聚酯类微球注射剂体外加速释放试验方法的研究进展

Research of method for accelerated in vitro drug release from poly-ester microsphere injection

聚酯类微球注射剂是长效注射给药系统的主要剂型,目前已有一些产品上市,微球的研发在生命科学和相关领域已引起高度重视。建立与实时释放相关的体外加速释放方法是长效微球剂研发和产品质量控制的一项重要课题。文中着重介绍了2种实时-加速释放相关性的评价方法,综述了以聚酯为骨架材料的长效微球注射剂体外释放加速试验方法的研究进展,概括了升高介质温度、降低介质pH、添加有机溶剂和放射性辐射等因素对加速微球释药和聚合物降解的作用,为在体外采用加速释放方法开展微球研发、控制微球质量提供新思路与科学依据。

The biodegradable polyester microsphere was one of the most important carriers of long-acting injection. It had gained a lot of interests from life science and other fields. Some products had appeared on the market. It was very important to establish an accelerated in vitro release method highly correlated with ＂real time＂ test either for formulation design or for quality control of long-acting microsphere injection. In this article, two ways were introduced to evaluate the correlation between accelerated and ＂real time＂ tests, and some factors that might speed up the drug release and polymer degradation of polyester microspheres were reviewed. These factors included raising the media temperature, lowering the media pH, adding organic solvents to media and gamma irradiation.