盐酸坦索罗辛缓释微丸的单颗粒及其颗粒群释放动力学研究  

Release kinetics of single pellets and the multi-pellet system of tamsulosin hydrochloride sustained release pellets

作　　者：杨硕[1,2] 王彩芬[2,3] 李雪[2] 李颖[2] 殷宪振[2] 郭涛[2] 张继稳[2,3] 何珺[1] 孙立新[3] 

机构地区：[1]贵州省生化工程中心,贵州贵阳550025 [2]中国科学院上海药物研究所,上海201203 [3]沈阳药科大学,辽宁沈阳110016

出　　处：《药学学报》2014年第4期535-542,共8页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目(81273453)

摘　　要：以盐酸坦索罗辛(tamsulosin hydrochloride,TSH)缓释胶囊为对象,采用液相色谱串联质谱法研究单微丸释放行为。依据单微丸含药量进行分组,将组内平均释药与整个胶囊的释药行为进行差异因子(f1)和相似因子(f2)分析,比较其差异性和相似性。采用主成分分析法研究微丸释放行为的分类特征;利用Matlab软件构建具有特定释药特征的颗粒群。结果表明,各单微丸的释放特征与含药量具有一定的相关性。与胶囊的整体释放行为相比,含药量较低组的释药相似(f2=62.2、67.1、53.9),含药量最高的一组微丸释药不相似(f2=43.3)。通过组合不同数量的单微丸,可构建具有目标释药特征的多单元给药系统。研究单微丸的释药特征对深入了解多单元给药系统的释放规律具有重要的方法学意义。The release behavior of single pellet was investigated by LC/MS/MS method with tamsulosin hydrochloride （TSH） as the model drug of the research and then the pellets were divided into four groups according to the drug loading. Comparison of dissolution profiles of each group and capsule were performed using f1 and f2 factor methods to study the difference and similarity. The release profiles of single pellet, each group and capsule were analyzed using principle component analysis （PCA）. The particle system was built through Matlab to get the target release profile. The result of this research demonstrated the release behavior of single pellet correlated well with the drug loading. While the dissolution profile of capsule as a reference, the similarity factor of dissolution profiles of the lower drug loading groups were 62.2, 67.1, 53.9, respectively and, 43.3 for highest drug loading group. The particle systems with different pellet distribution and same release profiles were built through release behavior of single pellet. It is of significance to investigate the release behavior of single pellets for studying the release regularity of multiple-unit drug delivery system.

关 键 词：盐酸坦索罗辛 单微丸 释放动力学 液相色谱串联质谱法 多单元给药系统 颗粒群 

分 类 号：R943[医药卫生—药剂学]