摘要
目的正交试验法优化酮洛芬羟丙基-β-环糊精包合物(KP-HP--βCD)的制备工艺。方法在确定较适宜的制备方法的基础上,以包合物溶解度为指标,考察主客分子摩尔比、制备温度和搅拌时间等因素对制备KP-HP--βCD包合物的影响。结果通过正交试验优化筛选出的最佳方案是主客分子比1.5∶1,制备温度45℃,搅拌4 h,此方案制备的包合物溶解度为49.91 g/L,收率为(96.21±5.73)%,载药量为(10.31±0.55)%;包合物可使酮洛芬在水中的溶解度增大47倍,其溶出速率参数Td和T50明显小于普通胶囊剂。结论优化工艺制备的包合物操作简便、适合工业化生产,且包合物可显著提高酮洛芬的溶出速率。
Objective To screen and optimize the manufactural conditions of ketoprofen-hydrox-ypropyl-β-cyclodextrin（KP-HP-β-CD） inclusive complex with stiring method. Methods The load-drug and solubility of KP-HP-β-CD were adopted as the index. Host-guest molar ratio, temperature and stiring time investigated in the techniques for KP-HP-β-CD preparing. Results Host-guest molar ratio 1.5：1, 45 ℃, and 4 h stiring time made the receiving rate of （90.53±4.57） % and load-drug volume of （9.12±0.19） % better than the ultrasonic method [ （70.68±5.68） % and （7.98±0.23） % ] and grinding method [ （86.45±7.13） % and （5.11±0.16） 96 ]. The solubility of ketoprofen was increased from 1.06 g/L to 49.91 g/L when it was included by HP-β-CD. At the same time, the dissolution test showed that ketoprofen was released faster than that in capsules or mixture form. Conclusion The optimizing techniques fit to prepare of KP-HP-β-CD .
出处
《福建医科大学学报》
2005年第4期437-440,共4页
Journal of Fujian Medical University
基金
福建省科技厅青年科技人才资助项目(2004J045)
关键词
酮洛芬
Β-环糊精
正交试验
工艺学
制药
β-cyclodextrin
orthogonal test
techorology, phar maceutical
