桂枝茯苓双层缓释片处方设计和优化研究

目的 确定桂枝、茯苓活性成分同步释放的双层骨架缓释片处方.方法 以常规制剂中芍药苷、苦杏仁苷、丹皮酚的溶出和吸收特点为依据,将桂枝茯苓方设计为芍药苷、苦杏仁苷、丹皮酚为同步释放的缓释制剂;以各提取物的表观溶解度为依据,将各提取物分为水溶性提取物和水难溶性提取物2部分;权重转换方程计算每个成分在2、4、10 h释放度的得分,以芍药苷、苦杏仁苷、丹皮酚的得分之和为综合评分指标,优选桂枝茯苓双层骨架缓释片的处方,以相似因子评价芍药苷、苦杏仁苷、丹皮酚释放的同步性.结果 当HPMCK4M为水难溶性成分层的15%,HPMCK4M为水溶性成分层的22%.EC20为水溶性成分层的27%时,芍药苷、苦杏仁苷、丹皮酚在2、4、10 h的释放度均在设定的理想释放度范围内(20%

Formula design and optimization of Guizhi Fuling double layers sustained-release tablet

Objective To set up the formula of Guizhi Fuling double layers sustained-release tablet with active ingredients synchronously releasing.Methods The Guizhi Fuling preparation was designed into double layers sustained-release tablet with peoniflorin,laetrile,and paeonol synchronously releasing based on dissolution and absorption characteristic of three active ingredients in ordinary formulation.Six extracts were divided into two groups based on their solubility in water,respectively.Calculating scores of the three active ingredients at 2,4,and 10 h by the equation for calculating transformed Fih,respectively,optimizing the formula based on the sum of the score of peoniflorin,laetrile,and paeonol at three time points,and evaluating the releasing synchronization of the three active ingredients based on the similarity factor value simultaneouslyResults The release percent of peoniflorin,laetrile,and paeonol at three time points in Guizhi Fuling double layers sustained-release tablet formula optimized was within criterion(20%F2 h40%,40%F4 h60%,and 75%F10 h95%) and released simultaneously,when 15% for non-soluble layer,22% for soluble layer of HPMCK4M,ane 27% for soluble layer of EC20.There was synchronization in releasing among the three active ingredients.Conclusion The formula optimized could give the satisfactory release of peoniflorin,laetrile,and paeonol.