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目的制备以果胶钙和醋酸纤维素为包衣材料,5-氨基水杨酸(5-ASA)为模型药物的酶触发渗透泵型结肠定位微丸,并考察其体外释药特征及释药机制。方法采用包衣锅法制备含药丸芯,选用L9(3)4正交实验设计,以体外释放度为评价指标优化包衣液处方及丸芯中渗透剂的用量,并进行体外释药模型拟合。结果制备5-ASA渗透泵酶触发微丸最佳工艺参数为:包衣增重25%;药物与NaCl(丸芯)比为3∶1;醋酸纤维素与果胶钙(包衣液)用量比为2∶3。所得微丸在人工胃液中2 h,人工小肠液中4 h累计释放率<8%,人工结肠液12 h累计释放率>70%,表明结肠定位性较为突出,且可以在结肠持续释放药物以维持局部药物浓度,进一步研究释药机理表明为零级释放。结论采用果胶钙与醋酸纤维素为包衣材料制备渗透泵酶触发结肠定位微丸可实现结肠定位作用。
OBJECTIVE To prepare enzyme-triggered osmotic pump colon-targeted pellets with 5-aminosalicylic acid (5-ASA) as coating material and pectin calcium and cellulose acetate as coating materials, and investigate its in vitro release characteristics and drug release mechanism. Methods The drug-containing pellets were prepared by the coating pan method. The orthogonal design of L9 (3) 4 was used to optimize the formulation of the coating solution and the amount of penetrant in the pellet with the release rate in vitro as evaluation index. The in vitro drug release model Together Results The optimum process parameters of 5-ASA osmotic pump-triggered pellets were as follows: coating weight gain 25%; drug to NaCl ratio 3: 1; dosage of cellulose acetate and calcium pectinate The ratio is 2: 3. The obtained pellets in artificial gastric juice 2 h, artificial intestinal fluid 4 h cumulative release rate of <8%, artificial colon 12 h accumulated release rate of> 70%, indicating that colon colonization is more prominent and can be sustained release of drugs in the colon to Maintaining local drug concentration, further study of drug release mechanism showed zero-order release. Conclusion The use of calcium pectinate and cellulose acetate as coating material preparation of osmotic pump-activated colon-targeted pellets can achieve colonic localization.