Influence of food on the disposition of the monoamine oxidase‐A inhibitor brofaromine in healthy volunteers

摘要

AbstractThe 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−1h when given to the fasted volunteers and 11.82 (3.78) μmoll−1h (p= 0.0413) when given after a substantial breakfast. Mean (± SD) maximum plasma concentrations (Cmax) were 0.71 (0.13) μmoll−1when given to the fasted volunteers and 0.85 (0.22) μmoll−1(p>0.05) when given after breakfast. Thus, both the average AUC andCmaxwere increased by approximately 20 per cent when brofaromine hydrochloride was given with food. The times whenCmaxwas reached (tmax) 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 variabili