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双硫仑-羟丙基-β-环糊精包合常数测定与包合物形成的热力学性质考察

Studies on equilibrium constants of DSF-β-CDHP inclusion complexes and thermodynamic properties

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【作者】 于凤波费学萍李德馨苏德森王思玲

【Author】 YU Feng-bo~1,FEI Xue-ping~2,LI De-xin~1,SU De-sen~1,WANG Si-ling~1(1.School of Pharmacy,Shenyang Pharmaceutical University,Shenyang 110016,China;2.Nursing Department of the Fourth Hospital,China Medical University,Shenyang 110016,China)

【机构】 沈阳药科大学药学院中国医科大学附属第四医院沈阳药科大学药学院 辽宁沈阳110016辽宁沈阳110032辽宁沈阳110016

【摘要】 目的测定双硫仑羟丙基β环糊精(DSFβCDHP)的包合常数;研究包合物形成的热力学性质。方法采用RP HPLC法。测定溶液中双硫仑含量,由测定结果计算各浓度的βCDHP溶液中双硫仑的溶解度,以双硫仑溶解度对βCDHP浓度作图,得到相溶解度图;测定不同色谱条件下双硫仑羟丙基β环糊精的保留时间,根据保留时间计算稳定常数及不同温度下的包合常数K。结果当羟丙基β环糊精浓度较低时,可形成1∶1包合物;30℃时DSFβCDHP的包合常数为1 624.41 L.mol-1;其包合反应的焓变(ΔH)为-25.25 kJ.mol-1,吉布斯自由能(ΔG)和熵变(ΔS)分别为-12.60 kJ.mol-1与-41.74 J.mol-1K-1。结论双硫仑与羟丙基β环糊精的包合作用为一放热过程,是分子间氢键和范德华力作用的结果;采用较低的温度有利于双硫仑完全形成包合物。

【Abstract】 Objective To study the thermodynamic properties of disulfiram-hydroxypropyl-β-cyclodextrin(DSF-β-CDHP) inclusion complexes and determine the equilibrium constants of the inclusion complex.Methods The reverse-phase high performance liquid chromatogram was employed to determine the retention times of DSF-β-CDHP under different conditions,then the equilibrium constants and thermodynamic parameters were calculated.Results The inclusion complexes containing equimolar disulfiram(DSF) and hydroxypropyl-β-cyclodextrin(β-CDHP) were formed when the concentration of β-CDHP was low.The equilibrium constant of inclusion complexes was confirmed to be 1 624.41 L·mol-1 at 30 ℃ through the way of RP-HPLC.The changes of enthalpy(ΔH0),Gibbs’ free energy(ΔG0) and entropy(ΔS0) of the system during the formation of DSFβ-CDHP were-25.25 kJ·mol-1,(-12.60 kJ·mol-1) and41.74 J·mol-1K-1 respectively.Conclusions The negative free energy change of this reaction demonstrate the spontaneous formation of DSF-β-CDHP,which caused by the intermolecular hydrogen bond and Van der Waals forces.The low temperature is useful for the formation of inclusion complexes.

  • 【文献出处】 沈阳药科大学学报 ,Journal of Shenyang Pharmaceutical University , 编辑部邮箱 ,2006年10期
  • 【分类号】TQ460.1
  • 【被引频次】4
  • 【下载频次】368
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