七元、八元瓜环对左羟丙哌嗪的包合作用及pH敏感释药性能  

Interaction of Cucurbit[n=7,8]urils with Levodropropizine and Their pH Sensitive Drug Slow Release Properties

作　　者：方权辉 曹德桢 林友文[1] 

机构地区：[1]福建医科大学药学院,福建福州350004

出　　处：《化学世界》2016年第11期693-698,共6页Chemical World

基　　金：福建省自然科学基金计划项目(2011J01289)

摘　　要：利用紫外光谱、荧光光谱、1 H NMR等技术研究七元瓜环（Q[7]）、八元瓜环（Q[8]）与左羟丙哌嗪（LDP）的主-客体包合作用。测定了Q[7]-LDP、Q[8]-LDP的包合作用pH敏感性、包合比、包合稳定常数及包合物的体外药物累积释放度。发现Q[7]-LDP、Q[8]-LDP体系的超分子包合作用均具有pH敏感性,包合比均为1∶1,Q[7]-LDP和Q[8]-LDP的包合平衡常数分别为3.7×10^3和3.8×10^3 L/mol,Q[7]及Q[8]的包合对LDP有明显的pH敏感性缓释作用。The interaction of cucurbit[n=7,8]uril with levodropropizine（LDP）and the drug slow release properties of inclusion complexes in vitro were investigated by means of UV-Vis spectroscopy,fluorescence spectroscopy and 1 H NMR,also the inclusion ratio and stability constant of inclusion complexes of Q[7]-LDP and Q[8]-LDP were determined.The results showed that the interaction of host-guest inclusion complexes was pH sensitive,and LDP formed 1∶1host-guest complexes with Q[n]（n=7,8）.The stability constants of inclusion complexes of Q[7]-LDP and Q[8]-LDP were 3.7×10^3 and 3.8×10^3L/mol,respectively.The drug release rates of Q[7]-LDP and Q[8]-LDP were obviously slower than that of LDP.Q[7]-LDP and Q[8]-LDP exhibited pH sensitive drug sustained-release in vitro,suggesting that they could be new potential carriers for pH stimuli-responsive drug delivery system.

关 键 词：瓜环 左羟丙哌嗪 包合作用 PH敏感性 缓释性能 

分 类 号：O636.12[理学—高分子化学]