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Lipophilicity measurements of protonated basic compounds by reversed-phase high-performance liquid chromatography : II. Procedure for the determination of a lipophilic index measured by reversed-phase high-performance liquid chromatography

The lipophilic properties of a series of basic neuropharmacological compounds were determined by reversed-phase high-performance liquid chromatography. Apparent capacity factors (log k x, pH = 7.5) were measured at different compositions of the methanol-water eluent and extrapolated to 100% water as...

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Bibliographic Details
Published in:Journal of Chromatography A 1985, Vol.320 (2), p.305-312
Main Authors: El Tayar, Nabil, Van de Waterbeemd, Han, Testa, Bernard
Format: Article
Language:English
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Summary:The lipophilic properties of a series of basic neuropharmacological compounds were determined by reversed-phase high-performance liquid chromatography. Apparent capacity factors (log k x, pH = 7.5) were measured at different compositions of the methanol-water eluent and extrapolated to 100% water as the eluent. While parabolic extrapolation was feasible only for a limited number of compounds, linear extrapolation to log k w values was possible for all 25 drugs investigated. Correction for solute ionization yielded log ▪ values which correlate well with published water-octanol partition coefficient (log P oct) values. The best procedure to obtain log K w values is discussed.
ISSN:0021-9673
DOI:10.1016/S0021-9673(01)90508-4