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  • Title: Impairment of captopril bioavailability by concomitant food and antacid intake.
    Author: Mäntylä R, Männistö PT, Vuorela A, Sundberg S, Ottoila P.
    Journal: Int J Clin Pharmacol Ther Toxicol; 1984 Nov; 22(11):626-9. PubMed ID: 6389377.
    Abstract:
    Single oral doses of captopril (50 mg) were given in a randomized cross-over study to 10 healthy volunteers after fasting, after a standardized breakfast (440 kcal; 1804 kJ) or with 50 ml of an antacid suspension. Blood and urine samples were analyzed by gas chromatography. The peak captopril concentrations attained were 701 +/- 81 ng/ml (mean +/- s.e.m.) after fasting, 351 +/- 56 ng/ml with an antacid (p less than 0.05) and 140 +/- 14 ng/ml after a meal (p less than 0.01). The peak concentrations were reached in 0.5, 0.9 and 1.5 h (p less than 0.01), and the areas under the blood concentration-time curves were 782 +/- 86, 456 +/- 60 (p less than 0.05) and 344 +/- 47 ng X h/ml (p less than 0.01), respectively. The relative bioavailability of captopril was 0.66 and 0.48 with antacid and after food, respectively. The deleterious effect of food - but not that of antacid - was reflected as a delayed hypotensive activity of captopril.
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