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化学学报
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化学学报 ›› 2009, Vol. 67 ›› Issue (18): 2116-2120. 上一篇    下一篇

研究论文

微乳液相色谱测定药物的油-水分配系数的新方法研究

李 宁 黄纪云 黄碎锦 高崇凯*   

  1. (广东药学院 广州 510006)
  • 投稿日期:2009-01-20 修回日期:2009-03-16 发布日期:2009-12-31
  • 通讯作者: 高崇凯

A Novel Determination of Oil-Water Partition Coefficients for Pharmaceuticals by Microemulsion Liquid Chromatography

Li, Ning Huang, Jiyun Huang, Suijin Gao, Chongkai*   

  1. (Guangdong College of Pharmacy, Guangzhou 510006)
  • Received:2009-01-20 Revised:2009-03-16 Published:2009-12-31
  • Contact: Gao, Chongkai

被引次数

22

建立快速微乳液相色谱法(MELC)测定药物的油-水分配系数(log P)的方法. 选择5种模拟生物膜的微乳流动相体系, 以7个标准药物的log P对保留因子(log k)的回归线性方程, 计算被测药物的log P值. 并以药物文献的log P值对实验测得log k值的线性相关系数为参数, 对微乳体系的表面活性剂和油相的种类进行考察, 得到测定非同类的中性、碱性药物的油-水分配系数最佳流动相体系为6.0% Brij35-6.6%正丁醇-0.8%正辛醇-86.6%磷酸缓冲液(0.05 mol• L－1, pH 7.0), 其测得值与文献的实验值平均相差0.3个对数单位. 结果显示该方法可靠、高效、重现性好, 可用于药物的油-水分配系数log P的测定.

关键词: 微乳液相色谱, 油-水分配系数, log P

A rapid screening assay determination of octanol-water partition coefficients (log P) of pharmaceuticals was developed by using microemulsion liquid chromatography (MELC). Seven standard compounds with known log P values were used for constructing the calibration curve of log P against the MELC log k, by which the log P values of the pharmaceuticals were calculated. The types of surfactants and oil phase were evaluated in the microemulsion systems using such parameters as linear correlation coefficients the literature log P values against the experimentally measured log k values. The optimized MELC system with microemulsion consisting of 6.0% polyoxyethylene lauryl ether (Brij35)-6.6% butanol-0.8% octanol-86.6% phosphate buffer (0.05 mol•L－1, pH 7.0) shows good correlation (r＝0.96) to the experimental log P (Elog P) values for noncongeneric neutral and basic pharmaceuticals. The average error of log P values measured by MELC is within 0.3 log unit of the values from the literature. The results indicate that MELC can serve as a high throughput, reliable and robust approach and as a valid model for log P determinations.

Key words: microemulsion liquid chromatography, oil-water partition coefficient, log P