相溶解度法研究不同环糊精对淫羊藿苷的增溶作用  

Study on Solubilization of Different Types of Cyclodextrin for Icariin by Phase Solubility Method

作　　者：王娜[1] 张抗怀[1] 毛文彬 王海涛[1] 杨鑫[1] Wang Na;Zhang Kanghuai;Mao Wenbin;Wang Haitao;Yang Xin(Department of Pharmacy,the Second Affiliated Hospital,Xi’an Jiaotong University,Xi’an 710004,China)

机构地区：[1]西安交通大学第二附属医院药学部,西安710004

出　　处：《中国药师》2020年第2期260-263,共4页China Pharmacist

基　　金：陕西省重点研发计划(编号:2017SF-302)。

摘　　要：目的:研究β-环糊精(β-CD)、羟丙基-β-环糊精(HP-β-CD)、甲基化-β-环糊精(RM-β-CD)、γ-环糊精(γ-CD)对淫羊藿苷的包合行为和增溶效果,为其包合物的制备提供理论依据。方法:采用相溶解度法分别研究不同浓度和不同温度下β-CD、HP-β-CD、RM-β-CD、γ-CD对淫羊藿苷的增溶作用,绘制相溶解度曲线,计算表观结合常数。结果:淫羊藿苷在四种环糊精中的相溶解度曲线均为AL型,淫羊藿苷与四种环糊精均以1∶1的比例包合。25℃时,淫羊藿苷与β-CD、HP-β-CD、RM-β-CD、γ-CD的表观结合常数为分别为33.32,52.01,36.05,和55.69 L·mmol^-1。结论:四种环糊精对淫羊藿苷均有一定程度的增溶作用,同一温度条件下,增溶作用的顺序为γ-CD>RM-β-CD>HP-β-CD>β-CD,温度对β-CD、HP-β-CD与淫羊藿苷的包合影响不大,但对RM-β-CD、γ-CD与淫羊藿苷的包合有所影响。Objective:To study the inclusion behavior and solubilization ofβ-cyclodextrin(β-CD),hydroxylpropyl-β-cyclodextrin(HP-β-CD),methylated-β-cyclodextrin(RM-β-CD)andγ-cyclodextrin(γ-CD)for icariin to provide the theoretical basis for the preparation of inclusion compounds.Methods:The solubilization ofβ-CD,HP-β-CD,RM-β-CD andγ-CD at different concentrations for icariin was studied by phase solubility method at various temperatures.The solubility curves were plotted and the apparent binding constants were calculated.Results:The phase solubility curves of icariin with the four cyclodextrins were both ALstyles,and the inclusion ratios of icariin versus the four cyclodextrins were all 1∶1.The apparent binding constant of icariin andβ-CD,HP-β-CD,RM-β-CD orγ-CD at 25℃was 33.32,52.01,36.05 and 55.69 L·mmol^-1,respectively.Conclusion:β-CD,HP-β-CD,RM-β-CD andγ-CD all show certain solubilization for icariin.The sequence of solubilization isγ-CD>RM-β-CD>HP-β-CD>β-CD at the same temperature.Temperature shows mild effect on the inclusion ofβ-CD and HP-β-CD for icariiin,while has obvious effect on the inclusion of RM-β-CD andγ-CD for icariin.

关 键 词：淫羊藿苷 环糊精 相溶解度法 增溶作用 

分 类 号：R944.9[医药卫生—药剂学]