六、七、八元瓜环对乌纠中黄酮类成分芦丁的包结作用及缓释性研究

Study on intenaction and slow release property of cucurbit[n = 6,7,8]with Rutin from flavones in wet jiub

利用紫外-可见吸收光谱法研究了六、七、八元瓜环与芦丁的相互作用以及p H对其作用的影响,考察了包合物的体外缓释性能。结果表明,六、七元瓜环可以与芦丁形成1∶1的主客体包结物,八元瓜环与芦丁形成1∶2的包结物。包结平衡常数分别为3.6×10~5L·mol^(-1)、2.1×105L·mol^(-1)、1.9×10^(10)L^2·mol^(-2)。芦丁原药,Q[6]-芦丁、Q[7]-芦丁、Q[8]-芦丁包结物在人工胃液(p H=1.2)中60 min内的累计释放度分别为60.19%、46.71%、49.57、32.54%,在人工肠液(p H=6.8)中的累计释放度分别为73.76%、48.58%、51.32%、33.58%,且缓释曲线非常相似。实验结果表明,瓜环-芦丁主客体包结物的体外累积释放度明显低于芦丁原药,瓜环Q(n=6、7、8)对芦丁均有明显的体外缓释作用,且Q[8]对芦丁的缓释效果最为显著。

The host-gust interaction between cucurbit[n]urils（ Q[n],n = 6,7,8]） and rutin from flavones in wet Jiub was investigated by using UV-vis spectroscopy in solution.The effect of p H on the interaction and the slow release properties of host-gust inclusion complexes were observed by UV-vis spectroscopy.The results related that a 1： 1 host to guest complex were formed between Q[n= 6,7]and rutin,however,the Q[8]include rutin with a 1 ∶ 2 ratio.The stability constants of inclusion are 3. 6×10^5L·mol^-1,2. 1×10~5L·mol^-1,1. 9×10^10L^2·mol^-2for Q[6]-rutin,Q[7]-rutin and Q[8]-rutin systems respectively. The cumulative release rate in rutin,Q[6]-rutin,Q[7]-rutin and Q[8]-rutin in artificial gastric juice（ p H = 1. 2） at 60 min were 60. 19%,46. 71%,49. 57,32. 54%respectively,and in artificial intestinal fluid（ p H = 6. 8） at 60 min were found to be 73. 76%,48. 58%,51. 32%,33. 58% respectively,and the curves of slow release were similarity.The experimental results show that the cumulative release rate of host-gust complex were obviously slower than rutin.The slow release property of cucurbit[n]urils（ Q[n],n = 6,7,8]） to rutin were obviously,and Q[8]to rutin the slow release effect is remarkable especially.