用胶束色谱法测定磺胺类药物的疏水性常数

Determination of Sulfonamide' s Hydrophobicity by Micellar Liquid Chromalography

在药物定量构效关系(QSAR)研究中,利用反相高效液相色谱法(RP-HPLC)保留值代替正辛醇-水分配系数logP_(ow)已有许多报道。但RP-HPLC保留值与logP_(ow)之间的相关性仅限于同类化合物(congeneric compounds)。对于疏水性强的化合物经常需要在流动相中加入有机改性剂。

The logKw(a theoretical capacity factor obtained by extrapolation of retention data in binary solvent system to pure water) and logk' (a capacity factor obtained by using micellar mobile phase) of sulfonamides were determined on C18 column. The Kmw(solute binding constants to micelle) and K0 (capacity factor at zero micelle concentration) were calculated. The correlations between these capacity factors and logPow (n-octanol-water partition coefficients) or biological activities of sulfonamides were studied. The results showed that the cationic surfactant( CATB) concentration.The correlations between logk' and logPow were better than those between logKw and logPow . Micellar liquidchromatography has been used to study the quantitativestructure-activity relationships of sulfonamides.