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鱼腥草素钠与β-环糊精包络常数的电泳法研究

Inclusion constant of sodium houttuyfonate and β-cyclodextrin measured by capillary electrophoresis

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【作者】 夏之宁项顺锋李珍义孙冠芸曾令高

【Author】 XIA Zhi-ning 1, XIANG Shun-feng 1, LI Zhen-yi 2, SUN Guan-yun 3, ZENG Ling-gao 4 (1. Institute of Chemistry and Chemical Engineering, Chongqing University, Chongqing 400044, China; 2. Chongqing Geologic Research Institute, Southwest Branch of China National Petroleum Co., Chongqing 400021, China; 3. Chongqing Academy of Chinese Materia Medica, Chongqing 400065, China; 4. Chongqing Institute for Drug Control, Chongqing 400015, China)

【机构】 重庆大学化学化工学院分子相互作用研究室西南油气田分公司重庆地质研究所重庆市中药研究院重庆市药品检验所 重庆400044重庆400044重庆400021重庆400065重庆400015

【摘要】 目的 建立用毛细管电泳法测定包络物稳定性的方法 ,并以此研究抗菌药鱼腥草素钠与 β 环糊精相互作用的强度 ,测定二者形成的超分子包络物的包络常数。方法 用毛细管电泳法测定鱼腥草素钠的淌度 ,变化缓冲溶液中环糊精浓度 ,通过“电泳峰漂移法”及其数学模型 ,从鱼腥草素钠的电泳淌度差计算获得包络物的包络常数。结果 鱼腥草素钠的淌度随着缓冲溶液中 β 环糊精浓度的增加而增大 ,当淌度到达极限值后 ,不再随 β 环糊精浓度的增加而变化。方法的重现性高。获得包络常数的对数值logKGH=3 81。结论 鱼腥草素钠与 β 环糊精间作用强 ,当1∶1混合时 ,鱼腥草素钠的理论转化率可达 98%。其超分子包络物的包络常数值与 β 环糊精浓度无关。毛细管电泳的电泳峰漂移法可以用于指导药物包络常数的测定 ,进一步可用于包络物在生理条件下的稳定性研究。

【Abstract】 Aim To establish a method to measure the inclusion constant of supramolecular compound by capillary electrophoresis. In addition, by employing this method to investigate the intensity of interaction of antibacterial sodium houttuyfonate and β-cyclodextrin, and to measure the stability constant of the inclusion compound formed. Methods The mobilities of houttuyfonate were measured in solutions with different concentrations of β-cyclodextrin by capillary electrophoresis. The stability constant of the inclusion compound was calculated by peak-shift model mathematically. Results The mobility of houttuyfonate shifts from its original value with the increased concentration of β-cyclodextrin. When the limit was reached, the mobility of sodium houttuyfonate did not change even by increasing the concentration of β-cyclodextrin. The reproducibility is well, and the logarithm of inclusion constant obtained was 3.81 regardless of β- cyclodextrin concentration added. The interaction of the sodium houttuyfonate and β-cyclodextrin is strong. If they blended at a radio of 1∶1 , the transform rate of sodium houttuyfonate is 98%. The value of stability constant of supramolecular inclusion compound is independent of concentration of β-cyclodextrin. Conclusion This technique of capillary electrophoresis can be used to the measurement of inclusion constant of drug with β-cyclodextrin. Furthermore, it can be applied to research the stability of inclusion compound drugs in physiological condition.

【基金】 教育部《跨世纪优秀人才培养计划》资助项目 (教技函 [2 0 0 1] 3 ) ;国家自然科学基金资助项目 (2 0 175 0 3 8)
  • 【文献出处】 药学学报 ,Acta Pharmaceutica Sinica , 编辑部邮箱 ,2003年01期
  • 【分类号】R284
  • 【被引频次】11
  • 【下载频次】202
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