八元瓜环对噻苯达唑的包合作用及pH敏感缓释性能

摘要

目的 研究八元瓜环(Q[8])与噻苯达唑(TBZ)的包合作用及包合物的体外释药性能.方法 采用1H NMR、紫外光谱、荧光光谱等技术考察Q[8]-TBZ体系的主-客体包合作用；测定Q[8]-TBZ体系的包合比、包合稳定常数、pH敏感性及包合物的体外药物累积释放度.结果 Q[8]与噻苯达唑在酸性和中性条件下均发生超分子包合作用,主客体的超分子包合作用具有pH敏感性,包合比为1∶KG-*3/52.原药TBZ及Q[8]-TBZ包合物在人工胃液(pH=1.2)中的400min累积释放度分别为99.8%、57.92%;在pH=4.0磷酸盐缓冲液中两者400min累积释放度分别为99.7%、68.94%;而在人工肠液(pH=6.8)中两者的400min累积释放度分别是99.5%、83.55%.结论 Q[8]包合对TBZ有明显的pH敏感性缓释作用.%OBJECTIVE The interaction of cucurbit[8] uril with thiabendaz ole (TBZ) and drug slow release properties of inclusion complexes in vitro were investigated.METHODS Drug slow release properties、inclusion r atio and stability constant of inclusion complexes of Q[8]-TBZ system were de termined by means of 1H NMR technique,UV-Vis spectroscopy,fluorescence spec troscopy.RESULTS Q[8] and TBZ occur supramolecular inclusion interaction.TBZ form a 1∶2 complex with Q[8].The interaction of host-gues t inclusion complexes have pH sensitive properties under acidic or neutral condi tions.The cumulative release rate in vitro of TBZ and Q[8]-TBZ in artificial gastric juice(pH=1.2) at 400min was 99.70% and 57.92% respectively;The cumu lative release rate in vitro of TBZ and Q[8]-TBZ in phosphate buffer solution(pH=4.0) at 400min was 99.81% and 68.92% respectively;and in artificial inte stinal fluid(pH=6.8) at 400min was found to be 99.84% and 83.55% respectively.CONCLUSION Q[8] could be a new potential carrier for pH sti muli-responsive drug delivery system.