摘要
本文使用胶束色谱法研究了某些非甾体抗炎药的疏水性。检查了胶束色谱保留值与文献logPow的相关性。观察了表面活性剂SDS浓度的影响。对于胶束洗脱剂,logK'与logPow的相关好于k与logPow.与logk'w((甲醇—水为洗脱剂得到的外推容量因子)相比,logk'与logPow的相关性较好。logKMw(胶束—水结合常数)或logK'o(胶束浓度为零时的保留因子)与logPow也存在着线性相关。结果表明在药物定量构效关系的研究中使用胶束色谱进行药物疏水性的定量测定是很有希望的。
Mi(?)ellar liquid chromatography(MLC) was used in the study of the hydrophobicities of some nonsteroidal anti-inflammatory drugs. The correlations between retention values of the drugs in MLC and referential logPow were examined. The effects of surfactant (SDS) concentrations were also investigated. For micellar eluents logk'vs logPow provided a better correlations than k'vs logPow. Compared with logk'w (a extrapolated capacity factor obtained by using hydroorganic eluents), the correlation between logk' and logPow was more desirable. Linear correlations between logKmm(micellewater binding constant) or logK'o(retention factor at zero micelle concentration) versus lopPow were observed. It is concluded that micellar liquid chromatography is a promising technique for the quantitation of hydrophobicity in quantitative structure-activity relationship research.
关键词
胶束色谱
疏水性
非甾体抗炎药
Micellar liquid chromatography(MLC)
Hydrophobicity
Nonsteroidal anti-inflammatory drugs
Quantitative structure activity relationships (QSAR)
Partition coefficient(logPow)