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Influence of food on the disposition of the monoamine oxidase‐A inhibitor brofaromine in healthy volunteers
Author(s) -
Degen P. H.,
Cardot J. M.,
Czendlik C.,
Dieterle W.
Publication year - 1993
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/bdd.2510140304
Subject(s) - cmax , bioavailability , bioequivalence , pharmacokinetics , tolerability , chemistry , oral administration , pharmacology , medicine , endocrinology , adverse effect
The effect of food on the bioavailability of brofaromine hydrochloride was investigated in a randomized cross‐over study. Eight healthy male volunteers were given single peroral doses of 75 mg brofaromine hydrochloride after overnight fasting or a fat‐ and proteinrich breakfast. Mean (± SD) areas under the plasma concentration‐time curves (AUC) were 9.66 (2.35) μmoll −1 h when given to the fasted volunteers and 11.82 (3.78) μmoll −1 h ( p = 0.0413) when given after a substantial breakfast. Mean (± SD) maximum plasma concentrations ( C max ) were 0.71 (0.13) μmoll −1 when given to the fasted volunteers and 0.85 (0.22) μmoll −1 ( p > 0.05) when given after breakfast. Thus, both the average AUC and C max were increased by approximately 20 per cent when brofaromine hydrochloride was given with food. The times when C max was reached ( t max ) as well as the elimination half‐lives were not influenced by concomitant intake of food. The tolerability was the same whether brofaromine was given before or after food in healthy volunteers. The slight effect of food on the bioavailability of brofaromine should be of little therapeutic consequence because of the observed wide inter‐subject variability of the plasma levels.