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Establishing population distribution of drug‐metabolizing enzyme activities for the use of salivary caffeine as a dynamic liver function marker in a Singaporean Chinese population
ABSTRACT Salivary paraxanthine/caffeine molar ratio has been proposed as a novel dynamic liver function test to guide dose adjustments of drugs hepatically‐cleared by CYP1A2. Its usability requires an established population norm as well as the factors influencing the ratio and actual concentrations. To address this knowledge gap, we measured salivary caffeine and paraxanthine concentrations at 4 h post caffeine dose in healthy Chinese individuals who have undergone 24 h of caffeine abstinence. Metabolic ratio was calculated and statistical analysis was performed. From the 52 participants (26 males; 30 regular caffein...
Source: Biopharmaceutics and Drug Disposition - January 1, 2016 Category: Drugs & Pharmacology Authors: Hazel Yiting Chia, Wai‐Ping Yau, Han Kiat Ho Tags: Original Paper Source Type: research

Effect of dietary fibers on losartan uptake and transport in Caco‐2 cells
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - December 1, 2015 Category: Drugs & Pharmacology Authors: Ayano Iwazaki, Naho Takahashi, Reiko Miyake, Yuka Hiroshima, Mariko Abe, Airi Yasui, Kimie Imai Tags: Original Paper Source Type: research

Identification of putative substrates for cynomolgus monkey cytochrome P450 2C8 by substrate depletion assays with 22 human P450 substrates and inhibitors
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - November 18, 2015 Category: Drugs & Pharmacology Authors: Shinya Hosaka, Norie Murayama, Masahiro Satsukawa, Shotaro Uehara, Makiko Shimizu, Kazuhide Iwasaki, Shunsuke Iwano, Yasuhiro Uno, Hiroshi Yamazaki Tags: Short Communication Source Type: research

Alteration of the intravenous and oral pharmacokinetics of valsartan via the concurrent use of gemfibrozil in rats
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - November 1, 2015 Category: Drugs & Pharmacology Authors: Seung Jun Yang, Bong Jin Kim, Lingxuan Mo, Hyo‐Kyung Han Tags: Original Paper Source Type: research

In vitro and in vivo characterization of CYP inhibition by 1‐aminobenzotriazole in rats
Abstract 1‐Aminobenzotriazole (ABT) is a non‐isoform specific, time‐dependent inhibitor of cytochrome P450 (CYP) enzymes used extensively in preclinical studies to determine the relative contribution of oxidative metabolism. Although ABT has been widely used, the extent and duration of its inhibitory effect is not well understood. The purpose of this study is to characterize ABT inhibition of CYP in rats at both the hepatic and intestinal levels. In vivo studies using midazolam (p.o. and i.v.), as a probe for CYP activity, demonstrated that CYP inhibition was not complete even at the highest dose (300 mg/kg). Additio...
Source: Biopharmaceutics and Drug Disposition - November 1, 2015 Category: Drugs & Pharmacology Authors: Karen E. Parrish, Jialin Mao, Jacob Chen, Allan Jaochico, Justin Ly, Quynh Ho, Sophie Mukadam, Matthew Wright Tags: Original Paper Source Type: research

Possible interaction of quinolone antibiotics with peptide transporter 1 in oral absorption of peptide‐mimetic drugs
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - November 1, 2015 Category: Drugs & Pharmacology Authors: Hiroshi Arakawa, Hiroki Kamioka, Masahiko Kanagawa, Yasuko Hatano, Yoko Idota, Kentaro Yano, Kaori Morimoto, Takuo Ogihara Tags: Original Paper Source Type: research

Incorporation of FcRn‐mediated disposition model to describe the population pharmacokinetics of therapeutics monoclonal IgG antibody in clinical patients
CONCLUSIONThis first reported semi‐mechanistic model may serve as important model framework for developing future population PK model of TMAbs in clinical patients. This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - November 1, 2015 Category: Drugs & Pharmacology Authors: Chee M. Ng Tags: Special Issue Article Source Type: research

A physiologically based pharmacokinetic model to predict the pharmacokinetics of highly protein‐bound drugs and impact of errors in plasma protein binding
This study uses a generic physiologically based pharmacokinetic (PBPK) model to predict human plasma concentration‐time profiles for 22 highly protein‐bound drugs. Tissue distribution was estimated from in vitro drug lipophilicity data, plasma protein binding, and blood:plasma ratio. Clearance was predicted with a well‐stirred liver model. Underestimated hepatic clearance for acidic and neutral compounds was corrected by an empirical scaling factor. Predicted values (pharmacokinetic parameters, plasma concentration‐time profile) were compared with observed data to evaluate model accuracy. Of the 22 drugs, less than...
Source: Biopharmaceutics and Drug Disposition - October 1, 2015 Category: Drugs & Pharmacology Authors: Min Ye, Swati Nagar, Ken Korzekwa Tags: Original Paper Source Type: research

