Institute of Pharmacy, Biopharmacy and Pharmaceutical Technology, Ernst Moritz Arndt University, 17 Friedrich Ludwig Jahn Street, Greifswald 17489, Germany.
AAPS J. 2010 Sep;12(3):397-406. doi: 10.1208/s12248-010-9203-3. Epub 2010 May 11.
Simulation of gastrointestinal conditions is essential to adequately predict the in vivo behavior of drug formulations. To reduce the size and number of human studies required to identify a drug product with appropriate performance in both the fed and fasted states, it is advantageous to be able to pre-screen formulations in vitro. The choice of appropriate media for such in vitro tests is crucial to their ability to correctly forecast the food effect in pharmacokinetic studies. The present paper gives an overview of the development and composition of biorelevant dissolution media that can be used for the in vitro simulation of different dosing conditions (fasted and fed states). In addition, the application of these media to predicting food effects is described in several case examples.
模拟胃肠道条件对于充分预测药物制剂的体内行为至关重要。为了减少在确定具有良好进食和禁食状态下性能的药物产品所需的人体研究的数量和规模,能够在体外预先筛选制剂是有利的。选择适当的介质进行此类体外测试对于其正确预测药代动力学研究中的食物效应至关重要。本文概述了可用于模拟不同给药条件(禁食和进食状态)的生物相关溶解介质的开发和组成。此外,还描述了这些介质在预测食物效应中的应用的几个实例。