目的 制备pH依赖-酶触型大黄结肠靶向微丸,并优化筛选微丸的制备处方。方法 采用滴制法制备丸芯,以载药量、包封率和释放度为指标,通过正交试验对丸芯处方进行优化。以丸芯包衣后的释药性能为评价指标,进行包衣增重的筛选,最终得到能够在结肠释放药物的大黄微丸。结果 以2%海藻酸钠-果胶溶液、0.7%壳聚糖溶液、1% CaCl₂溶液、pH 6.0的壳聚糖-CaCl₂溶液,投药量4:1(大黄-辅料)的处方制备丸芯,肠溶包衣增重30%,得包衣微丸。该微丸在人工胃液2 h和小肠液3 h的累积释放率分别为2.01%和8.72%,在人工结肠液中4 h累积释放率为92.58%。结论 确定了大黄结肠靶向微丸的制剂处方,初步实现了结肠靶向释放的效果。

Objective To prepare the pH dependent-microbially triggered colon targeted pellets of Rheum and optimize the preparation formulation of the targeted pellets. Methods The pill-core was prepared by dropping preparation method, the pill-core fomulation was optimized by the orthogonal test, with drug loading, entrapment rate, and releasing rate as indexes. With release performance as index, the lagging cover weight increment was screened, the Rheum pellet that released at colon was obtained. Results The 2% alginate-pectin solution, 0.7% chitosan solution, 1% CaCl₂ solution, chitosan-CaCl₂ solution with pH of 6.0, and the 4:1 quantity of reagent (Rheum-accessory) were chosen as the top gallant fomulation to prepare the pill core, then enteric coating weight increased to 30% and the enteric coated-pellet was obtained. In gastric juice after 2 h and in small intestinal juice after 3 h, the coated pellet is cumulatively released to 2.01% and 8.72%, respectively, and released to 92.58% in the colon fluid after 4 h. Conclusion The preparation fomulation of colon targeted pellet of Rheum is definited, and the colon targeted release is preliminary implemented.

国家自然科学基金资助项目(81274005)