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Retention–activity relationship studies of benzodiazepines by micellar liquid chromatography
Author(s) -
MoleroMonfort M.,
Sagrado S.,
VillanuevaCamañas R. M.,
MedinaHernández M. J.
Publication year - 1999
Publication title -
biomedical chromatography
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.4
H-Index - 65
eISSN - 1099-0801
pISSN - 0269-3879
DOI - 10.1002/(sici)1099-0801(199910)13:6<394::aid-bmc898>3.0.co;2-0
Subject(s) - chemistry , micellar liquid chromatography , chromatography , metabolite , partition coefficient , membrane , phase (matter) , lipophilicity , biological membrane , micelle , high performance liquid chromatography , organic chemistry , aqueous solution , biochemistry
Solute partitioning into lipid bilayers of biological membranes is the basis for drug and metabolite uptake, passive transport across membranes and bioaccumulation. In order to emulate in vitro the partitioning process in the biomembranes, different approaches have been proposed. The use of micellar solutions as mobile phases in reversed‐phase liquid chromatography (micellar liquid chromatography, MLC) has proven to be valid in the prediction of the biological activities of local anesthetics, catecholamines and barbiturates. In this paper we focus our attention on benzodiazepines. The retention of benzodiazepines using different concentrations of Brij35 as micellar mobile phase in modified C 18 stationary phase was studied. Quantitative retention–activity relationships (QRAR) in MLC were investigated for these compounds. An adequate correlation between the capacity factors (log k ) and the toxicity (log LD 50 ) and anxiolitic activity (log ED 50 ) of benzodiazepines was obtained. Copyright © 1999 John Wiley & Sons, Ltd.