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Food Increases the Bioavailability of Acitretin
Author(s) -
McNamara Patrick J.,
Jewell Roxanne C.,
Jensen Bradford K.,
Brindley Charles J.
Publication year - 1988
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1002/j.1552-4604.1988.tb03129.x
Subject(s) - acitretin , bioavailability , metabolite , crossover study , ingestion , pharmacokinetics , pharmacology , chemistry , absorption (acoustics) , area under the curve , oral administration , active metabolite , medicine , psoriasis , dermatology , physics , alternative medicine , pathology , acoustics , placebo
Eighteen healthy male volunteers received 50 mg oral doses of acitretin on two occasions, according to a random crossover design. Acitretin was administered during a complete fast or following a moderate breakfast. Plasma samples were obtained at various times and the concentration of acitretin and its 13‐cis isomeric metabolite (Ro 13–7652) were quantified by a specific HPLC assay. The AUC 0–15 for acitretin was increased when administered with food for all subjects (except one) with a mean increase of 90% (from 1175 to 2249 ng/ml ṁ hr). The maximum plasma concentration of acitretin (C max ) was increased by 70% when administered with food (from 245 to 416 ng/ml), while the time to reach C max was unaffected. The ratio of AUC of Ro 13–7652 to acitretin was the same for both the fasted and fed conditions; therefore, the formation of metabolite was not influenced by concomitant ingestion of food. The presence of food increases the apparent bioavailability of acitretin. A likely mechanism behind this observation is an increase in acitretin solubility in addition to an increase in the lymphatic absorption and a prolonged residence time of the drug in the gastrointestinal tract.