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Issue Information ‐ JIP
No abstract is available for this article. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - May 22, 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 - May 22, 2016 Category: Drugs & Pharmacology Tags: Issue Information ‐ TOC Source Type: research

Involvement of a Proton ‐Coupled Organic Cation Antiporter in the Blood‐Brain Barrier Transport of Amantadine
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - May 3, 2016 Category: Drugs & Pharmacology Authors: Toyofumi Suzuki, Takahiko Aoyama, Naoto Suzuki, Masaru Kobayashi, Toshiro Fukami, Yoshiaki Matsumoto, Kazuo Tomono Tags: Original Paper Source Type: research

Factor VIII associated with lipidic nanoparticles retains efficacy in the presence of anti‐Factor VIII antibodies in Hemophilia A mice
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - April 30, 2016 Category: Drugs & Pharmacology Authors: Krithika A. Shetty, Matthew P. Kosloski, Donald E. Mager, Sathy V. Balu‐Iyer Tags: Original Paper Source Type: research

TKI Combination Therapy: Strategy to Enhance Dasatinib Uptake through Inhibiting Pgp‐ And BCRP‐ Mediated Efflux
Abstract The overexpression of efflux transporters, especially P‐glycoprotein (Pgp, MDR1, ABCB1) and Breast Cancer Resistance Protein (BCRP, ABCG2), represents an important mechanism of multidrug resistance (MDR). Tyrosine kinase inhibitors (TKIs), a novel group of target‐specific anticancer drugs, have recently been found to interact with Pgp and BCRP and serve as both substrates and inhibitors. Considering their dual role, we anticipate that combination TKI therapy may represent a promising strategy to reverse efflux transporter mediated TKI resistance. Presently, investigations on these interactions are very limited...
Source: Biopharmaceutics and Drug Disposition - April 30, 2016 Category: Drugs & Pharmacology Authors: Ronilda D'Cunha, Sohyun Bae, Daryl J Murry, Guohua An Tags: Original Paper Source Type: research

In Vivo Use of the CYP Inhibitor 1‐Aminobenzotriazole to Increase Long‐term Exposure in Mice
In this study, we demonstrated a suitable dosing vehicle of ABT for continuous administration and increased exposure of antipyrine, which is a nonspecific probe of CYP, using ABT for a long period in mice. The dosing vehicle of ABT was the 0.5% (w/v) hydroxypropyl methylcellulose and 0.5% (v/v) Tween 80 in N,N‐Dimethylacetamide/20% hydroxypropyl‐β‐cyclodextrin aqueous solution (2:8, v/v) based on the duration of apparent solubility. After implantation of an ALZET osmotic pump with ABT, the plasma concentrations of ABT were maintained at more than 4.1 µg/mL over 336 h. Compared to the vehicle group, CLtot of ant...
Source: Biopharmaceutics and Drug Disposition - April 30, 2016 Category: Drugs & Pharmacology Authors: Ayahisa Watanabe, Kei Mayumi, Kyohei Nishimura, Hiromi Osaki Tags: Short Communication Source Type: research

Simultaneous evaluation of substrate‐dependent CYP3A inhibition using a CYP3A probe substrates cocktail
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - April 30, 2016 Category: Drugs & Pharmacology Authors: Eunyoung Lee, Jong Cheol Shon, Kwang‐Hyeon Liu Tags: Short Communication Source Type: research

Assessment of Penetrant and Vehicle Mixture Properties on Transdermal Permeability using a Mixed Effect Pharmacokinetic Model of Ex Vivo Porcine Skin
Abstract The accurate prediction of the rate and extent of transdermal absorption from topical exposure to chemical mixtures would be beneficial in risk assessment and drug delivery applications. The isolated perfused porcine skin flap (IPPSF) has been used as an ex vivo model for assessing transdermal absorption from topical exposures. A mixed effect, pharmacokinetic tissue model was used to model finite dose, transdermal, absorption data from IPPSF experiments for 12 penetrants dosed in up to 10 different vehicles. The model was able to identify permeability constant, while accounting for between and within unit variabil...
Source: Biopharmaceutics and Drug Disposition - April 30, 2016 Category: Drugs & Pharmacology Authors: Jason T. Chittenden, Jim E. Riviere Tags: Original Paper Source Type: research

