二苯乙烯苷及其β-环糊精包合物的稳定性研究  

The stability study of stilbene glucoside and its β-cyclodextrin inclusion complex

作　　者：王文静[1] 刘冬丽[1] 王葳[1] 魏泽英[1] 

机构地区：[1]云南中医学院中药学院,昆明650500

出　　处：《环球中医药》2016年第4期414-418,共5页Global Traditional Chinese Medicine

基　　金：国家自然科学基金(81060337)

摘　　要：目的明确影响二苯乙烯苷及其β-环糊精包合物稳定性的因素。方法以β-环糊精与二苯乙烯苷用量比、包合时间、包合温度为影响因素,按L9(34)正交实验筛选包合条件;利用高效液相色谱法,以二苯乙烯苷含量为指标,分别考察了人工胃液、人工肠液及醋酸-醋酸钠缓冲液、氨-氯化铵缓冲液、光照对二苯乙烯苷及其β-环糊精包合物稳定性的影响。结果 (1)根据正交实验结果,确定最佳包合条件为:8倍量的β-环糊精,包合时间为2小时,包合温度为35℃;(2)12小时内,二苯乙烯苷未包合物的含量在人工胃液中由100%下降至79.7%,在醋酸-醋酸钠缓冲液中由100%下降至15.9%;β-环糊精包合物中二苯乙烯苷含量在人工胃液中1小时达到100%,在醋酸-醋酸钠缓冲液中2小时达到100%,随后受酸度影响逐渐下降。二苯乙烯苷未包合物在人工肠液及氨-氯化铵缓冲液中的稳定性差,几乎无法存在;其β-环糊精包合物的稳定性有所改善,在肠液中0.5小时含量达95.8%,之后未检出;在碱性缓冲液中4小时达到峰值,6小时后未检出。光照条件下,48小时后二苯乙烯苷的含量由100%下降至50.2%;β-环糊精包合物的含量在实验条件下明显得到改善,48小时后含量仍可达90.5%。结论二苯乙烯苷及其β-环糊精包合物在酸性环境下较碱性条件下稳定;在酸性溶液中,随着溶液酸性增强,其稳定性变差;β-环糊精包合物的稳定性明显强于未包合物,说明利用β-环糊精对二苯乙烯苷进行包合可以在一定程度上使其稳定。Objective To make certain the influence factors of affecting the stability of stilbene glucoside and its β-cyclodextrin inclusion complex. Methods The β-cyclodextrin inclusion of stilbene glucoside was conducted according to an L9（ 34） orthogonal experiment design with three factors,namely the ratio of β-cyclodextrin amount to stilbene glucoside,the time and temperature of inclusion. The contents of stilbene glucoside were detected by HPLC in a simulated gastric fluid,a simulated intestinal fluid,an acetic acid-sodium acetate buffer solution,an ammonia-ammonium chloride buffer solution,and under illumination,respectively. Results 1. Optimal inclusion conditions from orthogonal experiments were an amount of β-cyclodextrin 8 times as much as that of stilbene glucoside,an inclusion time was 2. 0 h and inclusion temperature was 35℃. 2. The content of stilbene glucoside without β-cyclodextrin inclusion in the simulated gastric fluid went down from 100% to 79. 7% in 12. 0h,and in the acetic acid-sodium acetatebuffer solution declined from 100% to 15. 9%. The content of the β-cyclodextrin inclusion complex of stilbene glucoside in the simulated gastric fluid went up to 100% in 1. 0 h and 2. 0h in the acetic acid-sodium acetate buffer solution,and afterwards went down gradually influenced by the acidity of the fluid. Stilbene glucoside without β-cyclodextrin inclusion was very unstable in the simulated intestinal fluid and the ammonia-ammonium chloride buffer solution. The β-cyclodextrin inclusion complex of stilbene glucoside was more stable,and the content was reached 95. 8% in the simulated intestinal fluid in 0. 5h,and became undetectable afterwards,and it was reached peaked in 4. 0 h and became undetectable in 6. 0 h in the alkaline solution. Under illumination,the content of stilbene glucoside without β-cyclodextrin inclusion went down from 100% to 50. 2% in 48. 0h,and its β-cyclodextrin inclusion complex was more stable with the content of 90. 5% in 48. 0h. Conclusion Stilbene glucoside and its β-

关 键 词：二苯乙烯苷 Β-环糊精包合物 何首乌 稳定性 含量测定 

分 类 号：R932[医药卫生—生药学]