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目的:制备蛇床子素缓释微囊并考察其体外释放规律。方法:以明胶、阿拉伯胶为囊材,采用复凝聚法制备微囊,采用紫外分光光度法测含量,均匀设计优化制备工艺。分别以150 mL人工胃液与磷酸盐缓冲液(pH 6.8)为溶出介质,温度(37±0.5)℃,转速100 r·min-1,测定其体外释放度。结果:最佳制备工艺为囊心囊材质量比1∶1.5,温度60℃,戊二醛用量0.8∶120(戊二醛用量/系统体积),制备的微囊圆整光滑,粒径均匀,平均粒径(51.6±4)μm,包封率85.0%,载药量47.2%,体外缓释时间为6 h,其释药特征符合一级动力学过程。结论:蛇床子素微囊制备工艺简单,成囊性和重复性好,微囊具有明显的缓释效果。
OBJECTIVE: To prepare osthole sustained-release microcapsules and investigate its in vitro release patterns. Methods: The gelatin and gum arabic were used as the capsular material. The microcapsules were prepared by the complex coacervation method. The content of the microcapsules was determined by UV spectrophotometry. The optimal preparation technology was designed and optimized. The in vitro release of 150 mL artificial gastric juice and phosphate buffer (pH 6.8) as dissolution medium, temperature (37 ± 0.5) ℃, rotation speed of 100 r · min-1 were measured respectively. Results: The optimum preparation conditions were as follows: the mass ratio of capsule material was 1: 1.5, the temperature was 60 ℃, the dosage of glutaraldehyde was 0.8:120 (the dosage of glutaraldehyde / system volume) The average particle size (51.6 ± 4) μm, entrapment efficiency of 85.0%, drug loading capacity of 47.2% and in vitro sustained release time of 6 h, the release characteristics consistent with the first order kinetics. Conclusion: Osthol microcapsule preparation process is simple, saccharification and repeatability, the microcapsule has a significant sustained-release effect.