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舒林酸亲水凝胶缓释骨架片释药机制考察

Release mechanism of sulindac from sustained-release hydrogel matrix tablets
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摘要 目的研究舒林酸亲水凝胶缓释骨架片体外释放的影响因素,筛选最优处方。方法以羟丙基甲基纤维素(HPMC)、海藻酸盐为骨架材料,以乳糖、微晶纤维素(MCC)、预胶化淀粉及低取代羟丙基纤维素(L-HPC)为填充剂,采用粉末直接压片、湿法制粒压片制备舒林酸亲水凝胶缓释骨架片;采用浆法测定释放度,考察其释放行为。结果骨架材料的种类、型号及用量对舒林酸释放机制影响较大,填充剂对舒林酸释放有一定影响。结论难溶性药物的骨架与水形成的凝胶层黏度越大,即组成凝胶层的分子链越长,骨架越难以溶蚀,药物的释放越慢。 Objective To investigate factors influencing the in vitro release of sulindac from the hydrogel matrix tablets and optimize the formulation.Method The release behaviors were investigated by choosing HPMC and alginate as matrix materials and lactose,MCC,pregelatinized starch and L-HPC as fillers.The tablets were prepared by either direct compression or wet granulation method.The in vitro release was investigated by the paddle method.Result The sorts,model and amounts of matrix materials had remarkable influence on the release mechanism of sulindac from the matrix tablets,while the influence of the selected fillers was marginal.Conclusion The longer the molecular chain of the matrix materials,the higher the viscosity of the gel layer upon contact with water,which would delay the erosion process and therefore slow down the drug release rate.
出处 《中国药剂学杂志(网络版)》 2008年第5期248-255,共8页 Chinese Journal of Pharmaceutics:Online Edition
关键词 药剂学 缓释骨架片 浆法 舒林酸 羟丙基甲基纤维素 海藻酸盐 pharmaceutics sustained-release tablet paddle method sulindac hydroxypropylmethyhylcellulose(HPMC) alginate
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