不同酯化度果胶对苦豆子总碱水凝胶骨架片体外释放的影响  

Effect of pectins of different degree of esterification on in-vitro sophoridine release of hydrophilic matrix tablets containing total alkaloids of Sophora alopecuroides

作　　者：赵文昌[1] 邓虹珠[1] 宋丽军[1] 黄永恒[1] 黄德浩[1] 姚晖[1] 

机构地区：[1]南方医科大学中医药学院,广东广州510515

出　　处：《中国中药杂志》2008年第19期2188-2192,共5页China Journal of Chinese Materia Medica

基　　金：广州市科技局科技攻关项目(2006Z3-E5051-2)

摘　　要：目的:制备苦豆子总碱水凝胶骨架结肠定位释放片,研究不同酯化度果胶对其释放行为的影响。方法:采用湿法制粒压片法制备不同酯化度果胶骨架片,分别考察其在模拟胃液、肠液中6 h释放情况,在此基础上采用Kollicoat MAE 30DP包衣,分析其在模拟胃液、肠液、盲肠液介质中的释放行为。结果:不同酯化度果胶能够明显影响其在模拟胃液、肠液中的释放。采用Kollicoat MAE 30DP包衣的低酯果胶配方E能够使苦豆子总碱中槐定碱结肠释放,近似零级释放模型,属骨架溶蚀释药机制。结论:肠溶包衣的低酯果胶骨架片靶向性强,能够使苦豆子总碱定位释放,从而提高疗效。Objevtive： To prepare colon-targetting tablets of total alkaloids of Sophora alopecuroides and evaluate the effect of pectins of different degree of esterification （DE） on sophoridine release profiles in-vitro. Method： Wet granulation technique was employed to prepare petin-based matrix tablets, then tablets were coated the optimal formulation with Kollicoat MAE 30 DP based on the optimal formulation and analysed their release. Result： Coated formulation E could target total alkaloids of S. alopecuroides to colon and various DE of pectin exerted different effects on sophoridine release. The release of low DE pectin-based matrix tablets coating with Kollicoat MAE 30 DP approximatedly fitted zere-order eqution, which was erosion depended- Conclusion： Low DE pectin-based matrix tablet coating with Kollicoat MAE 30 DP can deliver sophoridine to colon, hence improve the effectiveness of sophoridine.

关 键 词：低酯果胶 高酯果胶 苦豆子总碱 槐定碱 结肠定位释放 

分 类 号：R283[医药卫生—中药学]