黄藤素结肠定位片的制备及其体外释放评价

目的:制备pH依赖、时滞双重机制控制的黄藤素结肠定位片释药系统,并考察其体外释放度.方法:以羟丙甲基纤维素和聚乙二醇6 000作为隔离层,以丙烯酸树脂Ⅳ号和聚乙烯吡咯烷酮作为时滞层,以pH依赖型丙烯酸树脂Ⅱ和丙烯酸树脂Ⅲ的混合溶液作为外层肠溶层.考察包衣片在体外模拟人体胃肠道环境中的释药情况.结果:制备的黄藤素结肠定位片在pH 1.0人工胃液中2h不释药；在pH 6.8人工小肠液中3.5h释药量＜1％；在人工结肠液中6h基本释药完全.结论:所制备的黄藤素结肠定位片具有良好的结肠定位效果.

Preparation and Evaluation its in vitro Release of Fibrauretinum Colon Targeting Tablets

Objective:To prepare fibrauretinum colon targeting tablets delivery system controlled by pH-dependent and time-dependent effects,and to investigate its in vitro release.Method:Fibrauretinum colon targeting tablets were coated sequentially with isolated layer of HPMC and PEG 6 000,time-dependent layer of polyacrylic resin Ⅳ and PVP,and outermost enteric coating layer of polyacrylic resin Ⅱand polyacrylic resin Ⅲ.Release situation of coated tablets in artificial gastrointestinal environment were investigated.Result:There was no drug release of prepared fibrauretinum colon targeting tablets in pH 1.0 artificial gastric juice in 2 hours;In pH 6.8 artificial intesrinal fluid,the amount of release was less than 1% in 3.5 hours;But in pH 7.6 artificial colon fluid,drug was completely released within 6 hours.Conclusion:This study reveals that fibrauretinum colon targeting tablets had a good effect of colon targeting.