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目的:研究主、客分子间静电力对离子型环糊精与解离型药物间包合作用的影响并探讨包合机制。方法:以诺氟沙星(norfloxacin,NFX)作为模型药物,磺丁基醚-β-环糊精(SBE--βCD)作为包合材料,分别在酸、碱及中性3种环境下,研究SBE--βCD对NFX紫外吸收光谱(UV)的影响,并测定SBE--βCD对NFX增溶作用的相溶解度图、包合物稳定常数(Ka)以及包合过程热力学参数。结果:在上述3种环境下,SBE--βCD对NFX的UV图谱的影响不同,相溶解度图、包合物Ka值也有差异,但包合作用热力学机制相同,表现为吉布斯自由能变化(△G)、焓变(△H)和熵变(△S)均为负值。结论:静电力对离子型环糊精与解离型药物间的包合过程具有重要影响。
Objective: To study the effect of electrostatic force between host and guest on the inclusion of cyclodextrins and dissociative drugs, and to explore the inclusion mechanism. Methods: Norfloxacin (NFX) was used as a model drug and sulfobutyl ether - β - cyclodextrin (SBE - βCD) was used as the inclusion compound in acid, alkali and neutral pH respectively. The effects of SBE - βCD on NFX UV absorption spectra were investigated. The phase solubility diagrams of SBE - βCD for NFX solubilization, the stability of inclusion complex (Ka) and the thermodynamic parameters of the inclusion process were also studied. Results: Under the above three conditions, the influence of SBE - βCD on the UV spectrum of NFX was different, and the phase solubility diagrams and inclusion Ka values were also different. However, the thermodynamic mechanism of inclusion was the same, showing the change of Gibbs free energy (△ G), enthalpy change (△ H) and entropy change (△ S) are negative. Conclusion: Electrostatic force has an important influence on the inclusion process between ionic cyclodextrins and dissociative drugs.