采用紫外分光光度法和液相色谱法研究β-环糊精衍生物与萘普生的包合作用,考察羟丙基β-环糊精与萘普生包合反应的热力学常数;加入乙醇和改变溶剂的离子强度以进一步对其包合机理进行探讨:用红外光谱法对固体包合物进行表征。研究结果表明:羟丙基β-环糊精和萘普生的包合比为1:1,整个包合反应的热力学常数△G,△H和△S都小于0,说明该过程为自发放热过程;在水溶液中,主体的包合能力较弱;加入乙醇以后表观包结稳定常数降低:溶剂离子强度增加有利于包合反应的发生:萘普生溶解度随pH值增大及羟丙基β-环糊精浓度的增大而增大,但表观稳定常数却随pH值增大而减小:环糊精衍生物对R,S-萘普生外消旋体具有不同的识别能力。
The inclusion stability constants of naproxen(NAP) with β-cyclodextrin derivatives (HPCD, HECD, MECD) in aqueous solution were studied by UV(ultraviolet rays) and HPLC(high performance liquid chromatography). Thermodynamic parameters for the binding of NAP and HPCD were investigated. The effects of alcohol and ionic strength on inclusion behavior were investigated. Stable inclusion complex in solid state was characterized by IR spectra, The results show that host-guest complex with molar ratio of 1:1 is formed. Three hosts all have weak binding ability with NAP in aqueous solution. The solubility of naproxen increases with the increase of pH value and the concentration of HPCD, but the apparent stability constants decrease with the increase ofpH value. AG, AH and AS ate all less than 0, so the inclusion process is a spontaneous and exothermic process. Binding ability of HPCD increases with the increase of ionic strength;β-cyclodextrin derivatives have chiral recognition ability for R- and S-naproxen.