pH依赖型重芪结肠靶向微丸的制备及体外释放性能的评价  

Preparation and in vitro release evaluation of pH-dependent colon targetting pellets of Paridis Rhizoma saponin and Astragali Radix polysaccharide

作　　者：刘天易[1] 王信[1] 杨田义[1] 曹广尚[1] 

机构地区：[1]山东中医药大学附属医院,山东济南250011

出　　处：《中草药》2016年第18期3199-3203,共5页Chinese Traditional and Herbal Drugs

基　　金：山东省中医药科技发展计划(2013-082;2015-086)

摘　　要：目的制备pH值依赖型重芪结肠靶向微丸,并对其进行体外释放性能评价。方法采用正交试验法优选微丸的挤出-滚圆法制备工艺参数;采用流化床进行微丸包衣;采用单因素法考察包衣液处方;以重楼皂苷I、重楼皂苷II为指标,进行体外释放性能评价。结果挤出-滚圆法制备pH值依赖型重芪结肠靶向微丸的最佳工艺参数为挤出速率为60 r/min,滚圆速度为1 200 r/min,滚圆时间为5 min;微丸包衣处方为Eudrugit S100增重15%,单硬脂酸甘油酯用量1.5%,柠檬酸三乙酯用量为5%;体外释放度实验表明,pH值依赖型重芪结肠靶向微丸在人工胃液中2 h几乎不释放,在人工小肠液中4 h累积释放度<10%,在人工结肠液中2 h累积释放度>90%。结论 pH值依赖型重芪结肠靶向微丸制备工艺合理可行,具有良好的体外结肠释药特征。Objective To prepare pH-dependent Paridis Rhizoma saponin（PRS） and Astragali Radix polysaccharide（ARP） colon targeting pellets for the treatment of colon cancer and finish its in vitro release performance evaluation. Methods The colon targeted pellets were prepared with extrusion-spheronization and air-flow coating method and the the process parameters were optimized by orthogonal design. The coating fluid prescription was investigated by single factor test. In vitro release performance evaluation of the pellets was evaluated with polyphyllin I and II as the indexes. Results The optimum technologic parameters of extrusion spheronization equipment were as follows： the rate of extrusion was 60 r/min, the rate of spheronization was 1 200 r/min, and the time of spheronization was 5 min. The optimum coating liquid formulation of pH-dependent colon targetting pellets was 15% weight gains of Eudrugit S100, 1.5% anti-plastering aid amount of Glycerin monostearate, and 5% plasticizer amount of TEC. In vitro release test showed that cumulative release rate of berberine hydrochloride was close to 0% in artificial gastric juice after 2 h and less than 10% in artificial intestinal fluid after 4 h, but the cumulative release rate in artificial colon juice after 2 h was more than 90%. Conclusion The preparation method can be applied to the preparation of colon targeted pellets and the pellets can achieve the targeted release in the colon.

关 键 词：重楼 黄芪 结肠靶向微丸 体外释放 累积释放度 pH值依赖 正交试验 挤出-滚圆法 重楼皂苷Ⅰ 重楼皂苷Ⅱ 

分 类 号：R283.6[医药卫生—中药学]