微球与原位凝胶植入剂长效策略与控制突释的研究进展

Strategies of microspheres and in situ forming gel implants in long-acting and research progress in controlling burst release

长效注射剂因可长时间控制药物释放,减少给药次数而显著改善了用药顺应性,在药物制剂研究领域中占据重要地位。本文以注射微球、原位凝胶植入剂两种类型的长效注射剂上市产品为切入点,剖析了此类长效制剂处方及工艺中为实现长时间释药所采用的策略与技术。同时就此类制剂普遍存在的突释现象,综述了现阶段研究中控制突释的相关策略,为此类长效制剂的设计、研发与优化提供理论参考。

Long-acting injectables(LAIs)play an important role in the field of drug preparation research because they can control drug release for a long time and decrease dosing frequency.In this review,two types of LAIs,including injectable microspheres and in situ forming gel implants,were used as the breakthrough point to analyze the strategies and technologies used in the formulation and process to achieve long-acting drug release.At the same time,in view of the common burst release phenomenon,the relevant coping strategies in the current research were summarized,which provides some reference for the design,development and optimization of such long-acting preparations.