苦参碱双敏感结肠定位小丸的制备及体外释放研究

Study on preparation of matrine double-sensitive conlon-specofic pellets and in vitro release

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 double-sensitive conlon-specofie pellets and study the factors affecting its quality and evaluateing the colon-specific effects of preparation. Method： Matrine enzyme-sensitive pellets core were prepared by carboxymethyl konjac glucomannan as the main carrier material, and coated the core by acrylic resin Ⅱ and Ⅲ to prepare matrine double-sensitive conlon-speeofic pellets. The prescription and technology of the matrine conlon-specofic pellets were studied by the single factor investi- gation , through the in vitro release test and coating rate determination. Result： The optimized process conditions ： FeC13 concentration is 4. 0 g·L^-1, chitosan concentration is 3.0 g·L^-1, earboxymethyl konjac glucomannan concentration is 20 g ·L^-1, mixed gel solu- tion pH value is 3. The release of matrine is less than 30% in the simulation of the upper gastrointestinal medium. The release of matrine is close to 100% in simulated full gastrointestinal medium, the coating weight is 7%. Conclusion： The prepared matrine pellets have good colon positioning effect in vitro.