五味子多糖微囊的制备及其体外释药特性考察

Preparation of Schisandrae Chinensis Fructus Polysaccharides Microcapsules and Investigation of Its in vitro Release Behavior

摘要:

目的：优选五味子多糖微囊的喷雾干燥工艺并评价其质量和体外释药模式。方法：以壳聚糖为载体，采用喷雾干燥法制备五味子多糖微囊，以收率和载药量的综合评分为指标，通过正交试验考察药物与壳聚糖质量比、壳聚糖质量分数、进样速度、进风温度对制备工艺的影响，评价五味子微囊的质量并考察其体外释药特性。结果：最佳制备工艺为壳聚糖质量分数2.0%，五味子多糖与壳聚糖质量比1：3，进风温度160 ℃，进液速度5 mL·min^-1，空气流速600 L·h^-1；制备的微囊表面光滑圆整、无黏连，载药量22.71%，收率62.04%，包封率83.27%，平均粒径13.47 μm，1，8 h累积释药率分别为47.86%，84.19%，在0~8 h内拟合Higuchi动力学方程Q=29.365t1/2+11.033（r=0.955 7）。结论：采用喷雾干燥法制备的五味子多糖微囊包封率较高，具有一定缓释性能和突释效应。

Abstract:

Objective: To optimize spray drying process of Schisandrae Chinensis Fructus polysaccharides microcapsules and evaluate its quality and in vitro release pattern. Method: With chitosan as a carrier,Schisandrae Chinensis Fructus polysaccharides microcapsules was prepared by spray drying method,orthogonal design was adopted to investigate effects of quality rate of drug-chitosan,the mass fraction of chitosan,inlet velocity and inlet air temperature on preparation technology by taking composite score of yield and drug loading as index,quality of Schisandrae Chinensis Fructus polysaccharides microcapsules was evaluated and investigate its in vitro release characteristics. Result: Optimal preparation process was as follows:drug-chitosan(1 ：3),the mass fraction of chitosan 2.0%,inlet air temperature 160 ℃,inlet velocity 5 mL·min^-1,air flow rate 600 L·h^-1;These prepared microcapsules had rounded smooth surface without adhesions,drug loading was 22.71%,yield was 62.04%,encapsulation efficiency was 83.27%,average particle size was 13.47 μm,cumulative release in 1,8 h were 47.86 and 84.19%,in vitro drug release profile could be described by Higuchi equation of Q=29.365t1/2+11.033(r=0.955 7) at 0-8 h. Conclusion: Entrapment efficiency of polysaccharides chitosan microcapsules prepared by spray drying method was high with some burst effects and sustained release performance.