摘要
目的采用中心复合设计-效应面法优化非洛地平缓释片处方。方法以羟丙甲基纤维素(HPMC)K4M和HPMC 100LV的用量为考察因素,以1,4,8 h的累积释放度(Y1h、Y4h、Y8h)为考察指标,利用二因素三水平中心复合设计-效应面法优化处方,并采用f2相似因子对自制片剂和原研制剂的体外释放度进行比较。结果 HPMC K4M和HPMC100LV的用量各占片剂质量的20.0%和10.0%时,所得缓释片各时间点释放度符合标准;自制片剂和原研制剂在不同释放介质中的释放度相似因子f2分别为70.87,74.19,59.68,69.25。结论 HPMC K4M和HPMC 100LV以一定比例联合使用可以有效控制药物释放,采用中心复合设计-效应面法优化的处方预测性良好,制得的非洛地平缓释片体外释放符合要求。
Objective The purpose of this study was to optimize the formulation of the felodipine extended-release tablets.Methods The felodipine extended-release tablets were prepared by employing the mixture of hydroxypropyl methylcellulose（HPMC） K4M and HPMC 100LV as the basic matrix materials.Factors that affected drug release were investigated.Thereafter,a central composite design-response surface methodology（CCD-RSM） was applied to optimize the formulation of the felodipine extended-release tablets.The release rate of the extended-release tablets and control tablets were compared by a similarity factor（f2 value）.Results The optimized formulation contained 20.0% of HPMC K4M and 10.0% of HPMC 100LV of the total weight and accumulative release percentages at 1,4,8 h were consistent with the criteria,which was 5%~30%,45%~70%,no less than 80%,respectively.The f2 for the extended-release tablets and control tablets in different solvents were 70.87,74.19,59.68,69.25.Conclusion Combing HPMC K4M and HPMC 100LV at a certain rate can effectively control drug release and the central composite design-response surface methodology is successfully used to optimize the formulation of felodipine extended-release tablets,which complying with requirements of the USP.
出处
《医药导报》
CAS
北大核心
2012年第11期1477-1480,共4页
Herald of Medicine
关键词
非洛地平
缓释片
羟丙甲基纤维素
中心复合设计-效应面法
Felodipine
Extended-release tablets
HPMC
Central composite design-response surface mexthodology
