Titre du document / Document title

Bioavailability of amiodarone tablets administered with and without food in healthy subjects

Auteur(s) / Author(s)

XU MENG ; MOJAVERIAN Parviz ; DOEDEE Marijo ; LIN Emil ; WEINRYB Ira ; CHIANG Soong T. ; KOWEY Peter R. ;

Affiliation(s) du ou des auteurs / Author(s) Affiliation(s)

Wyeth-Ayerst Research, Philadelphia, Pennsylvania, ETATS-UNIS
School of Pharmacy, University of California at San Francisco, San Francisco, California, ETATS-UNIS
Lankenau Hospital and Medical Research Center, Wynnewood, Pennsylvania, ETATS-UNIS

Résumé / Abstract

The tablet form of amiodarone is indicated for the treatment of recurrent ventricular fibrillation or hemodynamically unstable ventricular tachycardia. It is recommended that the tablet be taken with meals in cases of gastrointestinal intolerance. However, the effect of food on its bioavailability is unknown. The primary objective of this study was to determine the effect of food on the bioavailability of amiodarone. This was a 2-period crossover study conducted in 30 healthy male subjects. Subjects were randomly assigned to 1 of 2 sequences in which the following 2 treatments were administered: (1) a single-dose of amiodarone (three 200-mg Cordarone tablets) after an overnight fast, and (2) the same dose immediately after a standard high-fat breakfast. Plasma concentrations of amiodarone and desethylamiodarone (DEA) were measured for 6 weeks after each dose. Food enhanced the extent of absorption, resulting in a peak concentration (C_max) and area under the curve (AUC_T) 3.8 and 2.4 times the respective values under fasting conditions. Food also significantly increased the rate of absorption, reducing the time (t_max) to C_max from 7.1 to 4.5 hours. The effect of food on DEA levels was significant but less pronounced. An in vitro dissolution study confirmed a marked difference between amiodarone release under simulated fed and fasting conditions. Thus, food significantly enhances both the rate and extent of absorption of amiodarone, which is attributed partially to the effect of food on drug release from its formulation. Therefore, it is recommended that amiodarone tablets be taken consistently with meals.

Revue / Journal Title

The American journal of cardiology   ISSN 0002-9149   CODEN AJCDAG 

Source / Source

2001, vol. 87, n^o4, pp. 432-435 (9 ref.)

Langue / Language

Anglais

Editeur / Publisher

Elsevier, New York, NY, ETATS-UNIS  (1958) (Revue)

Mots-clés anglais / English Keywords

Amiodarone ; Bioavailability ; Route of administration ; Tablet ; Human ; Food ; Comparative study ; Exploration ; Food drug interaction ; Iodine Organic compounds ;

Mots-clés français / French Keywords

Amiodarone ; Biodisponibilité ; Voie administration ; Comprimé ; Homme ; Aliment ; Etude comparative ; Exploration ; Interaction aliment médicament ; Iode Composé organique ;

Mots-clés espagnols / Spanish Keywords

Amiodarona ; Biodisponibilidad ; Vía administración ; Tableta ; Hombre ; Alimento ; Estudio comparativo ; Exploración ; Interacción alimento medicamento ; Iodo Compuesto orgánico ;

Localisation / Location

INIST-CNRS, Cote INIST : 8674, 35400009797987.0110