AI Article Synopsis
- An isotope dilution assay was developed to specifically measure 14C-labelled oxprenolol and its nine metabolites in biological samples.
- After adding unlabelled carriers, the compounds were isolated using base- and acid-specific extraction, followed by separation with high-performance liquid chromatography.
- The assay showed high recovery rates (98.7 - 99.8%) in rat and dog blood and urine samples, and it effectively analyzed the metabolic pathways of oxprenolol in dogs.
Article Abstract
An isotope dilution assay for the specific determination of 14C-labelled oxprenolol and nine of its metabolites in the same biological sample is described. After addition of unlabelled carriers to the sample, oxprenolol and the metabolites were isolated by base- and acid-specific extraction and separated by normal-phase high-performance liquid chromatography using two different mobile phases. Quantitation of the various peaks was performed by on-line ultraviolet detection at 275 nm and off-line radiometry by liquid scintillation counting. Endogenous compounds and unknown metabolites did not interfere in the assay. The analysis of rat and dog blood, plasma and urine samples spiked with [14C]oxprenolol hydrochloride, showed mean recoveries between 98.7 and 99.8%. The assay was used to investigate the metabolic fate of [14C]oxprenolol in the dog. Analyses of blood and urine demonstrated the quantitative significance of the various metabolites in the biotransformation of oxprenolol.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/s0021-9673(01)88010-9 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Structural characterization of electrochemically and in vivo generated potential metabolites of selected cardiovascular drugs by EC-UHPLC/ESI-MS using an experimental design approach.
Talanta
January 2018
Department of Environmental Chemistry and Bioanalytics, Faculty of Chemistry, Nicolaus Copernicus University, Gagarin 7, 87-100 Torun, Poland; Centre for Modern Interdisciplinary Technologies, Nicolaus Copernicus University, Wilenska 4, 87-100 Torun, Poland.
In the last few years, a number of studies were conducted which aimed at understanding the mechanisms of cardiovascular drug, metabolism, and there is still the need to determine the metabolites of cardiac drugs for the purpose of metabolism control. In this study, we employ a direct combination of electrochemical oxidation and mass spectrometric (EC-MS) identification for monitoring the oxidation pathway of ten cardiovascular drugs (metoprolol, propranolol, propafenone, mexiletine, oxprenolol, pirbuterol, pindolol, cicloprolol, acebutolol and atenolol). Oxidation was accomplished in an electrochemical thin-layer cell coupled on-line to electrospray ionization mass spectrometry (EC/ESI-MS).
View Article and Find Full Text PDFSimultaneous determination of thirteen beta-blockers and one metabolite by gradient high-performance liquid chromatography with photodiode-array UV detection.
Forensic Sci Int
April 2004
Laboratoire de Pharmacologie-Toxicologie, Centre Hospitalier Universitaire Raymond Poincaré, 104 Boulevard R. Poincaré, 92380 Garches, France.
A new rapid and sensitive high-performance liquid chromatography (HPLC) method has been developed for the simultaneous identification and quantification in human plasma of the 13 most commonly prescribed beta-blockers and one active metabolite-atenolol, sotalol, diacetolol, carteolol, nadolol, pindolol, acebutolol, metoprolol, celiprolol, oxprenolol, labetalol, propranolol, tertatolol and betaxolol. It involves liquid-liquid extraction procedures followed by liquid chromatography coupled to photodiode-array UV detection with a fixed wavelength at 220 nm for quantification. Compounds were separated on a 5 microm Hypurity C(18) (ThermoHypersil) analytical column (250 mm x 4.
View Article and Find Full Text PDFRelationship between hydrophobicity and beta-blocking potencies, affinities or dissociation of beta-blockers from beta-adrenoceptors.
Res Commun Mol Pathol Pharmacol
August 2001
Department of Pharmacology, Niigata College of Pharmacy, Japan.
The present study was performed to assess the relationship between the hydrophobicity of drugs and (1) inhibitory strength (pA2) on chronotropic or inotropic actions, (2) displacemental potencies of 3H-CGP12177 or 125I-iodocyanopindolol binding to beta-adrenoceptors (beta-ARs) (pKi) or (3) dissociating potencies of these drugs from beta-ARs of atria strips pretreated with drugs. The beta-blockers used in the present study were bopindolol, active metabolite of bopindolol (18-502), atenolol, propranolol, pindolol, nadolol, alprenolol, oxprenolol, metoprolol, labetalol and acebutolol. The value of the partition coefficient of propranolol was the highest, and that of the beta1-selective blocker atenolol was the lowest.
View Article and Find Full Text PDFDetermination of drugs in biological fluids by high-performance liquid chromatography with on-line sample processing.
J Chromatogr A
February 1998
Institute of Clinical Pharmacology, Medical Faculty Carl Gustav Carus, Technical University Dresden, Germany.
An automated two column HPLC system with the new packing material LiChrospher RP-18 ADS (alkyl-diol-silica) was tested for the determination of several drugs and metabolites (talinolol, celiprolol, metoprolol, oxprenolol, triamterene, trimethoprim, tiracizine, articaine, detajmium, ajmaline, lamotrigine) in various biological fluids (serum, urine, intestinal aspirates, supernatants of cell cultures and supernatants after protein denaturation). The method allows the direct injection of biological fluids into a reversed-phase HPLC system and on-line clean-up and sample enrichment by a column-switching technique. Precision, accuracy and sensitivity were similar to conventional assays as described in the literature.
View Article and Find Full Text PDFDisposition of human drug preparations in the horse. V. Orally administered oxprenolol.
Biomed Chromatogr
February 1997
Vakgroep Farmacologie, Farmacie en Toxicologie, Faculteit Diergeneeskunde, Universiteit Gent, Merelbeke, Belgium.
Urinary concentrations of the beta-antagonist oxprenolol and some of its major human metabolites were determined following oral administration of a dose of 160 mg to five fasted horses. Quantitation was performed by gas chromatography-mass spectrometry (GC-MS) in the selected ion mode (SIM) by monitoring ion m/z 466 of the heptafluorobutyric derivatives. As early as 2 h after dosage oxprenolol could be detected in hydrolysed urine and remained detectable up to 24 h.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!