平衡溶解度实验基本程序和技术要求

Basic Procedure and Technical Requirements of Equilibrium Solubility Experiments

目的介绍平衡溶解度试验的基本程序和技术要求,为科研人员对平衡溶解度试验方案的设计和实施提供参考。方法从溶解度的概念及影响因素、试验的原理和测定方法、世界卫生组织(WHO)平衡溶解度项目等方面进行阐述分析。结果溶解度受缓冲液组成、温度、振荡时间、沉降时间、相分离方式等因素的影响。结论确定药物的BCS分类首先要测定药物在生理pH条件下的平衡溶解度,平衡溶解度的测定没有公认的标准方法,通过对WHO推荐的平衡溶解度试验程序的详细阐述,帮助我国广大医药工作者更好的实施平衡溶解度试验,对规范其在BCS分类和生物等效性豁免中的应用具有一定指导和借鉴意义。

OBJECTIVE To introduce the basic procedure and technical requirements of equilibrium solubility experiments and provide reference for design and conduct of equilibrium solubility experiments scheme.METHODS The concept and influence factors of solubility,principle and determination method of solubility experiments,equilibrium solubility project of world health organization were analyzed.RESULTS The influence factors of equilibrium solubility include composition of buffers, temperature,time of oscillation,time of sedimentation,techniques for separation of solid and liquid phases etc.CONCLUSION To ascertain the BCS classification of drugs,the first step is to determine the equilibrium solubility of drugs under physiological pH conditions.To date,there is no accepted standard method for the determination of equilibrium solubility.This paper introduces the basic procedure and technical requirements of equilibrium solubility experiments recommended by WHO,which would provide instructive and practical assists to conduct of equilibrium solubility experiments and standardize its application in BCS classification and biowaiver.