【摘要】 对挤出滚圆法制备缬沙坦速释微丸的成球促进剂进行筛选,并对缬沙坦速释微丸处方进行优化。通过单因素考察评价并比较微晶纤维素(MCC)、低取代羟丙基纤维素(L-HPC)、交联聚维酮(PVPP)、预胶化淀粉(PCS)及k-卡拉胶5种辅料制得的碳酸钙微丸的质量,初步筛选可用的成球促进剂;进一步评价并比较MCC、L-HPC及k-卡拉胶制得的缬沙坦速释微丸的质量,确定k-卡拉胶为制备缬沙坦速释微丸的最佳成球促进剂。采用Box-Behnken响应面法对该缬沙坦速释微丸的处方进行优化,确定最优处方:k-卡拉胶含量16.98 g,HPMC E5含量2.03 g,SLS含量0.26 g,在此条件下制备出的微丸的收率为91.23%,长径比为1.14,预测值与实际值相符。结果表明k-卡拉胶制得的缬沙坦速释微丸圆整度好、收率高、溶出迅速。更多还原

【Abstract】 The aim of the study was to select a suitable pelletisation aid of valsartan immediate-release pellets in the extrusion process and optimized the formulation.The properties of the pellets with five excipients which were microcrystalline cellulose( MCC),low-substituted hydroxypropyl cellulose( L-HPC),crospovidone( PVPP),pregelatinized starch( PCS) and k-carrageenan were evaluated and compared by the single factor test.And the pelletisation aids were chosen preliminary.The properties of the pellets with MCC,L-HPC,k-carrageenan respectively were evaluated and compared and k-carrageenan was determined as the most appropriate pelletisation aid.The Box-Behnken design was employed to optimize the formulation.The optimised formulation was k-carrageenan16.98 g,HPMC-E5 2.03 g,SLS 0.26 g.The yield and aspect ratio of pellets was 91.23% and 1.14,respectively.And there was no significant difference between observed and predictive responses.The results showed k-carrageenan pellets owned properties of a high yield,acceptable sphericity and fast drug release.更多还原