摘要
目的应用星点设计-效应面法优化尼可地尔脉冲迟释片制剂处方。方法采用干法压制包衣法制备尼可地尔脉冲迟释片,以包衣中羟丙甲基纤维素(HPMC)、乙基纤维素(EC)用量及填充剂比例[(乳糖∶微晶纤维素(MCC)]为自变量,4和5 h累积释药百分率为因变量,计算总评归一值(OD);采用星点设计-效应面法优选制剂处方,并进行处方验证。结果指标与因素之间采用二项式拟合,r2=0.970 1;最优处方为HPMC 88.96 mg、EC 46.21 mg、乳糖与MCC用量比为1.87;实测OD值为0.978 2±0.005 1,与预测值偏差0.43%。结论应用星点设计-效应面法优选出了最佳制剂处方,所建立的数学模型预测性良好;按优化处方制备的尼可地尔脉冲迟释片具有良好的体外释药特性。
Objective To optimize the formulation of controlled-onset extended-release tablets of nicorandilby central composite design-response surface method. Methods The tablets containing nicorandil were prepared bydry-compression coating technique.The influence factors included the amount of HPMC, the amount of EC, and the ratio of lactose/MCC in coating film. The evaluation parameter was Q4 h and Q5 h . The possibly optimal formulation was predicted by response surface method. Results The OD was simulated using second-order polynomial equation and the r2was 0.970 1.Optimal prescription was as follows：HPMC 89.96 mg, EC 46.21 mg, Lactose/MCC 1.87.Bias between the observed and predicted values of the OD was within 0.43%. Conclusion The controlled-onset extended-release tablets of nicorandil can release drug quickly in vitro at the predetermined time.Central composite design-response surface method can be used to optimize the formulation and the model developed in this study was proved highly predictable.
出处
《医药导报》
CAS
2016年第8期867-870,共4页
Herald of Medicine
关键词
尼可地尔
脉冲迟释片
制剂处方
星点设计-效应面法
Nicorandil
Delayed-release tablets
Preparation prescription
Central composite design-response surface method
