鞣花酸壳聚糖-海藻酸钠微球的制备工艺

Preparation process of chitosan-sodium alginatealginate ellagic acid microspheres

目的:优化鞣花酸壳聚糖-海藻酸钠微球的最佳制备工艺。方法:采用一步法,以壳聚糖-海藻酸钠作为载体材料制备鞣花酸微球,并以微球载药量和包封率为考察指标,通过单因素筛选及正交设计优化出鞣花酸壳聚糖-海藻酸钠微球的制备工艺。用溶出仪在900 ml释放介质(pH6.86)和120 r·min-1转速条件下测定释放度。结果:优化工艺为海藻酸钠与药物比为3∶1,氯化钙质量分数为2%,海藻酸钠质量分数为2%,壳聚糖质量分数为0.1%,温度为60℃,pH为5,所得鞣花酸平均粒径为(980±100)μm,平均载药量为27.22%,平均包封率为97.73%,48 h释放度为74.22%。结论:本制备工艺稳定,操作简便,重现性好,可用于鞣花酸壳聚糖-海藻酸钠微球的制备。

OBJECTIVE To optimize preparation process of chitosan-alginate ellagic acid microspheres.METHODS An improved one-step method was used to prepare ellagic acid microspheres with chitosan-alginate.Single factor screening and orthogonal design was applied by adopting standard of drug encapsulation efficiency and drug loading,to obtain optimal formulation of chitosan-alginate ellagic acid microspheres.Release rate was 900 mL for phosphate buffer（pH=6.86）and speed was120 r·min-1.RESULTS Optimal formulation was 3∶1 of mass ratio of alginate sodium/ellagic acid,2% CaCl2,2% Na-alginate,0.1% chitosan,at a temperature of 60 ℃,pH value of 5.Average diameter,drug loading and drug encapsulation efficiency were（980±100）μm,27.22%and97.73%,release rate was 74.22%at 48 h.CONCLUSION Optimized process is stable,practicable and repeatable.It is suitable for chitosan-alginate ellagic acid microspheres.