山奈酚羟丙基-β-环糊精包合物热力学及抗氧化能力

Properties of thermodynamics and antioxidant of Kaempferol inclusion complex with hydroxypropyl-β-cyclodextrin

相溶解度法考察羟丙基-β-环糊精对山奈酚的增溶作用和包合过程中的热力学参数变化规律,并考察其对1,1-二苯基-2-苦基肼自由基(DPPH·)清除力的抗氧化活性。结果表明,山奈酚羟丙基-β-环糊精包合物的相溶解度曲线为AL型,以n(山奈酚)∶n(羟丙基-β-环糊精)=1∶1形成包合物;t=45℃时,c(羟丙基-β-环糊精)=0~10 mmol/L,山奈酚溶解度可增大6.9倍,与25℃山奈酚在水中的饱和溶解度相比增大了20.6倍;包合过程的ΔH>0、ΔS>0、ΔG<0,升高温度有利于山奈酚与羟丙基-β-环糊精的包合,随着温度的升高,包合常数K不断增大,药物与环糊精之间的范德华力和氢键也发挥一定的作用。

Phase solubility method was used to investigate the solubilization of kaempferol by hydroxypropyl-β-cyclodextrin(HP-β-CD)and the change of thermodynamic parameters during the inclusion process.The antioxidant activity of HP-β-CD on DPPH radical scavenging was also investigated.The results showed that the solubility curve of kaempferol hydroxypropyl-β-cyclodextrin phase was AL type,and hydroxypropyl-β-cyclodextrin and kaempferol formed the aqueous soluble complexes with 1∶1 molar ratio.At 45℃,when the concentration of hydroxypropyl-β-cyclodextrin was in the range of 0~10 mmol/L,the solubility of kaempferol increased by 6.9 times,which was 20.6 times higher than that of kaempferol at 25℃ in water.The inclusion process ΔH>0,ΔS>0,ΔG<0,increasing temperature is beneficial to the inclusion of kaempferol and hydroxypropyl-β-cyclodextrin.With the increase of temperature,the inclusion constant K increases,van der Waals force and hydrogen bond between drugs and cyclodextrin also play a certain role.