鞣酸小檗碱口服结肠定位包衣片的制备及体外释药性  

Preparation and release in vitro of berberine tannate colon-specific coated tablets

作　　者：李雪[1] 金描真[1] 叶放 王晓明[1] 金鸽[1] 

机构地区：[1]广东药学院药剂教研室,广东广州510006 [2]广州白云山制药有限公司白云山化学药创新中心,广东广州510515

出　　处：《广东药学院学报》2009年第3期221-225,共5页Academic Journal of Guangdong College of Pharmacy

摘　　要：目的研究鞣酸小檗碱结肠定位包衣片的制备工艺,并考察体外释放条件对包衣片结肠定位及结肠释放行为的影响。方法以壳聚糖和聚丙烯酸树脂为包衣材料,采用喷雾包衣的方法制备pH依赖与酶降解相结合型结肠定位包衣片,并研究包衣片在模拟人体胃肠道环境中的释放情况。结果鞣酸小檗碱结肠定位包衣片在模拟胃液中2 h不释药、模拟小肠液(pH 6.8的磷酸盐缓冲液)的介质中5 h释药小于5%,在模拟结肠环境的介质(pH 7.6磷酸盐缓冲液,含30%大鼠结肠内容物)中累积释放度大于85%。结论鞣酸小檗碱结肠定位包衣片可在结肠定位,且体外释放度满足结肠定位制剂的要求。Objective To study the preparation of berberine tannate colon-specific coated tablets, and investigate the effects of in vitro release conditions on the colon-targeting effects of the coated tablets and colon-targeted release. Methods The pH-and enzyme degradation dependent colon-specific coated tablets were prepared by spraying coating method, coated with chitosan and polyacrylic resin, and the release profile of berberine tannate colon-specific coated tablets was determined in the simulated gastrointestinal tract environment. Results The tablets could not release in the simulated gastric fluid and in the simulated small intestine fluid（ pH = 6.8 phosphate buffer）, the drug release was under 5% in five hours, but the cumulative release rate exceeded 85% of labeled amount in the simulated colon fluid （ pH = 7. 6, containing 30% colonic contents of rats）. Conclusion Berberine tannate colon-specific coated tablets was colon-targeted and satisfied the requirement for in vitro release of colon-specific delivery.

关 键 词：鞣酸小檗碱 结肠定位包衣片 体外释放度 

分 类 号：R94[医药卫生—药剂学]