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Issue Information ‐ TOC
No abstract is available for this article. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - November 30, 2016 Category: Drugs & Pharmacology Tags: Issue Information ‐ TOC Source Type: research

Evaluation of species difference in peripheral lymphocyte reduction effect of CS ‐0777, a sphingosine 1‐phosphate receptor modulator, based on a pharmacokinetic/pharmacodynamic model analysis
Abstract Pharmacokinetic (PK) and pharmacodynamic (PD) modeling was conducted for the reduction of peripheral lymphocytes after oral administration of CS‐0777 to healthy rats, monkeys and experimental autoimmune encephalomyelitis (EAE) induced rats. The phosphorylated active metabolite of CS‐0777, M1, is a selective sphingosine 1‐phosphate receptor‐1 modulator. A linear one‐ and two‐compartment model with a reversible metabolism process characterized the time courses of CS‐0777 and M1 concentrations in rats and monkeys, respectively. The relationship between lymphocyte counts and M1 concentrations in blood wa...
Source: Biopharmaceutics and Drug Disposition - November 13, 2016 Category: Drugs & Pharmacology Authors: Shin ‐ichi Inaba, Maki Goto, Kaoru Tanaka‐takanaka, Hisako Tanaka, Wataru Tomisato, Hiroshi Yuita, Hiromi Doi‐Komuro, Ryotaku Inoue, Keiko Oshima, Takashi Kagari, Takaichi Shimozato, Takashi Izumi Tags: Original Paper Source Type: research

Efavirenz does not meaningfully affect the single dose pharmacokinetics of 1200  mg raltegravir
Abstract Raltegravir is a human immunodeficiency virus (HIV)‐1 integrase strand transfer inhibitor currently marketed at a dose of 400 mg twice daily (BID). Raltegravir for once daily regimen (QD) at a dose of 1200 mg (2 x 600 mg) is under development and offers a new treatment option for HIV‐1 infected treatment‐naive subjects. Since raltegravir is eliminated mainly by metabolism via an UDP‐glucuronosyltransferase (UGT) 1 A1‐mediated glucuronidation pathway, co‐administration of UGT1A1 inducers may alter plasma levels of raltegravir. Efavirenz, an UGT1A1 inducer, was used to assess the impact of altered UG...
Source: Biopharmaceutics and Drug Disposition - November 13, 2016 Category: Drugs & Pharmacology Authors: Rajesh Krishna, Lilly East, Patrick Larson, Tara Siringhaus, Lisa Herpok, Crystal Bethel ‐Brown, Helen Manthos, John Brejda, Michael Gartner Tags: Original Paper Source Type: research

Atazanavir increases the plasma concentrations of 1200 mg raltegravir dose
Abstract Raltegravir is a human immunodeficiency virus (HIV)‐1 integrase strand transfer inhibitor currently marketed at a dose of 400 mg twice‐daily (b.i.d.). Raltegravir 1200 mg once‐daily (q.d.) (investigational q.d. formulation of 2 × 600 mg tablets; q.d. RAL) was found to be generally well tolerated and non‐inferior to the marketed 400 mg b.i.d. dose at 48 weeks in a phase 3 trial. Since raltegravir is eliminated mainly by metabolism via a uridine diphosphate glucuronosyltransferase (UGT) 1A1‐mediated glucuronidation pathway, co‐administration of UGT1A1 inhibitors may increase the plasma levels of q.d. RA...
Source: Biopharmaceutics and Drug Disposition - November 3, 2016 Category: Drugs & Pharmacology Authors: Rajesh Krishna, Lilly East, Patrick Larson, Chandni Valiathan, Kathleen Deschamps, Julie Ann Luk, Crystal Bethel ‐Brown, Helen Manthos, John Brejda, Michael Gartner Tags: Original Paper Source Type: research

Selective Reduction in the Expression of UGTs and SULTs, a Novel Mechanism by which Piperine Enhances the Bioavailability of Curcumin in Rat
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - October 31, 2016 Category: Drugs & Pharmacology Authors: Xiaohui Zeng, Dake Cai, Qiaohuang Zeng, Zhao Chen, Guoping Zhong, Juncheng Zhuo, Haining Gan, Xuejun Huang, Ziming Zhao, Nan Yao, Dane Huang, Chengzhe Zhang, Dongmei Sun, Yuxing Chen 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 - October 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 - October 26, 2016 Category: Drugs & Pharmacology Tags: Issue Information ‐ TOC Source Type: research

Erratum
(Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - October 11, 2016 Category: Drugs & Pharmacology Tags: Erratum Source Type: research

Issue Information ‐ JIP
No abstract is available for this article. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - October 2, 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 - October 2, 2016 Category: Drugs & Pharmacology Tags: Issue Information ‐ TOC Source Type: research

