右旋布洛芬缓释微丸的制备及其释药行为分析
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篇名: 右旋布洛芬缓释微丸的制备及其释药行为分析
TITLE:
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Q1 h、

Q4 h、Q10 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。

ABSTRACT:

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 NE30D 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 NE30D was 1.5 ∶ 1,the increased

weight of coating material was 8%. Q1 h,Q4 h and Q10 h of 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.

期刊: 2016年第27卷第1期
作者: 李海刚,陈香,郭绍芬,葛朝晖
AUTHORS: LI Haigang,CHEN Xiang,GUO Shaofen,GE Chaohui
关键字: 右旋布洛芬;缓释微丸;离心造粒法;丙烯酸树脂;体外释药
KEYWORDS: Dexibuprofen;Sustained-release pellets;Centrifugal granulation;Eudragit;Drug release in vitro
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