紫杉醇微球的处方工艺优化及其体外释放性研究

目的:优化紫杉醇聚1,3-双(对羧基苯氧基)丙烷-癸二酸](P(CPP∶SA))微球处方工艺并评价其体外释放行为。方法:采用单乳化法制备药物缓释微球,以正交试验研究制备时搅拌速度(A)、处方中P(CPP∶SA)浓度(B)和乳化剂聚乙烯醇(PVA)的浓度(C)对微球包封率的影响;观察优化条件后制备的微球的外观形态,评价其体外释放行为。结果:当A为4000r.min-1、B为80mg.mL-1、C为1%时,所得微球形态完整,紫杉醇的包封率达到90%以上,体外持续释放30d,累积释药率达80%以上。结论:用优化条件制备的微球中紫杉醇的包封率高,并具有良好的体外缓释性。

Preparation and in Vitro Release Behavior of Paclitaxel Microsphere

OBJECTIVE： To optimize the formulation parameters of polyl, 3 bis（p-carboxyphenoxy） propane-sebacic acid （P（CPP ： SA）） microsphere and evaluate its drug release performance in vitro. METHODS： The paelitaxel microspheres were prepared by single emulsion method, and the effects of the factors such as the stirring speed （A）, P（CPP ： SA） concen- tration （B）, emulsifier polyvinyl alcohol （PVA） concentration （C） on encapsulation efficiency were evaluated by orthogonal test. The surface morphology of the prepared microsphere was observed and its drug release performance in vitro was evalu- ated. RESULTS： The optimal formulation of the microsphere obtained was as follows： A was 4 000 r · min 1, B was 80 mg·mL -1 and C was 1% , respectively. The morphology of microspheres was round and intact. The encapsulation efficiency of paclitaxel was up to above 90%. The sustained release duration was 30 days with an accumulative release rate of over 80%. CONCLUSION： Paclitaxel microspheres prepared by optimal formula display a high encapsulation efficiency and satisfactory sustained - release pattern.