Research advances in models of hepatic and intestinal first-pass drug metabolism

Abstract

Abstract: Low oral bioavailability of a drug could be attributed to poor absorption and/or extensive first-pass metabolism.The liver and small intestine are the two most important organs for first-pass metabolism. In this review, the important drug-metabolizing enzymes located in the human liver and small intestine are introduced and the effects of different physiological structures of the two organs on overall first-pass metabolism are presented. Moreover, the research advances of the methods used to estimate hepatic and intestinal first-pass metabolism, such as in vitro, in situ, in vivo, in vitro-in vivo combined, knockout and transgenic models, are also summarized.

Key words: First-pass metabolism, Drug-metabolizing enzyme, Liver, Intestine, Bioavailability

CLC Number:

R969.1

ZHU Jing, GUO Jian-jun, LIN Jun-hui, BU Hai-zhi, CHEN Xi-jing. Research advances in models of hepatic and intestinal first-pass drug metabolism[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2012, 17(8): 944-949.

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