应用十六醇与HPMC制备双氯芬酸钠缓释片的研究

摘要

目的：制备双氯芬酸钠混合骨架缓释片。方法采用不同用量和比例的的十六醇和HPMC制备双氯芬酸钠缓释片，根据参比制剂的体外释放情况筛选出最优处方；考察不同干燥温度，不同压片压力对缓释骨架片体外释放的影响。引入逾渗阈值的概念，估算混合骨架片中HPMC的逾渗阈值。结果和结论联合使用一定比例的十六醇和HPMCK4M的骨架片可以有效控制药物的缓慢释放；较低的干燥温度得到的骨架片释药变快；在一定范围内，压片压力越大，骨架片的药物释放越慢。混合缓释片中HPMC逾渗阈值在4％左右。%ABSTRACT:OBJECTIVE To prepare diclofenac sodium sustained-release tablets.METHODS Different a-mount and ratio of cetyl alcohol and HPMC were adopted as mixed matrix to make diclofenac sodium sustained-re-lease tablets.The formulation was optimized comparing with the release profiles in vitro of commercial products.The effect of drying temperature of wet granues and compression force on in vitro release of diclofenac sodium from the matrix tablets was investigated.Percolation theory had been applied to estimate the hypromellose ( HPMC) percola-tion thresholds in diclofenac sodium matrix formulations.RESULTS and CONCLUSION The results showed that the slow release of diclofenac sodium can be obtained from mixed matrix tablets with certain amount and ratio of cetyl alcohol and HPMCK4M.A lower drying temperature and smaller compression force accelerated the release of mixed matrix tablets.It has been found that the percolation threshold for HPMC in diclofenac sodium matrix formulations is about 4%.