非pH依赖性苦参碱缓释微丸的研制

Preparation of pH-independent sustained-release pellets of matrine

目的研制苦参碱缓释微丸。方法溶液上药法(流化床底喷装置)制备苦参碱微丸,分别选用乙基纤维素、丙烯酸树脂水分散体及两者同时应用作为包衣材料,采用自制微型流化床进行包衣,分别考察其体外释放度。结果单独使用乙基纤维素、丙烯酸树脂水分散体作控释膜的苦参碱微丸在不同pH条件下的释药行为相差较大;而采用适当比例的乙基纤维素和丙烯酸树脂双层包衣苦参碱微丸在不同pH条件下有相似的释药曲线,体外释放曲线较符合Weibull分布函数。结论苦参碱双层包衣微丸体外释放具有较好的缓释效果,释药不受pH条件的影响。

AIM To study the preparation of sustained-release double-coated pellets of matrine. METHODS Matrine pellets were prepared in a fluid-bed by solution layering and then, coated in a mini fluid-bed by surelease, eudragit or both of them respectively. The release profiles of matrine from coated pellets were studies in distilled water, pH 1.0 HCL and pH 6.8 phosphate buffered solution. RESULTS The drug release profile significantly changed at different pH when pellets were coated by surelease or eudragit, however, the drug release was almost the same in different pH media when pellets were coated by 6% surelease and 5 % eudragit, and accorded with Weibull equation. CONCLUSION The matrine pellets coated with 6% surelease and 5 % eudragit have an obviously sustained-release effect and almost the same drug release profile at different pH.