葛根素缓释微球的高分子材料考察及制备工艺优选

Investigation of Polymer Materials and Optimization of Preparation Process of Puerarin Sustained-release Microspheres

目的:筛选葛根素缓释微球的高分子材料并优选其制备工艺。方法:采用乳化溶剂挥发法制备葛根素缓释微球,以包封率、载药量及收率的综合加权评分为指标,通过正交试验优选高分子材料,考察投药量、聚乳酸(PLA)用量和聚乙烯醇(PVA)质量分数对葛根素缓释微球处方工艺的影响。采用扫描电镜(SEM)、综合热分析(TGA)、差示扫描热分析(DSC)及X射线衍射法(XRD)对微球进行表征。结果:葛根素缓释微球最适高分子材料为PLA,最佳制备工艺为投药量37.5 mg,PLA用量80 mg,PVA质量分数0.5%。葛根素缓释微球表面光滑圆整,无黏连,平均粒径104.3μm,载药量(26.20±2.24)%,包封率(68.92±1.88)%,收率(83.97±2.55)%;TGA,DSC,XRD等证实制备成微球后葛根素与聚合物分子空间结构可能发生了物理形式的变化。结论:采用乳化溶剂挥发法成功制备了葛根素缓释微球,工艺简单合理、操作稳定。

Objective： To optimize polymer materials and preparation process of puerarin sustained- release microspheres. Method： The microspheres were prepared by emulsion solvent evaporation method. Taking composite score of encapsulation efficiency, drug loading and yield as index, polymer materials and formulation process were optimized by orthogonal design. The microspheres were characterized by different techniques, such as scanning electron microscopy （SEM）, thermogravimetric analysis （TGA）, differential scanning calorimetry （ DSC ） , X-ray diffraction （ XRD）. Result： Optimum polymer material of puerarin sustained-release microspheres was polylactic acid （PLA） , optimum preparation parameters were as follows： dosage of 37.5 mg, PLA of 80 mg, polyvinyl alcohol （PVA） of 0.5%. Surface of puerarin sustained-release microspheres was smooth and round without adhesions, average particle size was 104.3 μm, drug loading was （26.20 ± 2.24）%, encapsulation efficiency was （68.92 ± 1.88） % , yield was （83.97 ± 2.55） %. TGA, DSC and XRD were indicated changes in physical form of molecular spatial relationship of copolymer and puerarin in the microspheres. Conclusion： Puerarin sustained-release microspheres can be successfully prepared by emulsion solvent evaporation method, optimized process is simple and reasonable.