In vitro-in vivo extrapolation (IVIVE) for predicting human intestinal absorption and first-pass elimination of drugs: principles and applications

被引：32

作者：

Cho, Hyun-Jong ^{[1
]}

Kim, Ji-Eon ^{[2
,3
]}

Kim, Dae-Duk ^{[2
,3
]}

Yoon, In-Soo ^{[4
,5
]}

机构：

[1] Kangwon Natl Univ, Coll Pharm, Chunchon, South Korea

[2] Seoul Natl Univ, Coll Pharm, Seoul, South Korea

[3] Seoul Natl Univ, Pharmaceut Sci Res Inst, Seoul, South Korea

[4] Mokpo Natl Univ, Coll Pharm, Jeonnam 534729, South Korea

[5] Mokpo Natl Univ, Nat Med Res Inst, Jeonnam 534729, South Korea

来源：

DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY | 2014年 / 40卷 / 08期

基金：

新加坡国家研究基金会;

关键词：

First-pass elimination; intestinal absorption; in vitro-in vivo extrapolation (IVIVE); oral bioavailability; pharmacokinetics; ENHANCED ORAL BIOAVAILABILITY; GUT-WALL METABOLISM; HEPATIC ELIMINATION; PHARMACOKINETIC SIMULATION; PHYSICOCHEMICAL PROPERTIES; PERMEABILITY COEFFICIENTS; DEVELOPABILITY ASSESSMENT; PRECLINICAL DATA; ORGAN CLEARANCE; RAT-LIVER;

D O I：

10.3109/03639045.2013.831439

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Oral administration remains the preferred dosing method in clinical practice and drug development. Oral bioavailability (F) is a function of the fraction absorbed (F-abs), gastrointestinal or gut wall availability (F-G), and hepatic availability (F-H). Therefore, predicting intestinal absorption (F-abs) and first-pass elimination (F-G and F-H) from in vitro data may facilitate the selection of more orally bioavailable drug candidates in earlier stages of drug discovery and development. This review provides an overview of the determinants of intestinal absorption and first-pass elimination of drugs and focuses on the principles and applications of conventional in vitro-in vivo extrapolation (IVIVE) methods to predict F-abs, F-G, and F-H in humans.

引用

页码：989 / 998

页数：10

共 91 条

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