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药物吸收的体内方法——比较生理学、模型选择、与体外方法的相关性(体外-体内相关性)以及在制剂/原料药/辅料特性表征中的应用,包括食物影响。

In vivo methods for drug absorption - comparative physiologies, model selection, correlations with in vitro methods (IVIVC), and applications for formulation/API/excipient characterization including food effects.

作者信息

Sjögren Erik, Abrahamsson Bertil, Augustijns Patrick, Becker Dieter, Bolger Michael B, Brewster Marcus, Brouwers Joachim, Flanagan Talia, Harwood Matthew, Heinen Christian, Holm René, Juretschke Hans-Paul, Kubbinga Marlies, Lindahl Anders, Lukacova Viera, Münster Uwe, Neuhoff Sibylle, Nguyen Mai Anh, Peer Achiel van, Reppas Christos, Hodjegan Amin Rostami, Tannergren Christer, Weitschies Werner, Wilson Clive, Zane Patricia, Lennernäs Hans, Langguth Peter

机构信息

Department of Pharmacy, Uppsala University, Uppsala, Sweden.

AstraZeneca R&D, Mölndal, Sweden.

出版信息

Eur J Pharm Sci. 2014 Jun 16;57:99-151. doi: 10.1016/j.ejps.2014.02.010. Epub 2014 Mar 15.

DOI:10.1016/j.ejps.2014.02.010
PMID:24637348
Abstract

This review summarizes the current knowledge on anatomy and physiology of the human gastrointestinal tract in comparison with that of common laboratory animals (dog, pig, rat and mouse) with emphasis on in vivo methods for testing and prediction of oral dosage form performance. A wide range of factors and methods are considered in addition, such as imaging methods, perfusion models, models for predicting segmental/regional absorption, in vitro in vivo correlations as well as models to investigate the effects of excipients and the role of food on drug absorption. One goal of the authors was to clearly identify the gaps in today's knowledge in order to stimulate further work on refining the existing in vivo models and demonstrate their usefulness in drug formulation and product performance testing.

摘要

本综述总结了人类胃肠道的解剖学和生理学方面的现有知识,并与常见实验动物(狗、猪、大鼠和小鼠)进行了比较,重点介绍了用于测试和预测口服剂型性能的体内方法。此外,还考虑了广泛的因素和方法,如成像方法、灌注模型、预测节段性/区域性吸收的模型、体外-体内相关性以及研究辅料作用和食物对药物吸收影响的模型。作者的一个目标是明确识别当今知识中的差距,以促进进一步完善现有体内模型的工作,并证明其在药物制剂和产品性能测试中的实用性。

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