穿心莲内酯微球制备工艺的优化

Optimization of preparation technology of andrographolide microsphere

目的优化穿心莲内酯微球的制备工艺。方法乳化交联法制备穿心莲内酯微球,以载药量、包封率等为指标,采用正交设计法筛选穿心莲内酯微球最佳制备工艺,并对工艺进行验证;对含药微球进行表征。结果微球外观形态良好;最佳工艺条件为明胶浓度为20%(g/m L),乳化温度为40℃,搅拌速度为2000r/min,平均载药量为3.88%,包封率为23.23%;工艺重现性良好。结论穿心莲内酯微球的制备工艺切实可行,为穿心莲内酯剂型的现代化提供参考。

Objective To optimize the conditions of preparation technology of andrographolide microsphere. Methods Andrographolide microspheres were prepared by a kind of emulsion crosslinking method. The preparation technology were optimized, through orthogonal design, using the encapsulation efficiency and drug loading as selection indexes. Technology conditions were verified. Microsphere appearance was studied. Results The microspheres had good appearance. The best optimum of the technological conditions were gelatin concentration of 20%（g/m L）, emulsification temperature of 40 C and stirring speed of 2000 r/min, average drug loading of 3.88%, and encapsulation efficiency of 23.23%. The process has good reproducibility. Conclusion This preparation technology of andrographolide microspheres is feasible. The development offers reference for modernization of dosage forms of andrographolide.