右旋布洛芬缓释微丸的制备及其释药行为分析  

Preparation of Dexibuprofen Sustained-release Pellets and Analysis on Drug Release Behavior

作　　者：李海刚[1] 陈香[2] 郭绍芬[1] 葛朝晖[1] 

机构地区：[1]临沂大学药学院,山东临沂276000 [2]临沂职业学院,山东临沂276017

出　　处：《中国药房》2016年第1期95-97,共3页China Pharmacy

摘　　要：目的:制备右旋布洛芬缓释微丸,并对其体外释药行为进行分析。方法:以3%羟丙基甲基纤维素(HPMC)为黏合剂,采用离心造粒粉末层积-丙烯酸树脂水分散体包衣法制备右旋布洛芬缓释微丸;以1、4、10 h的累积释放度(Q)的综合评分为指标,以蔗糖-药物的质量比、HPMC-丙烯酸树脂NE30D的质量比、包衣增质量为因素,用正交试验设计优化处方,验证并分析其体外释药情况。结果:最优处方为蔗糖-药物的质量比1∶10、HPMC-丙烯酸树脂NE30D质量比1.5∶1、包衣增质量8%;所制缓释微丸的Q_(1 h)、Q_(4 h)、Q_(10 h)分别为21%、57%、89%(n=3),其零级、一级、Higuchi方程释药模型的相关系数分别为0.956 6、0.989 9、0.996 5。结论:成功制得具有体外缓释作用的右旋布洛芬缓释微丸,其体外释药更符合Higuchi方程。OBJECTIVE：To prepare dexibuprofen sustained-release pellets,and to analyze the drug release behavior in vitro.METHODS：Centrifugal granulation powder layering-eudragit dispersion coating method was used to prepare dexibuprofen sustained-release pellets using 3%HPMC as adhesive agent. The formula of the pellets was optimized by orthogonal test with weight ratio of sucrose to dexibuprofen,weight ratio of HPMC to Eudragit NE30 D and coating weight as factors,using 1,4 and 10 h accumulated release rate（Q） as index. The release of the drug from the pellets was analyzed. RESULTS：The optimized formulation was that the proportion of sucrose to drug was 1 ∶ 10,the weight ratio of HPMC to Eudragit NE30 D was 1.5 ∶ 1,the increased weight of coating material was 8%. Q1 h,Q4 hand Q10 hof prepared pellets were 21%,57% and 89%,respectively（n=3）. The correlation coefficient of zero-order,one-order and Higuchi equation release model were 0.956 6,0.989 9,0.996 5. CONCLUSIONS：Prepared pellets show good sustained-release effect in vitro. Drug release of pellets is more in accordance with Higuchi equation.

关 键 词：右旋布洛芬 缓释微丸 离心造粒法 丙烯酸树脂 体外释药 

分 类 号：R943[医药卫生—药剂学]