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http://dx.doi.org/10.1016/s0140-6736(95)90193-0 | DOI Listing |
Int J Mol Sci
October 2024
School of Pharmaceutical Science and Technology, Hangzhou Institute for Advanced Study, University of Chinese Academy of Sciences, Hangzhou 310058, China.
Piperine has been reported to inhibit the enzyme activity of cytochrome P450 (CYP) 3A4. The aim of this study was to develop and validate a physiologically based pharmacokinetic (PBPK) model for piperine and to predict potential food-drug interactions (FDIs) between piperine and CYP3A4 substrate drugs using these models. The PBPK model for piperine was successfully developed and validated.
View Article and Find Full Text PDFMetabolites
September 2024
Center of Excellence in Drug Interaction Science, Certara USA, 4 Radnor Corporate Center, Suite 350, Radnor, PA 19087, USA.
Background/objectives: Index substrates are used to understand the processes involved in pharmacokinetic (PK) drug-drug interactions (DDIs). The aim of this analysis is to review metabolite measurement in clinical DDI studies, focusing on index substrates for cytochrome P450 (CYP) enzymes, including CYP1A2 (caffeine), CYP2B6 (bupropion), CYP2C8 (repaglinide), CYP2C9 ((S)-warfarin, flurbiprofen), CYP2C19 (omeprazole), CYP2D6 (desipramine, dextromethorphan, nebivolol), and CYP3A (midazolam, triazolam).
Methods: All data used in this evaluation were obtained from the Certara Drug Interaction Database.
CPT Pharmacometrics Syst Pharmacol
January 2025
Bayer AG, Pharmacometrics/Modeling and Simulation, Systems Pharmacology & Medicine - PBPK, Leverkusen, Germany.
Gastrointestinal first-pass metabolism plays an important role in bioavailability and in drug-drug interactions. Physiologically-based pharmacokinetic (PBPK) modeling is a powerful tool to integrate these processes mechanistically. However, a correct bottom-up prediction of GI first-pass metabolism is challenging and depends on various model parameters like the level of enzyme expression and the basolateral intestinal mucosa permeability (P).
View Article and Find Full Text PDFThe octanol/water partition coefficient, P (logP), is a hydrophobicity index and is one of the determining factors of the pharmacokinetics of chemical compounds. LogP values obtained from in silico software, open chemistry databases, and in vitro liquid chromatography retention factors may vary. Some chemicals (boscalid, etoxazole, and permethrin) have up to four-order-magnitude differences in in silico/in vitro P values.
View Article and Find Full Text PDFBMC Pharmacol Toxicol
September 2024
Laboratory of Regulatory Science, Faculty of Pharmacy, Musashino University, 1-1-20 Shinmachi, Nishitokyo-shi, Tokyo, 202-8585, Japan.
Background: Triazolam is a typical drug commonly used in the elderly; however, there have been concerns about its adverse events resulting from age-related changes in physiological function and drug interactions with concomitant drugs. Thus, updated information contributing to the appropriate use based on the latest pharmacokinetic and post-marketing surveillance methods is needed. In this study, we evaluated the appropriate use of triazolam in the elderly by integrating real-world data with a modeling and simulation approach.
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