微球制剂质量控制研究进展

Research progress in quality control of microspheres

与传统制剂相比,缓释微球制剂可以减少给药次数,提高患者顺应性,降低副作用,提高疗效,在临床上已突显优势,近年来已成为药物新剂型研发的热点。其质量控制研究对药物的研发、转化具有较大的促进作用,但是目前专门针对微球制剂的质量检测与评价的方法报道较少。本文概述了微球制剂的上市产品和主要生产工艺,并系统阐述了微球制剂的质控技术和质量参数表征方法,以及相关研究进展。重点介绍了微球制剂的形态、粒径及粒径分布,载药量和包封率以及体外释放度的检测技术与方法,为微球制剂的质量研究和质控方法提供参考。

Microsphere formulation has become a hot topic in pharmaceutical research and development in recent years. Compared to traditional dosage forms, microspheres are gaining popularity in clinical practice due to the advantages of lower administration frequency, better patient compliance, reduced side effects, and improved therapeutic effects as a result of consistent drug blood level. The quality control study will significantly promote the development and application of these drugs; however, few reports has focused on detection and evaluation methods of microsphere formulation currently. This review briefly introduced marketed microsphere drug products and related manufacturing technique. Moreover, quality characterization parameters and recent advances in quality control techniques were systematically summarized in this review. In particular, the introduction of approaches and tech- niques regarding detecting size and size distribution, drug loading and encapsulation efficiency, and in vitro release of microspheres were featured in this review. These will provide some strategies for quality research and control method of microsphere formulation.