非索伪麻双层缓释片的处方工艺研究及体外释放度考察

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60 g、乳糖60 g、磷酸氢钙30 g、微晶纤维素75 g、交联聚乙烯吡咯烷酮7.5 g,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120 g、山嵛酸甘油酯250 g、磷酸氢钙240 g、以10%乙基纤维素乙醇溶液100 g和1.2 g·mL^-1聚乙二醇6000水溶液15 mL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900 mL为溶剂,转速为每分钟100转,盐酸伪麻黄碱在0.5,2,4,8 h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.