摘要
目的制备紫薯花青素胃漂浮缓释片,并应用星点设计-效应面法进行处方优化。方法采用湿法制粒压片,以羟丙基甲基纤维素(HPMC)为主要辅材、碳酸氢钠为起泡剂、共聚维酮为黏合剂以及乳糖等制备紫薯花青素胃漂浮缓释片,以体外漂浮性能和体外释放度为评价指标,应用星点设计-效应面法优化制剂处方,并进行验证。结果最佳处方为:HPMC 19.08%、碳酸氢钠14.34%、共聚维酮7.12%、乳糖49.46%,整粒后加入硬脂酸镁1%。经最优处方制得紫薯花青素胃漂浮缓释片,起漂时间<5min,续漂时间>11h,体外释放曲线具有明显的缓释特征,11h累积释放率可达95%以上。体外释放曲线拟合方程后,证明其体外释放为非Fick扩散,过程以扩散与骨架溶蚀为主。结论应用星点设计-效应面法优化筛选出最佳处方,按照最优处方制备的紫薯花青素胃漂浮缓释片具有良好的漂浮性能并且能够持续缓慢释药。
Objective To prepare gastric-floating sustained release tablets of purple sweet potato anthocyanin and use central composite design-response surface methodology to optimize its formulation.Methods Purple sweet potato anthocyanin gastric-floating sustained release tablets were prepared by the wet granule compression technique,using HPMC as main auxiliary material,sodium bicarbonate as foaming agent,PVP/VA as binder and lactose,etc.The formulation of purple sweet potato anthocyanin gastric-floating sustained release tablets was optimized by central composite design-response surface methodology with in vitro floatability and in vitro release as evaluation indexes.Results The best prescription was HPMC 19.08%,sodium bicarbonate 14.34%,PVP/VA 7.12%,lactose 49.46%,and added 1% magnesium stearate after granulation.Purple sweet potato anthocyanin gastric-floating sustained release tablets were prepared by optimum formulation.Initial floating time was less than 5 minutes and the duration of floating was longer than 11 hours.The in vitro release curve showed obvious sustained release characteristics.The cumulative release rate of purple sweet potato anthocyanin was over 95% after 11 hours.After fitting the release curve in vitro,it was proved that the release in vitro was non-Fick diffusion,and the main process was diffusion and matrix dissolution.Conclusion Central composite design-response surface methodology was used to optimize the optimal formulation.Purple sweet potato anthocyanin gastric-floating sustained release tablets prepared according to the optimal formulation had good floating performance and sustained slow release.
作者
白明勇
周钥
姜雪冰
程忠
吴逸凡
杨洪致
陈秋红
Bai Ming-yong;Zhou Yue;Jiang Xue-bing;Cheng Zhong;Wu Yi-fan;Yang Hong-zhi;Chen Qiu-hong(Chengdu University of Technology,Chengdu 610051)
出处
《国外医药（抗生素分册）》
CAS
2020年第3期228-234,共7页
World Notes on Antibiotics
基金
成都理工大学青年骨干教师资助项目(10912-2019KYGG01516)
药食同源植物资源开发四川省高校重点实验室开放基金重点项目(10Y201806)
大学生创新创业训练计划(省级,201810616134)。
关键词
紫薯花青素
胃漂浮缓释片
星点设计-效应面法
purple sweet potato anthocyanin
gastric-floating sustained release tablets
central composite design-response surface methodology
