应用核磁共振技术研究盐酸非索非那定与β-环糊精包合的相互作用

The Interaction Study of the Inclusion of Fexofenadine with β-Cyclodextrin by NMR

摘要: 目的：研究溶液状态下盐酸非索非那定(FFD)与β-环糊精相互作用过程以及包合物立体构型。方法：应用核磁共振(NMR)技术如1D-NMR和2D-ROESY的方法研究了盐酸非索非那定(FFD)与β-环糊精在水溶液中的包合过程以及包合物的立体结构。结论：根据FFD/β-CD不同比例包合物¹H-NMR中化学位移的变化以及2D-ROESY，可以判定，盐酸非索菲那定与β-环糊精发生了包合，而且当比例为1:1时，主要是单取代苯环进入β-CD空腔内，而且是从β-CD的宽口进入。

Abstract: Objects: To study the interaction between Fexofenadine and β-cyclodextrin and the geometry structure of the complexation in solution. Methods: The interaction study of the inclusion between fexofenadine and β-cyclodextrin in aqueous solution was attempted by ¹H-NMR and 2D-ROESY. Conclusion: The results of ¹H-NMR of chemical shift changes and 2D-ROESY in different proportion complexation suggest that there was interaction between FFD and β-CD, and when the molar ratio of fexofenadine to β-cyclodextrin is one, the p-phenyl ring of fexofenadine is predominantly included within β-cyclodextrin cavity, which penetrates deep from the wider rim.