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目的:优选SPG膜乳化法制备丹参酮ⅡA-聚乳酸-羟基乙酸(PLGA)微球的工艺条件。方法:采用SPG膜乳化法制备丹参酮ⅡA-PLGA微球。在单因素试验基础上,以载药量、包封率及多分散系数(PDI)的综合评分为因变量,通过响应面法考察PLGA质量浓度、流动相流速、聚乙烯醇(PVA)质量浓度及油水相体积比等自变量对处方工艺的影响。结果:最佳处方工艺为PLGA质量浓度44.29 g·L-1,流动相流速825.68 r·min-1,PVA质量浓度2.5 g·L-1,油水相体积比1∶7.86;制备的丹参酮ⅡA-PLGA微球表面光滑圆整且粒径均一,平均粒径2.338μm,PDI指数0.328,载药量1.20%,包封率89.57%,与预测值相对误差较小。结论:采用SPG膜乳化法制备微球的工艺简单、方便,可用于提高丹参酮ⅡA的生物利用度。
OBJECTIVE: To optimize the preparation of tanshinone ⅡA-polylactic acid-glycolic acid (PLGA) microspheres by SPG membrane emulsification method. Methods: Tanshinone ⅡA-PLGA microspheres were prepared by SPG membrane emulsification method. Based on the single factor test, the mass concentration of PLGA, the flow rate of mobile phase, the mass concentration of polyvinyl alcohol (PVA) were determined by response surface method with the comprehensive scores of drug loading, entrapment efficiency and PDI as dependent variables And oil-water volume ratio and other independent variables on the process of prescription. Results: The optimal formulation was PLGA mass concentration of 44.29 g · L-1, mobile phase flow rate of 825.68 r · min-1, PVA concentration of 2.5 g · L-1 and volume ratio of oil to water of 1: 7.86. Tanshinone ⅡA- The surface of PLGA microspheres was smooth and uniform with the average particle size of 2.338μm, PDI index of 0.328, drug loading of 1.20% and entrapment efficiency of 89.57%, which was relatively smaller than the predicted value. Conclusion: The preparation of microspheres by SPG membrane emulsification method is simple and convenient, and can be used to improve the bioavailability of tanshinone Ⅱ A.