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第 35 卷第 10 期 精 细 化 工 Vol.35, No.10
2018 年 10 月 FINE CHEMICALS Oct. 2018

医药与日化原料
星点设计-效应面法优化制备右旋布洛芬/

酸改性蒙脱土

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李婷婷 ，赵乐乐 ，郑子良 ，孙艺丹 ，张淑秋
（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）
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。
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
中图分类号：O611.4 文献标识码：A 文章编号：1003-5214 (2018) 10-1702-06

Optimization of Preparation of S(+)-Ibuprofen/Acid-Montmorillonite Dry

Suspension by Central Composite Design-Response Surface Methodology

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LI Ting-ting , ZHAO Le-le , ZHENG Zi-liang , SUN Yi-dan , ZHANG Shu-qiu
（1. College of Pharmacy, Shanxi Medical University, Taiyuan 030001, Shanxi, China; 2. Translational Medicine
Research Center, Shanxi Medical University, Taiyuan 030001, Shanxi, China）
Abstract: 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.
Key words: central composite design; response surface methodology; S(+)-ibuprofen; acid-montmorillonite;
drug and cosmetic materials

收稿日期：2017-05-15; 定用日期：2018-02-12; DOI: 10.13550/j.jxhg.20170407
基金项目：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）
作者简介：李婷婷（1984—），女，讲师，博士，E-mail：lily8631@163.com。联系人：张淑秋（1962—），女，教授，博士生导师，
E-mail：shuqiu.zhang@126.com。