苯丙醇/β-环糊精包合作用研究  

Study on the Inclusion of Phenylpropanol/β-cyclodextrin

作　　者：王亚娜[1] 任勇[1] 陆亚鹏[1] 杨星昊[1] 涂荣华 周灿 付毅刚 

机构地区：[1]南京师范大学新药研究中心,南京210097 [2]宜昌人福药业有限公司,宜昌443001

出　　处：《中国药科大学学报》2005年第1期13-17,共5页Journal of China Pharmaceutical University

基　　金：国家自然科学基金资助项目 (No 3 0 3 71690)~~

摘　　要：目的 :研究苯丙醇与 β- 环糊精包合作用 ,探讨乙醇和硬脂酸镁对其包合作用的影响 ,为改进苯丙醇药物剂型提供理论基础。方法 :紫外分光光度法测定苯丙醇 / β- 环糊精包合常数及乙醇、硬脂酸镁对其包合常数的影响 ;沉淀法制备包合物 ;1HNMR法验证包合物以及乙醇、硬脂酸镁对包合的影响。结果 :中性条件下 ,苯丙醇 / β- 环糊精的包合常数为 1772M-1(2 5 1nm) ,加入微量乙醇或硬脂酸镁后 ,其包合常数分别降为 791M-1,12 2 5M-1(2 5 1nm) ;增加乙醇和硬脂酸镁浓度后 ,包合常数又分别降为 377M-1、774M-1(2 5 1nm) ;1HNMR图谱显示苯丙醇与 β- 环糊精形成了 1∶1二元包合物 ,乙醇、硬脂酸镁分别与苯丙醇 / β- 环糊精形成了三元包合物。 结论 :β- 环糊精技术可改进苯丙醇药物的剂型 ;乙醇和硬脂酸镁可降低 β 环糊精对苯丙醇的包合作用 ,故制备包合物时不宜用乙醇助溶或添加硬脂酸镁。AIM:To provide theoretical foundations for improvement on the dosage form of phenylpropanol by studying the inclusion of phenylpropanol/β-CD and the influence of ethanol and magnesium stearate on it.METHOD: The equilibrium constants of phenylpropanol/β-CD in the absence or presence of ethanol or magnesium stearate were determined by UV spectrophotometry.The inclusion complexes were prepared by precipitation method and their structures were identified by 1H NMR.The effect of ethanol and magnesium stearate on the preparation of inclusion complex was testified by 1H NMR.RESULT: In neutral solution and in the presence of ethanol or magnesium stearate,the equilibrium constant of phenylpropanol/β-CD reduced from 1 772 M -1 to 791 M -1 or 1 225 M -1.By increasing the concentration of ethanol or magnesium stearate,it reduced to 377 M -1 or 774 M -1 gradually. 1H NMR spectrum showed that a ternary complex among β-CD,phenylpropanol and ethanol or magnesium stearate was formed.CONCLUSION: In neutral conditions,phenylpropanol can be well included by β-CD.Ethanol or magnesium stearate can affect the inclusion action between phenylpropanol and β-CD by forming a ternary complex with β-CD and phenylpropanol.

关 键 词：苯丙醇 环糊精 平衡常数 三元包合 

分 类 号：R944[医药卫生—药剂学]