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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

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【作者】 王娜张抗怀毛文彬王海涛杨鑫

【Author】 Wang Na;Zhang Kanghuai;Mao Wenbin;Wang Haitao;Yang Xin;Department of Pharmacy,the Second Affiliated Hospital,Xi’an Jiaotong University;

【通讯作者】 王娜;

【机构】 西安交通大学第二附属医院药学部

【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。

【Abstract】 Objective: To study the inclusion behavior and solubilization of β-cyclodextrin( β-CD),hydroxylpropyl-β-cyclodextrin( HP-β-CD),methylated-β-cyclodextrin( RM-β-CD) and γ-cyclodextrin( γ-CD) for icariin to provide the theoretical basis for the preparation of inclusion compounds. Methods: The solubilization of β-CD,HP-β-CD,RM-β-CD and γ-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 and β-CD,HP-β-CD,RM-β-CD or γ-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 and γ-CD all show certain solubilization for icariin. The sequence of solubilization is γ-CD>RM-β-CD>HP-β-CD>β-CD at the same temperature. Temperature shows mild effect on the inclusion of β-CD and HP-β-CD for icariiin,while has obvious effect on the inclusion of RM-β-CD and γ-CD for icariin.

【基金】 陕西省重点研发计划(编号:2017SF-302)
  • 【分类号】R283.6
  • 【下载频次】404
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