequn Yin, Ralph Woessner, Corinne Emotte, Ruobing Li, Sanjeev Khindri, Hu Pei
Indacaterol is an inhaled, ultra–long-acting β2-agonist that provides 24-h bronchodilation with once-daily dosing in patients with chronic obstructive pulmonary disorder. This study evaluated the pharmacokinetics, safety, and tolerability of multiple daily inhaled doses of indacaterol 150 or 300 μg once daily in healthy Chinese volunteers. This was a single-center, randomized, double-blind, multip...... hiện toàn bộ
EventsEuropean Journal of Drug Metabolism and Pharmacokinetics - - 1981
Clinical study on the bioequivalence of two tablet formulations of flurbiprofenEuropean Journal of Drug Metabolism and Pharmacokinetics - Tập 34 - Trang 1-5 - 2009
Latif Ozbay, Durisehvar Ozer Unal, Iclal Cakici, Ayşen Fenercioglu, Dilek Erol
Flurbiprofen (CAS 5104-49-4) is a member of phenylaikanoic acid derivative group of nonsteroid anti-inflammatory drugs. It exhibits anti-inflammatory, analgesic and antipyretic activities. Two different tablets containing flurbiprofen (FLU) were investipted in 24 healthy volunteers to prove the bioequivalence between both treatments after single oral dose administrations. Fluroben® 100 mg tablet a...... hiện toàn bộ
Influence of pregnancy on one-compartmental bio-metric blood loss calculations after cesarean section and gynaecological surgeryEuropean Journal of Drug Metabolism and Pharmacokinetics - Tập 33 - Trang 53-59 - 2008
Jovan Popović, Zorica Grujić
To date there are no data in the literature on the procedure for the indirect measurement of blood loss during cesarean section, based on the post-operative drop in haemoglobin (Hb), which has been due to the lack of biometrically determined parameters for the calculation of blood volume in pregnant women. This study was therefore conducted to determine the applicability of the drop in Hb levels b...... hiện toàn bộ
Comparison of the rapidity of onset of the therapeutic effect between nateglinide and mitiglinide by PK/PD analysis in ratsEuropean Journal of Drug Metabolism and Pharmacokinetics - Tập 37 - Trang 9-15 - 2011
Toshiyuki Takanohashi, Harumi Arisaka, Kazuyuki Ubukata, Masahiro Hayashi, Yasuhiko Yamada
Nateglinide and mitiglinide are immediate short-acting insulinotropic agents. Both are administered preprandially to control postprandial hyperglycemia. Glinide drugs are characterized by immediate onset as well as rapid disappearance of effect as compared with sulfonylurea drugs. We examined the rapidity of onset of the therapeutic effect between nateglinide and mitiglinide by pharmacokinetic/pha...... hiện toàn bộ