摘要
目的以β-环糊精聚合物为载体材料,制备双氯芬酸钠-β-环糊精聚合物缓释微球(DFS-β-CDP微球),优化制备工艺,并对其进行结构表征及释药性能考察。方法采用L9(34)正交实验设计,以载药率和包封率为评价指标,判断药物溶液浓度、载药温度、微球与药物质量比、载药时间等各种因素对实验结果的影响。建立体外分析方法,考察各因素对药物释放的影响。结果制备DFS-β-CDP微球的最佳工艺条件为:DFS浓度为30%,载药温度45℃,微球与药物质量比为1∶1,载药时间24 h。其体外释放行为符合一级动力学方程,24 h累积释放量达86.13%。结论采用正交实验设计完成DFS-β-CDP缓释微球的工艺优化,优化后的处方工艺重复性良好,且具有很好的缓释效果。
Objective To optimize synthesis process of diclofenac sodium -β-cyclodextrin polymer microspheres（DFS-β-CDP MS）, to characterize its structure and evaluate its characteristics of in vitro release. Methods The orthogonal test wasemployed. Drug loading ratio and encapsulation efficiency served as evaluating indexes. The effects of various factors, such as drug concentration, drug loading temperature, mass ratio of microsphere to drug, and drug loading time on the experiment results were investigated. In vitro analytical method was established to study the influence of each ingredient on the release of DFS. Results The best technological conditions were：DFS% = 30% ; temperature = 45 ℃; m（β-CDP MS）m（DFS）= 11; time = 24 h. Drug release pattern in vitro was best described by first-order kinetics; the 24 h -accumulative release was 86. 13% . Conclusion Synthetic process of DFS -β-CDP MS is optimized. The reproducibility of the technology is good. The DFS-β-CDPMS has sustained release characteristic.
出处
《医药导报》
CAS
北大核心
2014年第2期249-254,共6页
Herald of Medicine
关键词
双氯芬酸钠
Β-环糊精
缓释微球
体外释放
Diclofenac sodium
β-cyclodextrin
Sustained release microspheres
In vitro release
