摘要
目的考察富马酸喹硫平缓释片的制备并通过D-混合设计法优化处方。方法采用湿法制粒压片工艺制备盐富马酸喹硫平缓释片,选择处方中HPMC K4M、HPMC K100LV和柠檬酸钠的使用量作为考察因素,以药物在1、6、12、20h时间点的释放度作为评价指标,利用D-混合设计法优化富马酸喹硫平缓释片处方,并比较自制制剂与参比制剂的释放度以及在4种释放介质中释放曲线的相似性。结果富马酸喹硫平缓释片的最优处方组成为:HPMC K4M、HPMC K100LV和柠檬酸钠的用量分别为8.3%、16.7%和15.0%,制备的富马酸喹硫平缓释片释放度符合质量标准,与参比制剂相比在4种释放介质中的相似因子f2分别为77.3、82.6、79.1和77.9。结论利用D-混合设计法优化的富马酸喹硫平缓释片处方体外释放符合质量要求,有望进一步生产放大。
Objective To prepare questiapine fumarate sustained-release tablets,and the optimize the formulation by D-optimal mixture design.Methods Quetiapine fumarate sustained-release tablets were prepared by the wet granulation process.HPMC K4 M,HPMC K100 LV and sodium citrate were selected as independent variables while the accumulative release percentages at 1,6,12 hand 20 hwere dependent variables.The formulation of quetiapine fumarate sustained-release tablets was optimized by D-optimal mixture design.Thein vitrodissolution and the similarity in four types of release media were compared.Results The optimal formulation of quetiapine fumarate sustained-release tablets was as follows：HPMC K4 M,HPMC K100 LV and sodium citrate made up 8.3% ,16.7% and 15.0% ,respectively.The in vitro dissolution of quetiapine fumarate sustained-release tablets was up to the quality standard.The similarity factor f2 of the preparation compared with the reference formulation in the four types of release media was 77.3,82.6,79.1 and 77.9,respectively.Conclusion The quality of quetiapine fumarate sustained-release tablets optimized by D-mixing design can meet requirements,which can facilitate production of such tablets.
出处
《解放军药学学报》
CAS
CSCD
2017年第6期545-549,共5页
Pharmaceutical Journal of Chinese People's Liberation Army
关键词
富马酸喹硫平缓释片
D-混合设计法
释放度
释放曲线
相似因子
quetiapine fumarate sustained-release tablets
D-optimal mixture design
in vitro dissolution
release curve
similarity factor
