目的 研究黄芪多糖pH依赖-时滞性结肠靶向微丸的制备工艺。方法 采用挤出-滚圆法及流化床包衣法制备结肠靶向剂黄芪多糖微丸,响应面优化法筛选最佳制备工艺。结果 丸芯组成:黄芪多糖药粉、微晶纤维素、微粉硅胶、交联羧甲基纤维素钠比例为25∶15∶8∶2,水为润湿剂挤出滚圆成丸,挤出速率为60 r·min^-1,滚圆速率为1 400 r·min^-1,滚圆时间为4 min。最佳流化床包衣条件是风机频率为29.50 Hz,喷枪压力为0.70 kg·cm^-2,包衣流速为3.00 mL·min^-1,包衣增重为15%。微丸在人工胃液中2 h释放度为0%,在人工小肠液中3 h释放度<5%,在人工结肠液2 h释放完全。结论 该制备方法适用于黄芪多糖微丸的制备,操作简单,重现性良好,适用于工业生产。

OBJECTIVE To study the preparation process of pH-dependent delayed colon targeting pellets of astragalus polysaccharide. METHODS Colon targeting agents of APS pellets were produced by extrusion-spheronization and fluid bed coating method and the best preparation technology was chosen by response surface optimization method. RESULTS The ratio of pill core:APS powder-avicel-tannic acid-carboxymethylcellulose sodium was 25∶15∶8∶2, the wetting agent was water, the rate of extrusion was 60 r·min^-1, the rate of spheronization was 1 400 r·min^-1, and the time of spheronization was 4 min. The best fluid bed coating condition was as follows the fan frequency was 29.50 Hz, the pressure of spray gun was 0.70 kg·cm^-2, the rate of coating flow was 3 mL·min^-1, and the colon coating weight was 15%.The release degree of pill for simulated gastric fluid in 2 h was 0%, The release degree of pill for artificial intestinal fluid in 3 h was less than 5%. The release degree of pill for artificial colon fluid in 2 h was release completely. CONCLUSION The preparation method can be qpplied to the preparation of APS pellets, it′s simplicity of operator and had good reproducibility, it can be applied to the industrial production.