左羟丙哌嗪缓释骨架片的制备及体外释药行为评价  

Preparation of levodropropizine sustained release matrix tablet and its in vitro evaluation of drug release

作　　者：曹青日[1] 崔载胜 崔京浩[1] 

机构地区：[1]苏州大学医学部药学院,苏州215123 [2]EuraPharmInc.中央研究所

出　　处：《中国新药杂志》2010年第14期1222-1224,1228,共4页Chinese Journal of New Drugs

基　　金：国家重大新药创制科技重大专项(2009ZX09502-009)

摘　　要：目的：制备左羟丙哌嗪缓释骨架片,考察其体外释放度,探讨其释药机制。方法：以亲水性高分子材料HPMC为骨架,采用湿法制粒,制备左羟丙哌嗪缓释骨架片,评价不同pH值条件下的释放度,并将释放数据拟合方程。结果：HPMC用量增加,左羟丙哌嗪释放速度下降;溶出介质pH对药物的释放特性有一定影响。在本实验条件下,HPMC用量对水溶液中药物的释放机制无明显影响,释药过程符合H iguchi方程（R^2=0.988 9-0.990 4）或一级方程（R^2=0.987 5-0.990 2）,释药机制为非Fickian扩散（n=0.615 3-0.633 9）。结论：左羟丙哌嗪缓释骨架片的体外释放符合缓释要求,释放表现为药物扩散和凝胶溶蚀的协同作用。Objective：To prepare levodropropizine sustained release matrix tablet,and to study the drug release behavior and mechanism in vitro.Methods：Sustained release matrix tablets of levodropropizine were prepared by wet granulation method using hydrophilic polymer HPMC.Release profiles of the tablets were characterized in four dissolution media with different pH,and fitted with different dissolution equation.Results：The release rate of drug was decreased as the increased amount of HPMC.The pH of dissolution media was also influenced on the release of levodropropizine from sustained release tablets.The drug release in water followed well to the Higuchi equation（R^2=0.988 9～0.990 4） and first order linear equation（R^2=0.987 5～0.990 2）.The mechanism of controlling drug release was displayed as the non-Fickian diffusion（n=0.615 3～0.633 9）.Conclusions：The release pattern of levodropropizine from HPMC sustained release matrix tablets conformed the requirement.The mechanism of drug release was proved as the combination of diffusion and erosion.

关 键 词：左羟丙哌嗪 缓释骨架片 释放度 释药机制 

分 类 号：R943.41[医药卫生—药剂学] R974.2[医药卫生—药学]