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目的:制备苦参碱双敏感结肠定位小丸,并研究影响其质量的因素和评价其结肠定位释药的效果。方法:以羧甲基魔芋胶为主要载体材料,制备酶敏感丸芯,再以丙烯酸树脂Ⅱ,Ⅲ包衣,制成苦参碱双敏感结肠定位小丸;通过体外释放试验和包封率测定,对影响制剂释药的处方和工艺进行单因素考察。结果:苦参碱双敏感结肠定位小丸的优化制备工艺条件为FeCl3质量浓度为4.0 g·L-1,壳聚糖质量浓度为3.0 g·L-1,羧甲基魔芋胶质量浓度为20 g·L-1,混合胶浆pH为3,包衣增重为7%;在模拟全消化道介质中,苦参碱累积释放接近100%,时滞为7 h。结论:所制苦参碱双敏感结肠定位小丸在体外具有良好的结肠定位效果。
OBJECTIVE: To prepare matrine dual sensitive colon-targeted pellets and investigate the factors influencing their quality and to evaluate their colon-specific release. Methods: Carboxymethyl konjac glucomannan was used as the main carrier material to prepare enzyme-sensitive pellets, which were then coated with acrylic resin Ⅱ and Ⅲ to make matrine double sensitive colonic pellets. Through in vitro release test and entrapment efficiency, The formulation and process of drug release affect single factor study. Results: The optimum preparation conditions of matrine dual sensitive colon-targeted pellets were as follows: the mass concentration of FeCl3 was 4.0 g · L-1, the concentration of chitosan was 3.0 g · L-1, the concentration of carboxymethyl konjac gum was 20 g · L-1, the pH value of mixed mortar was 3, and the weight gain of coating was 7%. In simulated total digestive tract medium, cumulative release of matrine was nearly 100%, with a time lag of 7 h. Conclusion: The matrine dual sensitive colon-targeted pellets have good colonic localization in vitro.