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.
作者
李婷婷
赵乐乐
郑子良
孙艺丹
张淑秋
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)
出处
《精细化工》
EI
CAS
CSCD
北大核心
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)~~
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
entral composite design
response surface methodology
S(+)-ibuprofen
acid-montmorillonite
drug and cosmetic materials