水溶性β-环糊精与华法林/阿魏酸包合物的制备及抗凝血性质测试和机理分析  

Preparation,Anticoagulant Property Test and Mechanism Discussion of Water Soluble Compound of β-Cyclodextrin with Warfarin/Frulic Acid

作　　者：杨美玲[1,2] 宋玉民[1] 卢小泉[1] 

机构地区：[1]西北师范大学化学化工学院,兰州730070 [2]运城学院应用化学系,运城044000

出　　处：《分析化学》2015年第6期836-842,共7页Chinese Journal of Analytical Chemistry

基　　金：国家自然科学基金(No.21062017);甘肃省生物电化学和环境分析重点实验室资助项目~~

摘　　要：采用研磨法和蒸馏法制备了阿魏酸(Ferulic acid,FA)和华法林(Warfarin,W)与β-环糊精(β-CD)的二元包合物,并采用红外光谱、紫外光谱、差热分析、扫描电镜和X粉末衍射法对其进行了表征,并在生理条件下研究了包合物的抗凝血性质及其与人血清白蛋白(Human serum albumin,HSA)的相互作用。结果表明,包合物的水溶性(包和物的溶解度约为5 g/L,华法林和阿魏酸为难溶物)和抗凝血指标都优于阿魏酸和华法林。与HSA作用的光谱结果表明,包合物可与HSA相互结合,增强了药物的血溶性,通过生成包合物避免了药物阿魏酸被氧化而失去原有的药效作用。说明华法林和阿魏酸经医药载体β-CD包合后水溶性增大,疗效增强,与HSA结合后可以达到药物通过血液输送的目的。Binary compounds of warfarin and ferulic acid with fl-CD were prepared by physical mixing, and co-evaporation method, and characterized by IR, DSC, SEM and X-ray powder diffraction method. Also the anticoagulant properties of these compounds and the binding reaction between this compounds and human serum albumin （HSA） in physiological conditions were studied. The results showed that the title compounds were formed and their water solubility was increased. The anticoagulant experiment presented that the whole blood clotting time （ CT）, recalcification time （ RT）, activated partial thromboplastin time （ AFIT）, etc. of these compounds were all superior to those of warfarin and ferulic acid. Spectrum tests showed that the inclusion compounds could be combined with HSA to enhance the drug solubility in blood and improve the treatment effect, and thus achieve the goal of drug delivery.

关 键 词：华法林 阿魏酸 Β-环糊精 包合物 抗凝血性质 人血清白蛋白 

分 类 号：O657.3[理学—分析化学] TQ460.1[理学—化学]