天然产物研究与开发 ›› 2015, Vol. 27 ›› Issue (10): 1836-1841.doi: 10.16333/j.1001-6880.2015.10.027

• 综述 • 上一篇    

人工胃肠液模型在药物稳定性研究中的应用现状

黄财顺1,李宝才1,向诚1,2*   

  1. 1 昆明理工大学生命科学与技术学院,昆明 650500;2 北京大学天然药物及仿生药物国家重点实验室,北京 100191
  • 出版日期:2015-10-30 发布日期:2015-10-30

A Review on Artificial Gastrointestinal Fluid Model Applied in Drug-stability Evaluation

HUANG Cai-shun1, LI Bao-cai1, XIANG Cheng1,2*   

  1. 1 Faculty of Life Science and Technology,Kunming University of Science and Technology,Kunming 650500,China; 2 State Key Laboratory of Natural and Biomimetic Drugs, Peking University,Beijing, 100191, China
  • Online:2015-10-30 Published:2015-10-30

摘要: 口服药物可能受胃肠液的消化作用而降解失活,所以进行胃肠道的稳定性研究具有一定的价值。人工胃肠液模型具有容易操作、重现性好的优点,是目前应用较广泛的研究药物胃肠道稳定性的体外模型。本文总结了目前采用该模型进行药物稳定性研究的不同实验设计方法、在新药研究中的应用和存在的不足,并提出包括时间、pH值、酶浓度和搅拌速度的四因素析因设计的实验方法,还认为可以将该模型应用于中药和天然产物的有效成分筛选,以期为更好地应用该模型提供参考。

关键词: 人工胃肠液, 药物稳定性, 析因设计

Abstract: Oral administration may lead to drugs inactivate since gastric fluid digestion,hence it is valuable to study gastrointestinal stability of oral-administrated drugs.Artificial gastrointestinal fluid model is widely used in this study in vitro with the advantages of easy operation and repeatability.This paper summarized the different experimental designs of the model,its application in drug discovery and the problems.At last,a developed method considering time,pH value,enzyme concentration and the speed of stirring was proposed in order to provide a reference for using the artificial gastrointestinal fluid models in future.

Key words: artificial gastrointestinal fluid model, drug stability, factorial design

中图分类号: 

R917