Physiologically based pharmacokinetic models of small molecules and therapeutic antibodies: a mini‐review on fundamental concepts and applications
Abstract The mechanisms of absorption, distribution, metabolism and elimination of small and large molecule therapeutics differ significantly from one another and can be explored within the framework of a physiologically based pharmacokinetic (PBPK) model. This paper briefly reviews fundamental approaches to PBPK modeling, in which drug kinetics within tissues and organs are explicitly represented using physiologically meaningful parameters. The differences in PBPK models applied to small/large molecule drugs are highlighted, thus elucidating differences in absorption, distribution and elimination properties between these ...
Source: Biopharmaceutics and Drug Disposition - March 29, 2016 Category: Drugs & Pharmacology Authors: Gregory Z. Ferl, Frank‐Peter Theil, Harvey Wong Tags: Invited Review Source Type: research

Pharmacokinetic considerations of antibody therapeutics
(Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - March 29, 2016 Category: Drugs & Pharmacology Authors: Harvey Wong, Matthew R. Wright Tags: Editorial Commentary Source Type: research

Issue Information ‐ JIP
No abstract is available for this article. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - March 29, 2016 Category: Drugs & Pharmacology Tags: Issue Information ‐ JIP Source Type: research

Issue Information ‐ TOC
No abstract is available for this article. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - March 29, 2016 Category: Drugs & Pharmacology Tags: Issue Information ‐ TOC Source Type: research

Analysis of gene expression for microminipig liver transcriptomes using parallel long‐read technology and short‐read sequencing
ABSTRACT Microminipig is one of the smallest minipigs that has emerged as a possible experimental animal model, because they share many anatomical and/or physiological similarities with humans, including the coronary artery distribution in heart, the digestive physiology, the kidney size and its structure, and so on. However, information on gene expression profiles, including those of drug‐metabolizing phase I and II enzymes, in microminipig is limited. Therefore, the aim of the present study was to identify transcripts in microminipig livers and determine gene expression profiles. De novo assembly and expression analyse...
Source: Biopharmaceutics and Drug Disposition - March 1, 2016 Category: Drugs & Pharmacology Authors: Chizuka Sakai, Shunsuke Iwano, Makiko Shimizu, Jun Onodera, Uchida Masashi, Eri Sakurada, Yuri Yamazaki, Yoshiji Asaoka, Naoko Imura, Yasuhiro Uno, Norie Murayama, Ryoji Hayashi, Hiroshi Yamazaki, Yohei Miyamoto Tags: Original Paper Source Type: research

Expression of UGT1A Subfamily in Rat Brain
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - February 29, 2016 Category: Drugs & Pharmacology Authors: Yukiko Sakakibara, Miki Katoh, Kuniyuki Imai, Yuya Kondo, Yuki Asai, Shin‐ichi Ikushiro, Masayuki Nadai Tags: Short Communication Source Type: research

Biliary excretion of pravastatin and taurocholate in rats with bile salt export pump (Bsep) impairment
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - February 29, 2016 Category: Drugs & Pharmacology Authors: Yaofeng Cheng, Chris Freeden, Yueping Zhang, Pamela Abraham, Hong Shen, Debra Wescott, W. Griffith Humphreys, Jinping Gan, Yurong Lai Tags: Original Paper Source Type: research

Long term human primary hepatocyte cultures in a microfluidic liver biochip show maintenance of mRNA levels and higher drugs metabolisms when compared to Petri cultures
Abstract We have cultivated, for 13 days, human primary hepatocytes in a microfluidic bioreactor and in Petri. mRNA kinetics have shown in biochips an increase of the levels of CYP2B6, CYP2C19, CYP2C8, CYP3A4, CYP1A2, CYP2D6, HNF4a, SULT1A1, UGT1A1 mRNA related genes when compared to post extraction levels. In addition, comparison with Petri have shown a higher levels of CYP2B6, CYP2C19, CYP2C8, CYP3A4, CYP1A2, CYP2D6 related genes at the end of cultures. Functional assays illustrated a higher urea and albumin production over the period of culture in biochips. Bioreactor drug metabolism (midazolam and phenacetin) was not s...
Source: Biopharmaceutics and Drug Disposition - February 29, 2016 Category: Drugs & Pharmacology Authors: Rachid Jellali, Thibault Bricks, Sebastien Jacques, Marie Jose Fleury, Patrick Paullier, Franck Merlier, Eric Leclerc Tags: Original Paper Source Type: research

