星点设计-效应面法优化制备右旋布洛芬/酸改性蒙脱土  

Optimization of Preparation of S(+)-Ibuprofen/Acid-Montmorillonite Dry Suspension by Central Composite Design-Response Surface Methodology

作　　者：李婷婷[1] 赵乐乐[1] 郑子良 孙艺丹[1] 张淑秋[1] LI Ting-ting;ZHAO Le-le;ZHENG Zi-liang;SUN Yi-dan;ZHANG Shu-qiu(College of Pharmacy,Shanxi Medical University,Taiyuan 030001,Shanxi,China;Translational Medicine Research Center,Shanxi Medical University,Taiyuan 030001,Shanxi,China)

机构地区：[1]山西医科大学药学院,山西太原030001 [2]山西医科大学转化医学研究中心,山西太原030001

出　　处：《精细化工》2018年第10期1702-1706,1718,共6页Fine Chemicals

基　　金：国家自然科学基金(81571747);山西省青年科技研究基金(201601D202105);山西医科大学校博士启动基金(03201529);山西医科大学青年基金(02201618)~~

摘　　要：以右旋布洛芬为原料,酸化蒙脱土为药物载体,制得右旋布洛芬/酸改性蒙脱土S（＋）-IBU/acid-MMT干混悬剂。通过星点设计-效应面法优化右旋布洛芬/酸改性蒙脱土干混悬剂的制备工艺。以蒙脱土的载药量为考察指标,采用三因素五水平星点设计考察了盐酸浓度、酸化时间、酸化温度对干混悬剂制备工艺的影响,并对结果进行了二元多项式线性回归方程拟合,经效应面法预测最佳处方;借助XRD和SEM技术对干混悬剂进行了结构表征。结果表明,右旋布洛芬/酸改性蒙脱土干混悬剂最佳制备条件为：盐酸浓度3.3 mol/L,酸化时间5.2 h,酸化温度54℃,在该条件下,干混悬剂载药量可达443.7 mg/g,较优化前（352.4 mg/g）提高了25.9%。星点设计-效应面法适用于右旋布洛芬/酸改性蒙脱土干混悬剂制备工艺优化,以该方法建立的数学模型具有良好的预测性,所得干混悬剂具有更高的载药量。The acid-montmorillonite（acid-MMT） was used as the carrier of S（＋）-ibuprofen（IBU） to produce S（＋）-IBU/acid-MMT dry suspension. The preparation process of S（＋）-IBU/acid-MMT dry suspension was optimized by central composites design-response surface methodology. Using drug loading as indexes, a three-factor and five-level central composite design was employed to investigate three factors affecting S（＋）-IBU/acid-MMT dry suspension preparation including hydrochloric acid concentration, acidification time and acidification temperature. The results were fitted by second-order polynomial equation, and the optimal formulation was predicted by response surface methodology. The prepared S（＋）-IBU/acid-MMT dry suspension were characterized by XRD and SEM. The optimum preparation conditions of S（＋）-IBU/acid-MMT dry suspension were obtained as follows： hydrochloric acid concentration 3.3 mol/L, acidification time 5.2 h and acidification temperature 54 ℃. The loading capacity under this kind of optimization condition was 443.7 mg/g, which was 25.9% higher than 352.4 mg/g before optimization. The central composite design-response surface methodology is suitable for the optimization of preparation process of S（＋）-IBU/acid-MMT dry suspension, and the mathematical model established by this method has good predictability. Moreover, the obtained dry suspension has a higher loading capacity.

关 键 词：星点设计 效应面法 右旋布洛芬 酸化蒙脱土 医药与日化原料 

分 类 号：O611.4[理学—无机化学]