Metabolic profiling of a novel antithrombotic compounds, S002‐333 and enantiomers: metabolic stability, species comparison and in‐vitro in‐vivo extrapolation
ConclusionIn‐vitro CLint values for S002‐333, S004‐1032 and S007‐1558 were 0.027 ± 0.005, 0.025 ± 0.004 and 0.036 ± 0.005 mL/min/mg respectively in PHLM, indicating S007‐1558, the most metabolically unstable among the three. LM of other species showed similar results. Common surrogate species to humans for S002‐333 and enantiomers was predicted as rabbit where extrapolated hepatic clearance (CLH) did not show significant difference with in‐vivo CLH values. However, none of the species closely mimic to humans with respect to proportion of major metabolites (M‐1 through M‐4) formed in‐vit...
Source: Biopharmaceutics and Drug Disposition - October 1, 2015 Category: Drugs & Pharmacology Authors: Amrita Saxena, Guru R. Valicherla, Girish K. Jain, Rabi S. Bhatta, Anil K. Saxena, Jiaur R. Gayen Tags: Original Paper Source Type: research

Murine Cyp3a knockout chimeric mice with humanized liver: prediction of the metabolic profile of nefazodone in humans
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - September 9, 2015 Category: Drugs & Pharmacology Authors: Naoyuki Nakada, Akio Kawamura, Hidetaka Kamimura, Koya Sato, Yasuhiro Kazuki, Masakazu Kakuni, Masato Ohbuchi, Kota Kato, Chise Tateno, Mitsuo Oshimura, Takashi Usui Tags: Original Paper Source Type: research

Physiologically‐based pharmacokinetic models of small molecules and therapeutic antibodies: mini‐review on fundamental concepts and applications
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - September 1, 2015 Category: Drugs & Pharmacology Authors: Gregory Z. Ferl, Frank‐Peter Theil, Harvey Wong Tags: Special Issue Article Source Type: research

Role of ABCB1, ABCG2, ABCC2 and ABCC5 transporters in placental passage of zidovudine
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - September 1, 2015 Category: Drugs & Pharmacology Authors: Zuzana Neumanova, Lukas Cerveny, Martina Ceckova, Frantisek Staud Tags: Original Paper Source Type: research

A physiologically based pharmacokinetic modeling approach to predict drug‐drug interactions between domperidone and inhibitors of CYP3A4
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - September 1, 2015 Category: Drugs & Pharmacology Authors: Ian Templeton, Paulien Ravenstijn, Carlo Sensenhauser, Jan Snoeys Tags: Original Paper Source Type: research

Similar substrate specificity of cynomolgus monkey cytochrome P450 2C19 to reported human P450 2C counterpart enzymes by evaluation of 89 drug clearances
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - September 1, 2015 Category: Drugs & Pharmacology Authors: Shinya Hosaka, Norie Murayama, Masahiro Satsukawa, Shotaro Uehara, Makiko Shimizu, Kazuhide Iwasaki, Shunsuke Iwano, Yasuhiro Uno, Hiroshi Yamazaki Tags: Original Paper Source Type: research

Point mutation of cytochrome P450 2A6 (a polymorphic variant CYP2A6.25) confers new substrate specificity towards flavonoids
Abstract CYP2A6 is a major hepatic member of the cytochrome P450 family in humans. Much variation in CYP2A6 levels and activity can be attributed to genetic polymorphisms of this gene. CYP2A6*25 comprises an amino acid substitution, F118L. To clarify the effect of the leucine substitution at position 118 in CYP2A6.25, this variant, wild type CYP2A6 and three additional variants consisting of artificial mutations at the substrate binding site (position 481) suggested by earlier reports using random mutagenesis studies [CYP2A6.1, CYP2A6.25, CYP2A6.1(F118A), CYP2A6.1(A481G) and CYP2A6.25(A481G)], were co‐expressed with NADP...
Source: Biopharmaceutics and Drug Disposition - August 31, 2015 Category: Drugs & Pharmacology Authors: Tomohide Uno, Chika Ogura, Chiho Izumi, Masahiko Nakamura, Takeshi Yanase, Hiroshi Yamazaki, Hitoshi Ashida, Kengo Kanamaru, Hiroshi Yamagata, Hiromasa Imaishi Tags: Original Paper Source Type: research