肠道药物转运体和其研究方法.pdf

·370 · 药学学报 Acta Pharmaceutica Sinica 2011, 46 (4): 370−376 肠道药物转运体及其研究方法 * 刘志浩, 刘克辛 (大连医科大学药学院临床药理教研室, 辽宁 大连 116044) 摘要: 口服药物在肠道中的吸收是决定药物生物利用度的重要因素。肠道中有许多药物膜转运蛋白介导药 物的吸收、分布、排泄及药物相互作用等。明确其转运机制有利于提高药物的安全性和有效性, 从而指导临床 合理用药。通过体内外方法预测药物经转运体在肠道中的转运情况。本文介绍了肠道内转运药物的主要膜转运 蛋白, 阐述了口服药物经肠道转运机制, 概括了研究肠道药物转运体的主要研究方法, 并对多种体内外转运体研 究方法的优缺点进行了比较。 关键词: 肠; 膜转运蛋白类; 药物吸收 中图分类号: R969.1 文献标识码: A 文章编号: 0513-4870 (2011) 04-0370-07 The transporters of intestinal tract and their study methods * LIU Zhi-hao, LIU Ke-xin (Department of Clinical Pharmacology, College of Pharmacy, Dalian Medical University, Dalian 116044, China) Abstract : The absorption of oral drug in the intestine is an important factor to determine the drug bioavailability. There are many intestinal transporters mediating drug absorption, distribution, excretion and drug-drug interaction. Understanding the transport mechanism can improve the effectiveness and safety of drug and guide clinical rational use of drugs. The in vivo and in vitro methods are used to predict the transport mechanism of drugs by intestinal transporters in the intestine. The purposes of this article are to introduce the main transporters in the intestinal tract, to explain the transport mechanism and to summarize the advantages and disadvantages of the research methods of them. Key words: intestine; membrane transport protein; drug absorption 20 世纪 80 年代以来, 随着分子生物学的发展, 提高