【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。更多还原

【Abstract】 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.更多还原