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Development of predictive retention–activity relationship models of antipsychotic drugs by micellar liquid chromatography

✍ Scribed by Y. Martín-Biosca; M. Molero-Monfort; S. Sagrado; R. M. Villanueva-Camañas; M. J. Medina-Hernández


Publisher
John Wiley and Sons
Year
1999
Tongue
English
Weight
201 KB
Volume
13
Category
Article
ISSN
0269-3879

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✦ Synopsis


The predictive and interpretative capability of quantitative chromatographic retention-biological activity models is supported by the fact that in adequate experimental conditions the solute partitioning into the chromatographic system can emulate the solute partitioning into lipid bilayers of biological membranes, which is the basis of drug and metabolite uptake, passive transport across membranes and bioaocumulation. The use of micellar solutions of Brij35 as mobile phases in reversed liquid chromatography has proven to be valid in predicting some biological activities of different kinds of drugs. In this paper, the correlations between the logarithm of capacity factors and pharmacokinetic, preclinical pharmacology and therapeutic efficacy parameters of phenothiazines are studied. Parabolic quantitative retention-activity relationship models with predictive and interpretative ability have been obtained.


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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