【摘要】 目的制备川芎嗪壳聚糖微球,并对其体外释药模式进行研究。方法采用喷雾干燥法制备川芎嗪壳聚糖微球,以包封产率为指标,考察处方及工艺因素对壳聚糖微球的影响,采用L9(34)正交设计对处方和工艺进行优化。结果壳聚糖质量浓度0.01 g/mL,川芎嗪与壳聚糖的质量比1∶4,进风温度120℃,空气流速500 L/h,所制得的川芎嗪壳聚糖微球表面圆整,载药量为(18.60±0.15)%,包封率为(93.01±0.76)%,平均粒径为(10.69±0.64)μm。体外释放具有良好的缓释特性,在1~15 h内拟合Higuchi方程Q=19.798 t1/2+25.209(r=0.997)。结论采用喷雾干燥法制得的川芎嗪壳聚糖微球包封产率较高,制备工艺简单、过程稳定,可望成为实现中药微球工业化的有效方法。更多还原

【Abstract】 Objective To prepare ligustrazine-chitosan microspheres and to investigate the drug release behavior in vitro. Methods Microspheres were prepared using the spray drying method.The encapsulation efficiency was used to evaluate the influence of different formulation and preparation factors,the formulation was optimized by L9(34) orthogonal design.Results The optimal formulation and preparation factors were as follows: chitosan concentration(0.01 g/mL),ratio of chitosan to ligustrazine(1∶4),inlet temperature(120 ℃),air flow rate(500 L/h).The optimized microspheres had a spherical shape,the loading capacity was(18.60±0.15)%,entrapment efficiency was(93.01±0.76)%,the average diameter was(10.69±0.64) μm.The drug release profile in vitro could be described by Higuchi equation Q=19.798 t1/2+25.209(r=0.997) at 1-15 h,which showed the prepared microspheres obviously had the sustained release effect.Conclusion The encapsulation efficiency of ligustrazine-chitosan microspheres is higher,the preparation method is simple,and the process is stable.It will provide the basis for realizing the industrialization in Chinese materia medica microspheres.更多还原