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目的:优选灯盏花乙素缓释微球的处方和制备工艺并考察其药剂学性能。方法:采用S/O/W型乳化溶剂挥发法制备灯盏花乙素微球,以载药量、包封率及收率的综合评分为指标,通过正交试验优选处方和制备工艺,考察其体外释药性能。采用激光粒度分析仪、扫描电镜、傅里叶红外光谱和X射线衍射法对微球进行表征。结果:最佳制备工艺为投药量25 mg,聚乳酸-羟基乙酸共聚物200 mg,聚乙烯醇质量分数1%,二氯甲烷-丙酮(1.7∶0.3),搅拌转速1 000 r·min-1。灯盏花乙素微球载药量(6.18±0.11)%,包封率(50.79±2.01)%,收率(91.18±2.19)%,释放30%药物所需时间不低于600 h,粒径(126.0±2.1)μm;表面圆整光滑,无黏连;微球内部含有大量灯盏花乙素晶体,灯盏花乙素在高分子材料中未改变其晶体结构。结论:该方法可有效制备灯盏花乙素缓释微球,优选的制备工艺简单合理,为灯盏花乙素制剂的开发提供了参考。
OBJECTIVE: To optimize the preparation and preparation of scutellarin sustained-release microspheres and study its pharmacological properties. Methods: The scutellarin microspheres were prepared by the S / O / W emulsification solvent evaporation method. The drug loading, encapsulation efficiency and yield of the scutellarein microspheres were used as indexes. The orthogonal test was used to optimize the formulation and preparation process, In vitro release properties. The microspheres were characterized by laser particle size analyzer, scanning electron microscopy, Fourier transform infrared spectroscopy and X-ray diffraction. Results: The optimum preparation conditions were as follows: dosage of 25 mg, polylactic acid-glycolic acid copolymer 200 mg, polyvinyl alcohol 1%, dichloromethane-acetone 1.7: 0.3, stirring speed 1000 r · min -1 . The drug-loading capacity of scutellarin microspheres was (6.18 ± 0.11)%, the entrapment efficiency was (50.79 ± 2.01)% and the yield was 91.18 ± 2.19% (126.0 ± 2.1) μm. The surface of the microspheres contained a large amount of scutellarin crystals, and scutellarin did not change its crystal structure in the polymer materials. Conclusion: The method can effectively prepare scutellarin sustained-release microspheres. The preparation process is simple and reasonable, which provides a reference for the development of scutellarin preparation.