八元瓜环对噻苯达唑的包合作用及pH敏感缓释性能

Interaction of Cucurbit[8] uril with Thiabendazole and pH Sensitive Slow Release Properties

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∶2。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 thiabendazole（TBZ） and drug slow release properties of inclusion complexes in vitro were investigated.METHODS Drug slow release properties、inclusion ratio and stability constant of inclusion complexes of Q[8]-TBZ system were determined by means of -1H NMR technique,UV-Vis spectroscopy,fluorescence spectroscopy.RESULTS Q[8] and TBZ occur supramolecular inclusion interaction.TBZ form a 1：2 complex with Q[8].The interaction of host-guest inclusion complexes have pH sensitive properties under acidic or neutral conditions.The cumulative release rate in vitro of TBZ and Q[8]-TBZ in artificial gastric juice（pH=1.2） at 400 min was 99.70% and 57.92% respectively;The cumulative release rate in vitro of TBZ and Q[8]-TBZ in phosphate buffer solution（pH=4.0） at 400 min was 99.81% and 68.92% respectively;and in artificial intestinal fluid（pH=6.8） at 400 min was found to be 99.84% and 83.55% respectively.CONCLUSION Q[8] could be a new potential carrier for pH stimuli-responsive drug delivery system.