PLASMA-LEVELS OF PROBUCOL IN MAN AFTER SINGLE AND REPEATED ORAL DOSES

Abstract

After a single oral dose of 3 g probucol to healthy volunteers, mean peak plasma concentrations were 3.9 .mu.g/ml at 24 h. Successive blood level measurements showed diphasic elimination, with half-lives of .apprx. 1 and 23 days. Plasma levels after a single 250 mg dose in volunteers are reported. In 51 hypercholesterdemic patients who received probucol 1 g daily for periods of 1-12 mo., a concentration plateau was obtained within 1-3 mo. of treatment; the mean plasma levels ranged from 18.2-39.2 .mu.g/ml depending on the duration of probucol therapy. In another study carried out on 8 patients who were given the same daily dose during 12 mo., the mean probucol plasma level at the end of that period was 18.9 .mu.g/ml. Repeated administration of probucol to healthy volunteers showed good correlation between dosage and blood levels.