High-performance liquid chromatography of a new 2-amino-2-oxazoline: application to pharmacokinetic studies in dogs |
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Authors: | M I Damaj J H Trouvin B Lambrey C Jacquot |
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Affiliation: | Laboratoire de Pharmacologie et de Pharmacocinétique, Faculté de Pharmacie, Chatenay-Malabry, France. |
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Abstract: | 5-(1'-Phenyl-4'-piperazinomethyl)-2-amino-2-oxazoline (1; COR3224), a derivative of 2-amino-2-oxazolines with antidepressant properties in rats, was assayed in plasma by high-performance liquid chromatography. After back extraction, 1 and a ortho-O-methyl derivative of 1 as the internal standard were separated by reversed-phase liquid chromatography and measured by UV detection (235 nm). The method is rapid and specific: the detection was linear in the range 125-1000 micrograms.L-1, with a detection limit of 50 micrograms.L-1. This method allowed the determination of pharmacokinetic parameters in six beagle dogs after intravenous and oral administration of 14C-labeled 1 ([14C]1) in a crossover study. The comparison of the results obtained from total radioactivity counting and unchanged product evaluated by HPLC-UV suggest the presence of metabolites. |
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