静电力对诺氟沙星与磺丁基醚-β-环糊精包合作用的影响  

Effect of electrostatic force on the complexation of ionized cyclodextrins with dissociated drugs in aqueous solution

作　　者：谷福根[1] 郝朵[2] 孟根达来[1] 王毅[1] 吴春芝[1] 李文妍[2] 

机构地区：[1]内蒙古医学院附属医院,内蒙古呼和浩特010059 [2]内蒙古医学院药学院,内蒙古呼和浩特010059

出　　处：《中国医院药学杂志》2011年第7期540-543,共4页Chinese Journal of Hospital Pharmacy

基　　金：内蒙古自然科学基金资助课题(编号:2009MS1202)

摘　　要：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。OBJECflVE To investigate the effect of electrostatic force on the complexation of ionized cyclodextrins with dissociated drugs in aqueous solution and further explore the complexing mechanism. METHODS Norfloxacin （NFX） was uesd as a model drug, and SBE-β-CD as a complexing material. The UV spectra of NFX, phase solubility diagrams, complex stability constants （Ka） and thermodynamic parameters for the drug complexation with SBE-β-CD in aqueous solutions were determined and compared under acid, neutral and alkaline pHs, respectively. RESULTS The UV spectra of NFX, phase solubility diagrams, Ka were obvious different at above three different pHs, but the thermodynamic parameter values for the complexation process such as △G, △H and △S were all negative, indicating that the mechanisms for the complexation process of com- plexation seemed to be unchanged. CONCLUSION For the charged cyclodextrin and ionized drugs, electrostatic effect is one of main host-guest molecular forces and the media pH will exert an imprtant influence on the complexation process.

关 键 词：诺氟沙星 SBE-β-CD 静电作用 KA 热力学参数 包合机制 

分 类 号：R943[医药卫生—药剂学]