β-环糊精聚合物微球的合成及药物控释行为的研究  

Synthesis of β-Cyclodextrin Polymer Beads and Its Behavior of Drug Release

作　　者：吴文娟[1] 郑敦胜[1] 蔡诗填[1] 黄远铿[1] 

机构地区：[1]广东药学院药剂系,广东广州510006

出　　处：《中药材》2007年第3期329-332,共4页Journal of Chinese Medicinal Materials

摘　　要：目的:制备药物控释载体β-环糊精聚合物(β-CDP)微球,并探讨微球对中药制剂的控释机理。方法:以反相乳液聚合法制备β-CDP微球,用相溶解度法研究β-CD对盐酸小檗碱(BH)的包合作用,并以人工肠(胃)液为释放介质,用分光光度法研究微球的体外释放。结果:在pH=1.4(胃)和pH=7.4(肠)条件下,β-CD可与BH形成1∶1摩尔比的包合物,包合常数Ka分别为48.85 L/mol和122.11 L/mol。BH在β-CDP微球中的释放速率存在明显的零级释放规律,且pH=1.4下的释放速率比pH=7.4下的快。结论:β-环糊精聚合物微球是一理想的药物控释载体。Objective： To prepare β-cyclodextrin polymer（β-CDP） beads using as a drug carrier and study the release behaviors of Berberine Hydrochlorrde （BH） in β-CDP beads. Methods： β-CDP beads were synthesized by inverse emulsion polymerization. The inclusion complex between β-CD and BH were investigated by phase solubility method. And the release of BH in vitro was studied by UV spectra. Results ： Inclusion compounds of β-CD and BH with 1 ： 1 molar ratio were found under the condition of pH 1.4 and pH 7.4, with corresponding stability constants of 48.85 L/mol and 122.11 L/mol, respectively. Finally, the controlled release behavior of BH in polymer beads were studied and the release rate of BH kept almost constant after 24h. Release rate of BH was higher at pH 1.4 than that at pH 7.4. Conclusion ： β-CDP beads may be an ideal controlled drug release carrier.

关 键 词：β-环糊精聚合物微球 盐酸小檗碱 包合物 药物控制释放 

分 类 号：R286.02[医药卫生—中药学]