盐酸地尔硫卓与七八元瓜环的包合作用及体外释药性能  

Interaction of Cucurbit[n=7,8]urils with Diltiazem Hydrochloride and Drug Release Properties in vitro

作　　者：方权辉 林友文[1] FANG Quanhui;LIN Youwen(College of Pharmacy,Fujian Medical University,Fuzhou 350122,China)

机构地区：[1]福建医科大学药学院

出　　处：《福建医科大学学报》2019年第5期314-318,共5页Journal of Fujian Medical University

基　　金：福建省自然科学基金(2011J01289)

摘　　要：目的研究七元及八元瓜环(Q[7]及Q[8])与盐酸地尔硫卓(DIL)的包合作用及包合物的体外释药性能。方法利用紫外光谱、荧光光谱、1H NMR等技术研究Q[7]-DIL及Q[8]-DIL体系的包合作用,测定包合比、包合稳定常数及包合物的体外药物累积释放度。结果Q[7]-DIL及Q[8]-DIL体系的包合比均为1∶1,包合平衡常数分别为6.28×10^3和8.69×10^3 L/mol。在pH分别为1.2,4.0及6.8的3种介质中,包合物Q[7]-DIL的400 min体外累积释放度分别为44.80%,56.16%及68.05%,包合物Q[8]-DIL的体外累积释放度分别为39.28%,52.70%及58.34%,DIL原药的体外累积释放度分别为98.51%,97.76%及97.80%。结论Q[7]和Q[8]的包合对DIL具有明显的pH敏感性缓释作用。Objective To investiage the interaction of cucurbit[n=7,8]urils with Diltiazem Hydrochloride(DIL)and drug slow release properties of inclusion complexes in vitro.Methods Drug slow release properties,inclusion ratio and stability constant of inclusion complexes of Q[7]-DIL and Q[8]-DIL system were determined by means of UV-Vis spectroscopy,fluorescence spectroscopy,and 1 H NMR technique.Results DIL both formed a 1∶1 host-guest complex with Q[7]and Q[8].Stability constant of inclusion complexes of Q[7]-DIL and Q[8]-DIL were 6.28×10^3 L/mol and 8.69×10^3 L/mol,respectively.In pH=1.2,pH=4.0,and pH=6.8 various medium,the cumulative release rate in vitro of Q[7]-DIL at 400 min were 44.80%,56.16%,and 68.05%respectively,while the cumulative release rate in vitro of Q[8]-DIL at 400 min were 39.28%,52.70%,and 58.34%respectively.The cumulative release rate in vitro of DIL at 400 min were 98.51%,97.76%,and 97.80%respectively.Conclusion Q[7]-DIL and Q[8]-DIL are obviously pH sensitive drug sustained-release in vitro.

关 键 词：盐酸地尔硫卓 氢离子浓度 迟效制剂 药用制剂 

分 类 号：R341[医药卫生—基础医学] R544.1