pH-时滞型苦参结肠靶向微丸包衣工艺研究及体外评价  

Coating technique of pH-time lag colon-specific matrine delivery mini-pill

作　　者：李小芳[1] 王娇[1] 李珂[1] 曹小勇[1] 熊婷婷[1] 薛钰 

机构地区：[1]成都中医药大学,四川成都610075 [2]香港确思医药公司,四川成都610075

出　　处：《中成药》2009年第12期1841-1844,共4页Chinese Traditional Patent Medicine

基　　金：国家"十一五"科技支撑计划(2006BAI09B08-14);四川省科技支撑项目(2008SZ0044);成都市科技计划(07GGYB520SF-010)

摘　　要：目的:对苦参微丸包控释衣、肠溶衣,制备得pH-时滞型结肠靶向微丸,并对其释放性能进行评价。方法:以苦参碱、氧化苦参碱体外释放度及微丸的外观为指标,对包衣辅料用量、包衣增重等进行筛选。结果:控释层包衣液由2%乙基纤维素、0.4%邻苯二甲酸二乙酯、2%滑石粉的乙醇溶液组成,包衣增重15%。肠溶层包衣液由5%Eudragit S100、3%滑石粉和0.5%柠檬酸三乙酯的乙醇溶液组成,包衣增重35%。该制剂在人工胃液2h后中未见苦参碱、氧化苦参碱的释放,在人工小肠液4h后两指标累积释放百分率均<15%,在人工结肠液2h后分别释放80.7%、83.5%。结论:该微丸能在结肠定位释药。AIM：To study the coating technique of pH-time lap colon-specific matrine delivery mini-pill consisted of the time lag release coating （inner layer） and enteric coating （out layer）. METHODS：To filter the coating composition based on the index of dissolution of matrine and oxymatrine in vitro and the appearance rating of miui-pill. RESULTS：4 The coating composition of inner layer was the alcoholic solution,consisted of 2% EC,0.4% DEP and 2% talc powder. Then the coating composition of out layer was the alcoholic solution consisted of 5% Eudragit S100, 3% talc powder and 0.5% TEC. The dissolution tests in vitro indicated that matrine and oxymatrine were not dissolved in the simulated gastric juice in 2 h. The accumulative amount of matrine and oxymatrine were less than 15% in the simulated intestinal fluid in 4 h. The amount of matrine and oxymatrine were 80.7% and 83.5% in the simulated colon juice in 2 h. CONCLUSION： The mini-pill could achieve the goal of delivering in the specific colon.

关 键 词：pH-时滞型结肠靶向微丸 包衣工艺 体外评价 

分 类 号：R944[医药卫生—药剂学]