European Journal of Drug Metabolism and Pharmacokinetics
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Protein Binding and Stability of Drug Candidates: The Achilles’ Heel in In Vitro Potency Assays
European Journal of Drug Metabolism and Pharmacokinetics - Tập 45 - Trang 427-432 - 2020
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
Herb-drug interaction between irinotecan and psoralidin-containing herbs
European Journal of Drug Metabolism and Pharmacokinetics - Tập 40 - Trang 481-484 - 2014
Herb-drug interaction strongly limits the clinical utilization of herbs and drugs. Irinotecan-induced diarrhea is closely related with the UDP-glucuronosyltransferase 1A1-catalyzed glucuronidation of SN-38 which has been widely regarded to be the toxic substance basis of irinotecan. The present study aims to determine the influence of herbal component psoralidin toward the toxicity of irinotecan. ...... hiện toàn bộ
Effects of capsaicinoids on oxidative metabolism of caffeine in isolated rat hepatocytes
European Journal of Drug Metabolism and Pharmacokinetics - Tập 20 - Trang 179-184 - 1995
The metabolism of caffeine was studied in isolated rat hepatocytes, in the absence and presence of capsaicinoids. Caffeine and four primary metabolite fractions were identified by high performance liquid chromatography: 1,7-dimethylxanthine, 3,7-dimethylxanthine, 1,3-dimethylxanthine and 1,3,7-trimethyluric acid. The incubation with the lowest concentrations (0.1 and 1 μM) of capsaicinoids (natura...... hiện toàn bộ
Effects of phenobarbital and 3-methylcholanthrene pretreatment on the pharmacokinetics of praziquantel in rats
European Journal of Drug Metabolism and Pharmacokinetics - Tập 18 - Trang 261-264 - 1993
The effects of phenobarbital (PB) and 3-methylcholanthrene (MC) pretreatment on the pharmacokinetics of praziquantel (PZQ), a schistosomicide were studied in Sprague-Dawley rats. Blood samples at different time intervals were obtained by severing the tail vein and were analyzed for unchanged PZQ by HPLC. The PB-pretreated rats showed a 6-fold decrease in AUC, a 5-fold decrease in Cmax and an 8-fol...... hiện toàn bộ
Maximal biliary transport of sulfobromophthalein in patients with a T-tube placed in the common bile duct
European Journal of Drug Metabolism and Pharmacokinetics - Tập 22 - Trang 135-139 - 1997
In 19 adult patients with choledocholithiasis who were operated on, excretion of free and conjugated sulfobromophthalein (BSP) in the bile collected through a T-tube inserted in the common bile duct was determined. The transport maximum (Tm) for BSP was calculated by the constant-infusion technique after an intravenous infusion of the dye at a rate of 0.3 and 0.09 mg/kg/min for the first and secon...... hiện toàn bộ
Pharmakokinetik und Biotransformation von N-Propyl-ajmalin-hydrogentartrat beim Menschen
European Journal of Drug Metabolism and Pharmacokinetics - - 1982
Nach Applikation von N-Propyl-ajmalin-hydrogentartrat (N-PAB, Neo-Gilurytmal®) in den Dosierungen 10 mg i.v. und 20 mg p.o. wurden Pharmakokinetik und Metabolismus an sechs gesunden männlichen Freiwilligen untersucht. Für die Untersuchung wurde14C-markiertes N-PAB verwendet. N-PAB wird schnell und vollständig resorbiert. Die Bioverfügbarkeit beträgt 78%. Die Eliminationshalbwertszeit für die Mutte...... hiện toàn bộ
Influence of phenylbutazone, mofebutazone and aspirin on the pharmacokinetics of dexamethasone in the rat
European Journal of Drug Metabolism and Pharmacokinetics - Tập 6 - Trang 11-20 - 1981
Phenylbutazone suppresses the C-6 hydroxylation, absorption rate, bioavailability, and renal and plasma clearance rates of dexamethasone administered orally to normal and oedemateous rats. It increases the half life and the volume of distribution. Aspirin exerts an effect which is less pronounced and involves the enhancement of the C-6 hydroxylation. Aspirin suppresses the half life and renal clea...... hiện toàn bộ
Chronopharmacokinetic and bioequivalence studies of two formulations of trimipramine after oral administration in man
European Journal of Drug Metabolism and Pharmacokinetics - Tập 14 - Trang 139-144 - 1989
The bioavailability of two oral formulations of trimipramine, tablets and solution, was performed in twelve healthy volunteers, in a cross-over study. Each formulation was administered in the morning after a fasted period, and in the evening after a meal, in order to evaluate the role of both administration time and food consumption on the plasma kinetic parameters, under usual therapeutic conditi...... hiện toàn bộ
Metabolism of small antimicrobial β2,2-amino acid derivatives by murine liver microsomes
European Journal of Drug Metabolism and Pharmacokinetics - Tập 37 - Trang 191-201 - 2012
We have investigated the in vitro metabolism of three small antimicrobial β2,2-amino acid derivatives (M
w < 500) that are highly potent against methicillin resistant Staphylococcus aureus, and are among the first compounds designed from small cationic antimicrobial peptides with potential for oral administration. The β2,2-amino acid derivatives are virtually completely resistant a...... hiện toàn bộ
Enantioselective Pharmacokinetics of Bambuterol in Preclinical Species: Does S-bambuterol Influence the Clearance of the R-antipode?
European Journal of Drug Metabolism and Pharmacokinetics - Tập 41 - Trang 197-198 - 2016
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