Titre du document / Document title

Pharmacokinetics of a new extended-release nifedipine formulation following a single oral dose, in human volunteers

Auteur(s) / Author(s)

CAINAZZO M. M. ⁽¹⁾ ; PINETTI D. ⁽¹⁾ ; SAVINO G. ⁽¹⁾ ; BARTIROMO M. ⁽²⁾ ; FORGIONE A. ⁽³⁾ ; BERTOLINI A. ⁽¹⁾ ;

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

⁽¹⁾ Clinical Pharmacology and Toxicology Section, University of Modena and Reggio Emilia, School of Medicine, Policlinico of Modena, Modena, ITALIE
⁽²⁾ Institute of Biotechnology, University of Napoli Federico II,, ITALIE
⁽³⁾ Department of Experimental Medicine, Section of Pharmacology Leonardo Donatelli, School of Medicine, 2nd University of Naples, ITALIE

Résumé / Abstract

This study aimed to define the pharmacokinetics of nifedipine following oral administration of a new extended-release formulation. Twelve healthy volunteers of both sexes, aged 39 ± 4 years, were treated with a single oral tablet of a new extended-release formulation containing 40 mg of nifedipine. Samples of venous blood were taken before dosing, after 30 min and at 1, 2, 4, 8, 12, 16, 20 and 24 h after administration. Nifedipine concentration was measured by means of a high-performance liquid chromatography method. Noncompartmental pharmacokinetics parameters were then calculated. The plasma concentration of nifedipine increased slowly and in seven subjects biphasic peaks occurred. The mean values were as follows: t_max: 8.5 ± 1.2 h; C_max: 36.55 ± 6.76 ng/ml; AUC: 347.06 ± 51.61 ng/h/ml; AUC∞: 409.99 ± 61.08 ng/h/ml; A_half-life: 2.26 ± 0.36 h; D_half-life: 2.43 ± 0.44 h; E_half-life: 4.62 ± 0.79 h. Twenty-four hours after administration nifedipine was still detectable (3.17 ± 0.67 ng/ml). Arterial blood pressure decreased and heart rate increased concurrently and proportionally to the increase in nifedipine concentration. Extended-release nifedipine formulations have better tolerability profiles than immediate-release formulations, which are at present not recommended in the treatment of hypertension, hypertensive crises or myocardial infarction. This new extended-release formulation has interesting pharmacokinetic parameters and may be effective in conditions in which dihydropyridine calcium channel blockers are indicated.

Revue / Journal Title

Drugs under experimental and clinical research   ISSN 0378-6501   CODEN DECRDP 

Source / Source

2005, vol. 31, n^o3, pp. 115-121 [7 page(s) (article)] (17 ref.)

Langue / Language

Anglais

Editeur / Publisher

Bioscience Ediprint, Geneva, SUISSE  (1977) (Revue)

Mots-clés anglais / English Keywords

Dihydropyridine derivatives ; Calcium antagonist ; Dosage form ; Volunteer ; Human ; Oral administration ; Single dose ; Formulation ; Nifedipine ; Controlled release form ; Pharmacokinetics ;

Mots-clés français / French Keywords

Dihydropyridine dérivé ; Antagoniste calcium ; Forme pharmaceutique ; Volontaire ; Homme ; Voie orale ; Dose unique ; Formulation ; Nifédipine ; Forme libération contrôlée ; Pharmacocinétique ;

Mots-clés espagnols / Spanish Keywords

Dihidropiridine derivado ; Antagonista calcio ; Forma farmacéutica ; Voluntario ; Hombre ; Vía oral ; Dosis única ; Formulación ; Nifedipino ; Forma liberación controlada ; Farmacocinética ;

Localisation / Location

INIST-CNRS, Cote INIST : 17208, 35400013217527.0040