Effects of Poloxamer 407‐induced hyperlipidemi a on hepatic multidrug resistance protein 2 (Mrp2/Abcc2) and the pharmacokinetics of mycophenolic acid in rats
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - April 30, 2016 Category: Drugs & Pharmacology Authors: Mi Hye Kwon, Ji Na Yoon, Yu Jin Baek, Yu Chul Kim, Yong Yeon Cho, Hee Eun Kang 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 - April 23, 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 - April 23, 2016 Category: Drugs & Pharmacology Tags: Issue Information ‐ TOC Source Type: research

The pharmacokinetics of dronedarone in normolipidemic and hyperlipidemic rats
The objectives of the current study were to characterize the pharmacokinetic profile of dronedarone in the rat, and to examine the effect of hyperlipidemia on its pharmacokinetics. Single doses of dronedarone were administered to rats intravenously (4 mg/kg), orally (55 mg/kg) and intraperitoneally (65 mg/kg). To induce hyperlipidemia, some of the rats were administered intraperitoneal doses of poloxamer 407 before giving an oral dose of dronedarone. After intravenous doses of 4 mg/kg dronedarone, plasma clearance and volume of distribution at steady‐state were 25.1 ± 8.09 mL/min/kg and 10.8 ± 4.77 L/...
Source: Biopharmaceutics and Drug Disposition - March 31, 2016 Category: Drugs & Pharmacology Authors: Yousef A. Bin Jardan, Dion R. Brocks Tags: Original Paper Source Type: research

The Role of the Equilibrative Nucleoside Transporter 1 on Tissue and Fetal Distribution of Ribavirin in the Mouse
Abstract Ribavirin is used for the treatment of hepatitis C virus (HCV) infection. The equilibrative nucleoside transporter 1 (ENT1) expressed in hepatocytes transports ribavirin into the liver, the site of efficacy of the drug. However, it is still unclear whether ENT1 plays a dominant role in the hepatic distribution of the drug in vivo. In addition, due to fetal toxicity, administration of ribavirin to pregnant women with HCV infection is contraindicated. ENT1 might play a role in the fetal distribution and therefore the fetal toxicity of ribavirin. The aim of the present study was to investigate the in vivo contributio...
Source: Biopharmaceutics and Drug Disposition - March 31, 2016 Category: Drugs & Pharmacology Authors: Christopher J. Endres, Aaron M. Moss, Kazuya Ishida, Rajgopal Govindarajan, Jashvant D. Unadkat Tags: Original Paper Source Type: research

Involvement of a Proton‐Coupled Organic Cation Antiporter in the Blood‐Brain Barrier Transport of Amantadine
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - March 31, 2016 Category: Drugs & Pharmacology Authors: Toyofumi Suzuki, Takahiko Aoyama, Naoto Suzuki, Masaru Kobayashi, Toshiro Fukami, Yoshiaki Matsumoto, Kazuo Tomono Tags: Original Paper Source Type: research

A quantitative threshold for high/ low extent of urinary excretion of compounds in humans
In conclusion, 16.8% is a quantitative threshold value to distinguish between high and low UE and new molecular entities with cLogP and ACD labs cLogP values of ≤0.7 and ≥1.0 and ACD labs cLogD(pH=7.4) values of ≤0.0 and ≥0.5 could be identified as exhibiting high and low UE, respectively. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - March 31, 2016 Category: Drugs & Pharmacology Authors: Rutwij A. Dave, Marilyn E. Morris Tags: Original Paper Source Type: research