星点设计-效应面法优化苯扎贝特渗透泵片处方

Optimization of the Formulation of Bezafibrate Osmotic Pump Tablets by Central Composite Design-response Surface Methodology

目的:制备苯扎贝特渗透泵片,运用星点设计-效应面法优化处方。方法:选择渗透泵片辅料聚氧乙烯(PEO)N80处方用量(A)、Na2CO3用量(B)和包衣增重(C)为考察因素,以该片在1h、6h的累积释药量以及累积释放量对时间进行线性拟合的相关系数为考察指标,采用星点设计-效应面法优化处方,并进行优化处方验证。结果:优化处方为A40mg、B20mg、C29mg,以该优化处方制备的渗透泵片具有较好的释药行为,各指标偏差的绝对值均小于5%。结论:星点设计-效应面法可用于苯扎贝特渗透泵片的处方优化,所建模型具有良好的预测能力。

OBJECTIVE： To prepare bezafibrate osmotic pump tablets（BOPT） and optimize its formulation by central composite design-response surface methodology （CCDRSM）. METHODS： The amount of polyoxyethylene （PEO） N80 which used as an adjuvant of Bezafibrate osmotic pump tablets （A）, the amount of Na2CO3 （B）, and the coating weight increase （C） were used as 3 factors for investigation, and the cumulative release amount at 1 h and 6 h respectively, and the linear correlation coefficient （r） of the cumulative release amount versus time were taken as indexes. The formulation of BOPT was optimized by CCDRSM and the optimized formulation was verified. RESULTS： The optimized formulation obtained was as follows： A 40 mg, B 20 mg, and C 29 mg. The tablets prepared in optimized formulation demonstrated good release behavior, with the absolute value of deviation of each index being less than 5%. CONCLUSION： The CCDRSM can be applied to optimize the formulation of BOPT and the established model is of satisfactory predictive value.