[关键词]
[摘要]
目的 优选大黄总蒽醌(RTA)壳聚糖(CS)口服结肠定位微球的制备工艺.方法 以包封率和粒径为考察指标,CS为载体材料,采用乳化-交联法制备RTA壳聚糖微球(RTA-CMS),并用正交试验优选最佳制备工艺,再采用肠溶材料Eudragit S100进行包衣.结果 优选的最佳工艺为CS质量分数为2.5%,RTA与CS质量比为1:4,液体石蜡与二氯甲烷的比例为1:1,司盘-80用量为2%,微球包封率为64.5%,粒径为(248.8±54.2)μm,包衣后粒径为(269.3±172.7)μm.结论 根据优选工艺制备的RTA-CMS包封率较高,微球形态良好,可用于RTA结肠定位CMS的制备.
[Key word]
[Abstract]
Objective To optimize the preparation technology of colon-specific chitosan microspheres of rhubarb total anthraquinones (RTA-CMS). Methods With chitosan as material, RTA was made into microspheres. According to the entrapment efficiency (EE) and particle diameter, the best preparation technology was selected using orthogonal design. The enteric material Eudragit S100 was used to coat the CMS. Results The best preparation technology was as follows: The concentration of chitosan was 2.5%; The mass ratio of RTA and chitosan was 1:4; The ratio of paraffin and dichloromethane was 1:1; The amount of span-80 was 2%. The EE of CMS was 64.5%. The particle diameter of the CMS was (248.8 ± 54.2) μm, and the mean diameter was (269.3 ± 172.7) μm after coating. Conclusion RTA-CMS prepared with the best preparation technology has a high EE. And the microspheres form is good. The technology could be used to prepare colon-specific RTA-CMS.
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[基金项目]
国家自然科学基金资助项目(81073146,81341143);河北省高等学校科学技术研究重点项目(ZH2012050);河北省高校重点学科建设项目