High body clearance and low oral bioavailability of alantolactone, isolated from Inula helenium, in rats: extensive hepatic metabolism and low stability in gastrointestinal fluids
ABSTRACT Alantolactone (ALA) is a major bioactive sesquiterpene lactone present in the roots of Inula helenium L. (Asteraceae) which has been widely used in traditional medicine against various diseases such as asthma, cancer, and tuberculosis. Pharmacologic activities of ALA have been well characterized, yet information on the physicochemical and pharmacokinetic properties of ALA and their mechanistic elucidation are still limited. Thus, this study aims to investigate the oral absorption and disposition of ALA and their relevant mechanisms. Log P values of ALA ranged from 1.52 to 1.84, and ALA was unstable in biological s...
Source: Biopharmaceutics and Drug Disposition - February 10, 2016 Category: Drugs & Pharmacology Authors: Jae‐Young Lee, Sang‐Bum Kim, Jaemoo Chun, Kwang Ho Song, Yeong Shik Kim, Suk‐Jae Chung, Hyun‐Jong Cho, In‐Soo Yoon, Dae‐Duk Kim Tags: Original Paper Source Type: research

A physiologically based pharmacokinetic modeling approach to predict drug–drug interactions between domperidone and inhibitors of CYP3A4
Abstract Domperidone is a dopamine receptor antagonist and a substrate of CYP3A4, hence there is a potential for CYP3A inhibition‐based drug–drug interactions (DDI). A physiologically based pharmacokinetic model was developed to describe DDIs between domperidone and three different inhibitors of CYP3A4. Simcyp V13.1 was used to simulate human domperidone pharmacokinetics and DDIs. Inputs included domperidone chemical and physical properties (LogP, pKa, etc.), in vitro human liver microsomal data and pharmacokinetic parameters from single‐dose intravenous clinical studies in healthy participants. The simulated mean ma...
Source: Biopharmaceutics and Drug Disposition - January 26, 2016 Category: Drugs & Pharmacology Authors: Ian Templeton, Paulien Ravenstijn, Carlo Sensenhauser, Jan Snoeys Tags: Original Paper Source Type: research

Issue information ‐ JIP
No abstract is available for this article. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - January 26, 2016 Category: Drugs & Pharmacology Tags: Issue information ‐ JIP Source Type: research

Issue information ‐ TOC
No abstract is available for this article. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - January 26, 2016 Category: Drugs & Pharmacology Tags: Issue information ‐ TOC Source Type: research

Tissue distribution of teneligliptin in rats and comparisons with data reported for other dipeptidyl peptidase‐4 inhibitors
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - January 8, 2016 Category: Drugs & Pharmacology Authors: Yoshinobu Nakamaru, Fumihiko Akahoshi, Hiroaki Iijima, Noriko Hisanaga, Toshiyuki Kume Tags: Original Paper Source Type: research

Pharmacokinetics and Pharmacodynamics of Propofol and Fentanyl in Patients Undergoing Abdominal Aortic Surgery – a Study of Pharmacodynamic Drug‐Drug Interactions
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - January 1, 2016 Category: Drugs & Pharmacology Authors: Paweł Wiczling, Krzysztof Bieda, Krzysztof Przybyłowski, Roma Hartmann‐Sobczyńska, Agnieszka Borsuk, Jan Matysiak, Zenon J Kokot, Paweł Sobczyński, Edmund Grześkowiak, Agnieszka Bienert Tags: Original Paper Source Type: research

In silico evaluation of warfarin‐bucolome therapy
In conclusion, the concomitant administration of bucolome might not be useful for reducing the inter‐patient variation of (S)‐warfarin pharmacokinetics. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - January 1, 2016 Category: Drugs & Pharmacology Authors: Hisakazu Ohtani, Ryoko Hakoda, Ayuko Imaoka, Takeshi Akiyoshi Tags: Original Paper Source Type: research