非索伪麻双层缓释片的处方工艺研究及体外释放度考察  

Study on optimization of preparation technology and in vitro dissolution rate of fexofenadine/pseudoephedrine extended-release tablets

作　　者：吴亚利[1] 毛士龙[1] 苗积康[1] 计英[1] 季爱玲[1] 朱建民[1] 

机构地区：[1]上海市徐汇区中心医院,上海200031

出　　处：《药物分析杂志》2010年第8期1472-1476,共5页Chinese Journal of Pharmaceutical Analysis

摘　　要：目的:研究非索伪麻双层缓释片的制备方法,筛选出最佳处方制备工艺条件。方法:采用正交设计对缓释部分的处方进行优化,确定出最佳制备处方工艺,并对优化的试验结果进行了验证,同时考察了缓释部分体外的释放度效果。结果:速释层最佳处方为盐酸非索非那定60g、乳糖60g、磷酸氢钙30g、微晶纤维素75g、交联聚乙烯吡咯烷酮7.5g,2%淀粉浆制软材,70℃干燥整粒,按干颗粒重量0.5%的硬脂酸镁混合均匀即得;缓释层最佳处方为盐酸伪麻黄碱120g、山嵛酸甘油酯250g、磷酸氢钙240g、以10%乙基纤维素乙醇溶液100g和1.2g·mL-1聚乙二醇6000水溶液15mL混合液制软材,50℃干燥整粒,加入干颗粒重量0.5%的硬脂酸镁混合均匀即得,双层压片制得1000片;所制备的样品采用溶出度测定第2法的装置,以水900mL为溶剂,转速为每分钟100转,盐酸伪麻黄碱在0.5,2,4,8h的体外累积释放度分别为24.87%,49.47%,65.09%,98.34%。结论:制备的非索伪麻双层缓释片的体外累积释放率好,工艺重现性好。Objective：To study the preparation method of fexofenadine/pseudoephedrine extended-release tablets and to optimize the formulation of these preparations.Methods：The preparation technology conditions were optimized by orthogonal design.The in vitro accumulated drug release of the pseudoephedrine hydrochloride were examined.Results：The optimized preparation technology condition of rapid release layer was as follows：fexofenadine hydrochloride 60 g,lactose 60 g,dibasic calcium phosphate 30 g,microcrystalline cellulose 75 g,crosslinked polyvinylpyrrolidone 7.5 g,2% starch paste,0.5% magnesium stearate.The optimized preparation technology condition of extend layer was as follows：the amounts of pseudoephedrine hydrochloride,glyceryl behenate,dibasic calcium phosphate,10% ethyl cellulose ethanol solution and 1.2 g·mL-1 PEG 6000 solution were 120 g,250 g,240 g,100 g,15 mL,respectively;and pseudoephedrine hydrochloride in vitro release rates at 0.5,2,4 and 8 h were 24.87%,49.47%,65.09%,98.34%.Conclusion：The preparation technology is reproducible,and the in vitro accumulated drug release is in conformity with the requirements.

关 键 词：非索伪麻 双层缓释片 正交试验设计 制备工艺 体外累积释放度 

分 类 号：R917[医药卫生—药物分析学]