目的:制备苦豆子总碱结肠定位水凝胶骨架片。方法:以瓜尔胶为骨架材料,采用湿法制粒压片法,通过片在模拟胃液、小肠液、结肠液中的体外释放度评价不同比例瓜尔胶配方对槐定碱的释放影响。结果:骨架片配方A,B,C,D,E所制的颗粒色泽均匀一致,有较好的流动性。苦豆子总碱定位释放片在模拟胃液、小肠液、结肠液中的释放结果表明,瓜尔胶骨架片在6 h内槐定碱释放为13.5%～25.6%,在结肠液中最初6 h释放明显加快,达55.4%～75.1%,至24 h或26 h完全释放。为进一步延缓其最初6 h内释放,作者在配方C的基础上直压瓜尔胶阻止层100 mg制备双层片,体外释放表明双层片在胃液中不释放,在小肠液中释放仅为6.78%,24 h内完全释放,显示了较好的定位释放特性。采用Higuichi方程、一级方程、零级方程模型拟合,配方A,B,C,D,E接近Higuichi释药模型,一级方程模型拟合最差。用Korsmeyer-Peppas equation分析其释药机制为骨架溶蚀释药。结论:苦豆子总碱水凝胶骨架片工艺合理,能够达到结肠定位释放的目的。 OBJECTIVE: To prepare the total alkaloid colon-targeting hydrogel matrix tablets of Sophora alopecuroides. Methods: Guar gum was used as the matrix material to evaluate the release of sophoridine from different proportions of guar gum through the wet granulation and tabletting method in vitro. Results: The tablets made from matrix tablets A, B, C, D, E have the same color and luster, good fluidity. The release of total alkaloids released from Sophora alopecuroides in simulated gastric juice, small intestine fluid and colonic fluid showed that the release of sophoridine was 13.5% ~ 25.6% at 6 h and released in colonic fluid for the first 6 h Significantly accelerated, reaching 55.4% ~ 75.1%, to 24 h or 26 h completely released. In order to further delay its release within the first 6 h, the authors based on the formula C direct guar gum blocking layer 100 mg prepared double-layer tablets, in vitro release shows that the double-layer tablets in the gastric juice is not released in the intestinal fluid release only 6.78%, completely released within 24 h, showing a better positioning release characteristics. The Higuichi equation, the first-order equation and the zero-order equation model were fitted. The formulas A, B, C, D and E were close to the Higuichi release model, and the first-order equation fitted the worst. Korsmeyer-Peppas equation analysis of its release mechanism for the dissolution of skeleton dissolution. Conclusion: Sophora alopecuroides hydrogel matrix piece is reasonable and can achieve the purpose of colon positioning and release.