相溶解度法研究两种不同类型环糊精对吲达帕胺的包合作用

目的:研究两种不同类型环糊精羟丙基-β-环糊精(HP-β-CD)、γ-环糊精(γ-CD)对吲达帕胺的包合增溶作用,并进行包合物的鉴定.方法:运用相溶解度法考察不同类型环糊精对药物的增溶作用,并用差示扫描量热(DSC)法和红外光谱(IR)法对包合物进行鉴定.结果:确定了吲达帕胺与HP-β-CD和γ-CD包合物的相溶解度图,并计算了表观稳定常数,用DSC法和IR法确证2种不同类型环糊精的包合物均已形成.结论:2种不同类型环糊精对吲达帕胺都有显著的增溶作用,且都能形成包结比为1:1的包合物,γ-CD的增溶作用更强,形成的包合物更稳定.

Study on Two Indapamide-loaded Cyclodextrin Inclusion Complexes by Phase Solubility Method

Objective： To investigate the solubilization effect of hydroxypropyl-β-cyclodextrin（HP-β-CD） and γ-cyclodextrin（γ-CD） on indapamide and identify the inclusion compounds.Method： The solubility of inclusion compounds were evaluated by phase solubility method.The inclusion compounds were identified by differential scanning calorimetry（DSC） and infrared spectroscopy（IR）.Result： The phase-solubility diagrams of indapamide/HP-β-CD and indapamide/γ-CD inclusion compounds were drawn and the stability constants were calculated.The results of DSC and IR showed the inclusion compounds were prepared successfully.Conclusion： Both the cyclodextrins have significant solubilization effect on indapamide and can form inclusion compounds at the formation ratio of 1∶ 1.The solubilization effect of γ-CD is better and the inclusion compounds are more stable.