星点设计-效应面法优化盐酸苯环壬酯控释片的处方  

The optimization of formulation of phencynonate hydrochloride bi-layer osmotic controlled tablets using central composite design-response surface methodology

作　　者：郭真君 曾媛 张芸 刘辉[1] GUO Zhen-jun;ZHANG Yun;LIU Hui(Department of Pharmacy,Central Theater Command General Hospital of PLA,Hubei Wuhan 430070, China;College of Pharmacy,Hubei University of Chinese Medicine,Hubei Wuhan 430065, China;Department of Pharmacy,The First People's Hospital of Jiangxia District of Wuhan City,Hubei Wuhan 430200, China)

机构地区：[1]中国人民解放军中部战区武汉总医院药剂科,湖北武汉430070 [2]湖北中医药大学药学院,湖北武汉430065 [3]武汉市江夏区第一人民医院药剂科,湖北武汉430200

出　　处：《中国医院药学杂志》2018年第24期2512-2517,共6页Chinese Journal of Hospital Pharmacy

基　　金：国家"十二五";"十三五"重大新药创制科技重大专项经费资助课题(编号:2013ZX09J13109-05C;2018ZX09J18110-002)

摘　　要：目的:采用星点设计-效应面法优化盐酸苯环壬酯控释片处方,制备盐酸苯环壬酯控释片并考察其稳定性。方法:根据单因素实验结果,选择含药层氯化钠含量、助推层高取代聚氧乙烯(WSR-HM)含量和包衣增重为自变量,以12h累积释放度和药物释放曲线拟合度为因变量,应用星点设计-效应面法筛选最佳处方并验证。结果:Quadratic多项式模型为最佳拟合模型,盐酸苯环壬酯控释片的最优处方为:含药层氯化钠含量为5mg/片,助推层高取代聚氧乙烯含量为47.5mg/片,包衣增重为14%。优化制得的3批样品12h平均累积释放度分别为99.89%、98.66%、99.36%,释药曲线线性拟合度R2分别为0.897 1、0.921 0、0.931 9,实测值与预测值无显著差异。稳定性试验表明,该制剂稳定性良好。结论:采用星点设计-效应面法筛选得到的优化处方合理,制得的盐酸苯环壬酯控释片具有显著缓释作用。OBJECTIVE To prepare and optimize the formulation of phencynonate hydrochloride bi-layer osmotic controlled tablets by central composite design-response surface methodology and to investigate its stability.METHODS According to univariate results,the amounts of sodium chloride in the drugcontaining layer,WSR-HM content in the push layer and coating weight were selected as independent variables,12hcumulative release and drug release curve fitting degree as the dependent variables,the optimized prescription was decided and validated by using central composite design-response surface methodology.RESULTS The quadratic polynomial model was the best fitting model.The optimal prescription of phencynonate hydrochloride controlled-release tablets were as follows : 5mg/tablets of NaCl in drug layer,47.5mg/tablets of WSR-HM in push layer,and 14% of coating weight.The 12hcumulative release and fitting degree R 2 of drug releases of imperatorin with opti-mized three batches were 99.89%,98.66%,99.36%and 0.897 1,0.921 0,0.931 9,respectively,with no significant difference between the predicted values.It also showed good stability by stability tests.CONCLUSION A reliable model is estab-lished using response surface methodology and formulation of phencynonate hydrochloride bi-layer osmotic controlled release tablets can be optimized reasonably and effectively.

关 键 词：盐酸苯环壬酯控释片 星点设计-效应面法 稳定性试验 

分 类 号：R927.2[医药卫生—药学]