pH敏感结肠宁靶向微丸的制备及体外释药性能评价

Preparation and in Vitro Drug Release Evaluation of pH-Sensitive Jiechangning Colon-Targeted Pellets

目的研制pH敏感结肠宁靶向口服微丸。方法由结肠宁药粉、微晶纤维素、交联羧甲基纤维钠和羧甲基淀粉钠制备软材,经挤出滚圆机制备素丸,以EudragitS100、滑石粉和柠檬酸三乙酯为主要成分的包衣材料对干燥的素丸进行包衣,包衣分别增重10%,15%,18%,并评价体外药物释放度。结果包衣增重10%,15%,18%的靶向微丸在pH=1.0的盐酸溶液中的释放度分别为19.64%,9.67%,6.50%,在pH=6.8的磷酸盐缓冲液中的释放度分别为77.80%,89.13%,92.37%。结论以EudragitS100、滑石粉和柠檬酸三乙酯为包衣材料,包衣增重15%以上,可制备出较理想的结肠宁靶向微丸。

Objective To research the pH- sensitive oral Jiechangning Colon-Targeted Pellets. Methods Jiechangning powder, mi- crocrystalline cellulose, cross- linked carboxymethyl cellulose sodium, sodium carboxymethyl starch were blent into soft materials and the pellets were prepared by the rolling extrusion machine. Then the dried pellets were coated by the coating materials with Eudragit S100, talcum powder and triethyl citrate as the main ingredients. The increments of coating weight was 10%, 15% and 18% respectively. Results The release rates of coated pellets with coating weight increment of 10%, 15% and 18% were 19.64%, 9.67% and 6.50% in pH = l. 0 hydrochloric acid solution respectively, which were 77.80%, 89. 13% and 92.37% in pH = 6.8 phosphate buffer respectively. Conclusion With Eudragit~ S100, talcum powder and triethyl citrate as the coating materials and the coating weight increment 〉 15%, the more ideal Jiechangning Colon- Targeted Pellets can be prepared.