Stable isotope methodology for studying the performance of metoprolol Oros tablets in comparison to conventional and slow release formulations

Metoprolol Oros tablets were designed to deliver their drug content as a constant rate over a period of time longer than that currently recorded with slow-release dosage forms. The bioavailability of 7/95, 14/190 and 21/285 Oros tablets was compared to that of either 100 mg conventional or 200 mg sl...

Full description

Saved in:
Bibliographic Details
Published in:European journal of drug metabolism and pharmacokinetics 1994-10, Vol.19 (4), p.375-380
Main Authors: RICHARD, J, CARDOT, J.-M, GODBILLON, J
Format: Article
Language:English
Subjects:
Absorption
Adult
Antihypertensive agents
Biological and medical sciences
Biological Availability
Cardiovascular system
Chemistry, Pharmaceutical
Delayed-Action Preparations
Deuterium
Dose-Response Relationship, Drug
Female
Humans
Individuality
Injections, Intravenous
Male
Medical sciences
Methods
Metoprolol - administration & dosage
Metoprolol - pharmacokinetics
Pharmacology. Drug treatments
Tablets
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Metoprolol Oros tablets were designed to deliver their drug content as a constant rate over a period of time longer than that currently recorded with slow-release dosage forms. The bioavailability of 7/95, 14/190 and 21/285 Oros tablets was compared to that of either 100 mg conventional or 200 mg slow-release Lopresor tablets in 3 two-period change over experiments. In each experiment, 6 healthy volunteers received intravenous deuterated metoprolol concomitantly with one of the Oros systems or with one of the other two formulations. The Oros tablets gave rise to lower and steady plasma levels of metoprolol over 24 h than the other formulations. Their mean absorption time was around 3 times longer than that of the slow-release tablets. The amount of the drug absorbed unchanged was linearly related to the dose. The influence of the gastrointestinal transit time on the performance of Oros tablet was limited. These studies demonstrated the value of the stable isotope methodology in bioavailability assessment for drugs presenting a high inter-subject variability in their plasma clearance such as metoprolol.
ISSN:0378-7966
2107-0180
DOI:10.1007/BF03188865