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Titre du document / Document title

Effect of concomitant colestipol hydrochloride administration on the bioavailability of diltiazem from immediate- and sustained-release formulations

Auteur(s) / Author(s)

TURNER Scott W. (1) ; JUNGBLUTH Gail L. (1) ; KNUTH Dean W. (1) ;

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

(1) Pharmacia Corporation, 7000 Portage Road, Kalamazoo, MI 49007, ETATS-UNIS

Résumé / Abstract

Effects of concomitant colestipol administration on plasma concentrations of diltiazem and desacetyldiltiazem from immediate-release (IR) and sustained-release (SR) formulations were assessed in two studies. In the first study, 12 subjects received 120-mg diltiazem hydrochloride (diltiazem) SR capsules or 120-mg diltiazem IR tablets administered alone and in combination with colestipol hydrochloride (colestipol). Following concomitant administration of SR diltiazem with colestipol, AUC0→∞ and Cmax, respectively, were 22 and 36% less, and were 27 and 33% lower for IR diltiazem. In the second study, subjects received 120-mg diltiazem SR capsules at staggered times, without colestipol, 1 h prior to or 4 h following multiple doses of colestipol. A 17% decrease in AUC0-∞ was observed when diltiazem was taken 1 h before colestipol was given, and a 22% decrease when diltiazem was taken 4h after colestipol, relative to diltiazem SR alone. Cmax values were similarly decreased. Results from these two studies show that colestipol can cause a significant decrease in diltiazem absorption from both IR and SR dosage forms. Staggering the administration of colestipol and diltiazem SR did not blunt this effect, indicating that concomitant administration of diltiazem and colestipol should be used with caution, and that the efficacy of diltiazem should be monitored to assure adequate dosing.

Revue / Journal Title

Biopharmaceutics & drug disposition    ISSN  0142-2782   CODEN BDDID8 

Source / Source

2002, vol. 23, no9, pp. 369-377 [9 page(s) (article)] (20 ref.)

Langue / Language

Anglais

Editeur / Publisher

Wiley, Chichester, ROYAUME-UNI  (1979) (Revue)

Mots-clés anglais / English Keywords

Absorption

;

Bioavailability

;

Benzothiazepine derivatives

;

Application method

;

Pharmacokinetics

;

Oral administration

;

Human

;

Controlled release form

;

Immediate release form

;

Dosage form

;

Drug interaction

;

Drug combination

;

Antiarrhythmic agent

;

Calcium antagonist

;

Coronary vasodilator agent

;

Antianginal agent

;

Ion exchange resin

;

Antilipemic agent

;

Diltiazem

;

Colestipol

;

Mots-clés français / French Keywords

Absorption

;

Biodisponibilité

;

Benzothiazépine dérivé

;

Modalité traitement

;

Pharmacocinétique

;

Voie orale

;

Homme

;

Forme libération contrôlée

;

Forme libération immédiate

;

Forme pharmaceutique

;

Interaction médicamenteuse

;

Association médicamenteuse

;

Antiarythmique

;

Antagoniste calcium

;

Vasodilatateur coronarien

;

Antiangoreux

;

Résine échangeuse ion

;

Hypolipémiant

;

Diltiazem

;

Colestipol

;

Mots-clés espagnols / Spanish Keywords

Absorción

;

Biodisponibilidad

;

Benzotiazepina derivado

;

Modalidad tratamiento

;

Farmacocinética

;

Vía oral

;

Hombre

;

Forma liberación controlada

;

Forma liberación inmediata

;

Forma farmacéutica

;

Interacción medicamentosa

;

Asociación medicamentosa

;

Antiarrítmico

;

Antagonista calcio

;

Vasodilatator coronario

;

Antianginoso

;

Resina intercambiadora ión

;

Hipolipemiante

;

Diltiazem

;

Colestipol

;

Mots-clés d'auteur / Author Keywords

colestipol

;

drug interaction

;

diltiazem

;

desacetyldiltiazem

;

Localisation / Location

INIST-CNRS, Cote INIST : 17959, 35400010718576.0030

Nº notice refdoc (ud4) : 14410059



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