Evaluation of species difference in peripheral lymphocyte reduction effect by CS ‐0777, a sphingosine 1‐phosphate receptor modulator, based on a pharmacokinetic/pharmacodynamic model analysis
Abstract The pharmacokinetic (PK) and pharmacodynamic (PD) modeling was conducted for the reduction of peripheral lymphocytes after oral administration of CS‐0777 to healthy rats, monkeys and experimental autoimmune encephalomyelitis (EAE) induced rats. M1, the phosphorylated active metabolite of CS‐0777, is a selective sphingosine 1‐phosphate receptor‐1 modulator. A linear one‐and two‐compartment model with reversible metabolism process characterized the time courses of CS‐0777 and M1 concentrations in rats and monkeys, respectively. The relationship between lymphocyte counts and M1 concentrations in blood w...
Source: Biopharmaceutics and Drug Disposition - September 30, 2016 Category: Drugs & Pharmacology Authors: Shin ‐ichi Inaba, Maki Goto, Kaoru Tanaka‐takanaka, Hisako Tanaka, Wataru Tomisato, Hiroshi Yuita, Hiromi Doi‐Komuro, Ryotaku Inoue, Keiko Oshima, Takashi Kagari, Takaichi Shimozato, Takashi Izumi Tags: Original Paper Source Type: research

P ‐gp Activity and Inhibition in the Different Regions of Human Intestine Ex Vivo
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - September 30, 2016 Category: Drugs & Pharmacology Authors: Ming Li, Inge A.M. Graaf, Marina H. Jager, Geny M. M. Groothuis Tags: Special Issue Article Source Type: research

Identification of Non ‐Reported Bupropion Metabolites in Human Plasma
Abstract Bupropion and its three active metabolites exhibit clinical efficacy in the treatment of major depression, seasonal depression, and smoking cessation. The pharmacokinetics of bupropion in humans is highly variable. It is unknown if there are any non‐reported metabolites formed in humans in addition to the three known active metabolites. In this paper, we report newly identified and non‐reported metabolites of bupropion in human plasma samples. Human subjects were dosed with a single oral dose of 75 mg of an immediate release bupropion HCl tablet. Plasma samples were collected and analyzed by LC‐MS/MS at 0,...
Source: Biopharmaceutics and Drug Disposition - September 30, 2016 Category: Drugs & Pharmacology Authors: Jamie N. Connarn, Ruijuan Luo, Jim Windak, Xinyuan Zhang, Andrew Babiskin, Marisa Kelly, Gloria Harrington, Vicki L. Ellingrod, Masoud Kamali, Melvin McInnis, Duxin Sun Tags: Original Paper Source Type: research

Efavirenz does not meaningfully affect the single dose pharmacokinetics of 1200  mg raltegravir
Abstract Raltegravir is a human immunodeficiency virus (HIV)‐1 integrase strand transfer inhibitor currently marketed at a dose of 400 mg twice daily (BID). Raltegravir for once daily regimen (QD) at a dose of 1200 mg (2 x 600 mg) is under development and offers a new treatment option for HIV‐1 infected treatment‐naive subjects. Since raltegravir is eliminated mainly by metabolism via an UDP‐glucuronosyltransferase (UGT) 1A1‐mediated glucuronidation pathway, co‐administration of UGT1A1 inducers may alter plasma levels of raltegravir. Efavirenz , an UGT1A1 inducer) was used to assess the impact of altered ...
Source: Biopharmaceutics and Drug Disposition - September 30, 2016 Category: Drugs & Pharmacology Authors: Rajesh Krishna, Lilly East, Patrick Larson, Tara Siringhaus, Lisa Herpok, Crystal Bethel ‐Brown, Helen Manthos, John Brejda, Michael Gartner Tags: Original Paper Source Type: research

Effect of hesperidin on the pharmacokinetics of CPT ‐11 and its active metabolite SN‐38 by regulating hepatic Mrp2 in rats
This study examined the effect of hesperidin on the pharmacokinetics of CPT‐11 and SN‐38 as well as the regulatory effect on the hepatic expression of Mrp2. Compared with the control group, the AUC5‐t was increased to 115% of CPT‐11 and 122% of SN‐38; the CL was decreased to 87% for CPT‐11; the tissue concentration was increased in the liver, kidney and colon; and the accumulated biliary excretion was significantly decreased to 77% for CPT‐11 and 76% for SN‐38 in hesperidin‐treated rats. Furthermore, the expression of Mrp2 in the liver was significantly decreased to 37% in the hesperidin‐treated rats co...
Source: Biopharmaceutics and Drug Disposition - September 14, 2016 Category: Drugs & Pharmacology Authors: Xingdong Wang, Zhi Rao, Hongyan Qin, Guoqiang Zhang, Yanrong Ma, Yongwen Jin, Miao Han, Axi Shi, Yanping Wang, Xinan Wu Tags: Original Paper Source Type: research