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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。
Objective To optimize the preparation of rhubarb anthraquinone (RTA) chitosan (CS) oral colonic microspheres. Methods The encapsulation efficiency and particle size were taken as the investigation indexes and CS as the carrier material. The RTA-CMS was prepared by emulsion-cross-linking method. The optimal preparation process was optimized by orthogonal test. Material Eudragit S100 for coating. The optimum conditions were as follows: 2.5% CS mass fraction, 1: 4 mass ratio of RTA to CS, 1: 1 ratio of liquid paraffin to methylene chloride, 2% Span-80, The rate was 64.5% with a particle size of (248.8 ± 54.2) μm and a particle size of (269.3 ± 172.7) μm after coating. Conclusion The encapsulation efficiency of RTA-CMS prepared according to the preferred process is high, and the morphology of the microspheres is good. It can be used for the preparation of RTA colon-localized CMS.