羟丙基-β-环糊精对高乌甲素的包合作用及其热力学稳定性  

Study on inclusion complex of hydroxypropyl-β-cyclodextrin with lappaconitine and its thermodynamic stability

作　　者：马君义[1,2] 张继[1,2] 李佳佳[1] 邢润苗[1] 黄玉龙[1] 

机构地区：[1]西北师范大学生命科学学院,甘肃兰州730070 [2]甘肃特色植物有效成分制品工程技术研究中心,甘肃兰州730070

出　　处：《西北师范大学学报（自然科学版）》2012年第4期66-70,共5页Journal of Northwest Normal University(Natural Science)

基　　金：西北师范大学教学研究项目(2008045B);西北师范大学大学生学术科研资助金资助项目(2010-083)

摘　　要：运用平衡相溶解度法和双倒数作图法考察不同温度、不同pH条件下羟丙基-β-环糊精(HP-β-CD)对高乌甲素(LA)的包合作用、包合摩尔比、表观稳定常数以及包合过程中的热力学参数.结果表明,在研究温度、pH和浓度范围内,LA与HP-β-CD可形成摩尔比为1∶1的包合物,平衡相溶解度图为AL型,且在弱碱性包合条件下其表观稳定常数和增溶能力较大,分别为46.28L.mol-1和3.61倍.HP-β-CD对LA的包合作用是一个吸热过程和熵驱动过程,适当升高温度有利于包合物的形成和稳定性的提高.HP-β-CD对难溶性药物LA具有明显的增溶作用.The equilibrium phase solubility and double reciprocal plot method were used to investigate the inclusion complex of hydroxypropyl-β-cyclodextrin（HP-β-CD） with lappaconitine（LA） under different temperature and pH.The molar ratio between HP-β-CD and LA,the apparent stability constants and thermodynamic constants of the inclusion complex were also studied simultaneously.The results showed that HP-β-CD can react with LA forming a 1∶1 host-guest complex under the given temperature,pH and concentration.The equilibrium phase solubility diagram were AL type.The apparent stability constants was 46.28 L·mol-1 and the solubilization capacity was 3.61 respectively.The inclusion procedure of HP-β-CD with LA was controlled mainly by endothermic process and driven by entropy.The formation and stability of the inclusion complex could be improved by rising the inclusion temperature appropriately.The solubility of LA is significantly increased by inclusion complex with HP-β-CD.

关 键 词：羟丙基-Β-环糊精 高乌甲素 包合物 热力学稳定性 

分 类 号：R284.4[医药卫生—中药学] R943.4[医药卫生—中医学]