白益母草总生物碱聚乳酸-羟基乙酸共聚物微球的制备

Preparation of Poly(lactide-co-glycolide)Microspheres Containing Total Alkaloids of Panzeria alaschanica

目的:优化蒙药白益母草总生物碱的聚乳酸-羟基乙酸共聚物(PLGA)微球的处方工艺,制备微球并对其进行质量考察。方法:采用复乳-液中干燥法制备白益母草总生物碱PLGA微球,以处方中PLGA质量浓度、聚乙烯醇(PVA)浓度及内水相/油相体积比为因素,以微球的载药量、包封率、收率的综合评分为指标,采用L9(34)正交试验优化制备微球的处方工艺,并考察微球形态、粒径及体外释药情况。结果:最优工艺为PLGA 200 mg/ml、PVA 2%、内水相/油相的体积比为1∶5;验证试验中平均包封率为(83.2±2.4)%,平均载药量为(4.16±0.17)%,平均收率为(86.7±3.6)%,综合评分结果为(95.7±4.4)%,RSD均小于5.0%(n=3);制备的微球形态圆整,表面光滑,粒径分布均匀,平均粒径为(22.3±2.4)μm;微球24 h体外累积释放度为(82.3±3.5)%,符合一级释放模型(r=0.972 4)。结论:优选工艺稳定;制备的微球具有良好的缓释性能,质量符合要求。

OBJECTIVE：To optimize the formulation and technology of poly（lactide-co-glycolide）（PLGA）microspheres containing total alkaloids of Panzeria alaschanica,and to prepare microspheres and conduct quality investigation. METHODS：PLGA microspheres containing total alkaloids of P. alaschanica（PTPM） was prepared by double emulsion-solvent evaporation method.The formulation of microspheres was optimized by L9（34）orthogonal design using mass concentration of PLGA,PVA concentration,ratio of water phase to oil phase as factor,drug-loading amount,encapsulation efficiency,yield as index. The morphology,particle size and drug release of microspheres were all investigated. RESULTS：The optimal formulation was as follows as the mass concentration of PLGA 200 mg/ml,the concentration of PVA 2%,and the water phase-oil phase ratio 1 ∶ 5. In validation test,average encapsulation efficiency was（83.2±2.4）%,average drug-loading amount（4.16±0.17）%,average yield（86.7±3.6）%,and comprehensive score（95.7 ± 4.4）%;all RSDs were lower than 5.0%（n=3）. Prepared microspheres were spherical with smooth surface and uniform particle size. The average particle size was（22.3±2.4）μm and accumulative release rate of 24 h was（82.3±3.5）%,which conformed to first-order release model（r=0.972 4）. CONCLUSIONS：Optimized technology is stable. Prepared microspheres show good sustained-release property,and fit to quality requirements.