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Food increases the bioavailability of acitretin
P J McNamara1, R C Jewell, B K Jensen
1College of Pharmacy, University of Kentucky, Lexington 40536.
Journal of Clinical Pharmacology
|November 1, 1988
Summary
Taking acitretin with food significantly enhances its bioavailability, increasing absorption and plasma concentration. Food intake does not affect the formation of its primary metabolite, Ro 13-7652.
Area of Science:
- Pharmacology
- Drug Metabolism
- Gastroenterology
Background:
- Acitretin is a systemic retinoid used for treating dermatological conditions.
- Understanding acitretin's absorption and bioavailability is crucial for optimizing therapeutic outcomes.
- Food intake is known to influence the absorption of various oral medications.
Purpose of the Study:
- To investigate the effect of food on the oral bioavailability of acitretin.
- To determine how food affects the pharmacokinetic profile of acitretin and its metabolite Ro 13-7652.
Main Methods:
- A randomized crossover study involving 18 healthy male volunteers.
- Administration of a 50 mg oral dose of acitretin under fasted and fed (post-breakfast) conditions.
- Quantification of acitretin and its metabolite Ro 13-7652 in plasma samples using HPLC.
Main Results:
- Acitretin administration with food resulted in a 90% increase in AUC0-15 and a 70% increase in Cmax compared to fasted conditions.
- The time to reach maximum plasma concentration (Cmax) for acitretin remained unaffected by food.
- The ratio of the metabolite Ro 13-7652 to acitretin was consistent between fasted and fed states, indicating no influence on metabolite formation.
Conclusions:
- Concomitant food intake significantly increases the apparent bioavailability of oral acitretin.
- Enhanced solubility, lymphatic absorption, and prolonged gastrointestinal residence time are likely mechanisms for increased acitretin absorption with food.
- Dietary considerations can optimize acitretin therapy by enhancing drug absorption.