茴三硫-2-羟丙基-β-环糊精包合物制备工艺的研究

Complexation of anethol trithione with 2-hydroxypropyl-β-cyclodextrin

目的:研究茴三硫-2-羟丙基-β-环糊精(2-Hydroxypropyl-β-cyclodestrin,2-HP-β-CD)包合物制备工艺及2-HP-β-CD对茴三硫的增溶作用。方法:在单因数试验基础上,采用正交试验优化法,以包合率为指标,考察主客分子摩尔比、搅拌速度和搅拌时间等因素对制备包合物的影响;运用热分析法测定包合物中药物的溶解度并对包合物进行验证。结果:结果表明茴三硫-2-羟丙基-β-环糊精包合物对茴三硫具有明显的增溶作用。结论:经过包合后茴三硫包合物的溶解度是原料药460倍。

Objective：To study the solubilization effect of 2-hydroxypropyl-β-cyclodextrin（2-HP-β-CD） on anethol trithione and the complexation of anethol trithione with 2-HP-β-CD.Methods：On the basis of single factor experiment,the drug complexed rate was adopted as the index,to study the effects of factors like host-guest molar ratio,alcohol concentration,stiring rate and stiring time on the techniques of preparing anethol trithione-2-HP-β-CD;the inclusion complex was identificated and solubility was detected by diferential scanning calorimeter （DSC） methods. Results：2-HP-β-CD can obviously enhance solubility of anethol trithione. Conclusion： The solubility of inclusion complex increased by 460 times when it was included by 2-HP- β -CD.