20(S)-原人参二醇聚乳酸-羟基乙酸缓释微球的制备

Preparation of 20(S)-protopanaxadiol Polylactic Acid-glycolic Acid Sustained Release Microspheres

目的:制备20(S)-原人参二醇聚乳酸-羟基乙酸微球。方法:以聚乙烯醇为乳化剂,乙酸乙酯和二氯甲烷混合液为油相,采用乳化溶剂挥发法制备20(S)-原人参二醇聚乳酸-羟基乙酸微球,在单因素试验基础上,以微球收率、包封率、载药量的综合评分为指标,通过正交试验设计优选处方工艺,并进行体外释放特性研究。结果:优选的处方工艺为O/W体积比1∶50,PVA质量分数0.5%,投药量20 mg。制备的微球外观圆整,平均粒径约1.16μm,收率35.58%,包封率41.76%,载药量19.61%。微球在前0.5 h内的释放量18.24%,至192 h时,累积释放量高达98.99%。结论:该优选处方和制备工艺稳定可行,制备的微球具有明显的缓释效果。

Objective： To prepare 20（S）-protopanaxadiol polylactic acid-glycolic acid（PLGA）microspheres. Method： 20（S）-protopanaxadiol PLGA microspheres were prepared by emulsion-solvent evaporation method, with polyvinyl alcohol（PVA）as emulsifier, mixture of ethyl acetate and methylene chloride as oil phase.Based on single factor test, with composite score of microspheres yield, encapsulation efficiency and drug-loading as index, formulation technology was optimized by orthogonal test, then to investigate its in vitro release characteristics. Result： Optimized formulation technology was as following：volume ratio of O/W 1：50, the mass fraction of PVA 0.5%, feeding dosage 20 mg.These prepared microspheres had round appearance with average particle size of about 1.16 μm, microspheres yield of 35.58%, encapsulation efficiency of 41.76%, drug loading of 19.61%.In vitro release of these microspheres within the first 0.5 h was 18.24%, and cumulative release was up to 98.99% in 192h. Conclusion： This optimized formulation and preparation technology was stable and feasible.These prepared microspheres had significant sustained release effect.