The Role of Transporters in the Pharmacokinetics of Orally Administered Drugs

被引：318

作者：

Shugarts, Sarah ^{[1
]}

Benet, Leslie Z. ^{[1
]}

机构：

[1] Univ Calif San Francisco, Dept Biopharmaceut Sci, San Francisco, CA 94143 USA

来源：

PHARMACEUTICAL RESEARCH | 2009年 / 26卷 / 09期

关键词：

BDDCS; drug transporters; hepatic; intestinal; transporter/enzyme interplay; PREGNANE-X-RECEPTOR; CONSTITUTIVE ANDROSTANE RECEPTOR; INTESTINAL P-GLYCOPROTEIN; CANCER RESISTANCE PROTEIN; ORGANIC CATION TRANSPORTERS; ATP-BINDING CASSETTE; CONCENTRATIVE NUCLEOSIDE TRANSPORTER; MEMBRANE MONOAMINE TRANSPORTER; BLOOD-BRAIN-BARRIER; OATP-C SLC21A6;

D O I：

10.1007/s11095-009-9924-0

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Drug transporters are recognized as key players in the processes of drug absorption, distribution, metabolism, and elimination. The localization of uptake and efflux transporters in organs responsible for drug biotransformation and excretion gives transporter proteins a unique gatekeeper function in controlling drug access to metabolizing enzymes and excretory pathways. This review seeks to discuss the influence intestinal and hepatic drug transporters have on pharmacokinetic parameters, including bioavailability, exposure, clearance, volume of distribution, and half-life, for orally dosed drugs. This review also describes in detail the Biopharmaceutics Drug Disposition Classification System (BDDCS) and explains how many of the effects drug transporters exert on oral drug pharmacokinetic parameters can be predicted by this classification scheme.

引用

页码：2039 / 2054

页数：16

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