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采用离子交联法制备当归超临界提取物丸芯,以丸芯载药量和包封率为指标,对影响载药量和包封率的多个因素进行考察,并采用Box-Behnken试验设计和响应面分析法对载药丸芯的处方进行优化,然后进行包衣工艺研究。通过体外释放研究,优选当归超临界提取物结肠定位微丸的包衣工艺及处方并评价其结肠靶向性。确定最佳的丸芯制备工艺∶3%果胶,果胶与卵磷脂比为4∶1,果胶药物比为4∶5,4%的醋酸锌溶液为交联剂,混匀温度35℃,交联温度35℃,交联时间30 min;包衣工艺∶包衣材料为尤特奇FS30D,包衣材料1.5%的柠檬酸三乙酯和聚氧乙烯脱水山梨醇单油酸酯(吐温-80),包衣材料1.2%的单硬脂酸甘油酯,包衣增重15%。最优工艺制备的当归超临界提取物结肠定位微丸在人工胃液中2 h几乎无释放,人工小肠液中4 h释放小于20%,人工结肠液中6 h释放大于90%,说明制备的当归超临界提取物结肠定位微丸具有良好的结肠靶向性。
The preparation of Angelica sinensis supercritical extract pellets by ion-crosslinking method was carried out by taking the drug loading and entrapment efficiency of pellets as indices to study the factors influencing drug loading and entrapment efficiency. The Box-Behnken test design And response surface analysis method to optimize the prescription of loaded pills, and then study the coating process. Through the study of in vitro release, the process and prescription of Angelica supercritical extract colon-targeting pellets were optimized and colon targeting was evaluated. Determine the best core preparation process: 3% pectin, pectin and lecithin ratio of 4: 1, pectin drug ratio of 4: 5, 4% zinc acetate solution as a crosslinking agent, mixing temperature 35 ℃ , Crosslinking temperature of 35 ℃, crosslinking time of 30 min; coating process: the coating material is Eutech FS30D, coating material 1.5% triethyl citrate and polyoxyethylene sorbitan monooleate Temperature -80), 1.2% of coating material glycerol monostearate, coating weight gain of 15%. Angelica supercritical fluid colloidal pellets prepared by the optimal process were almost not released for 2 h in artificial gastric juice, less than 20% in artificial intestinal fluid for 4 h, and more than 90% in artificial colon fluid for 6 h, indicating that Angelica sinensis Supercritical fluid colonic colonized pellets have good colon targeting.