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(infinity): 409.99 +/- 61.08 ng/h/ml; A(half-life): 2.26 +/- 0.36 h; Dhalf-life: 2.43 +/- 0.44 h; Ehalf-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.

Pharmacokinetics of a new extended-release nifedipine formulation following a single oral dose, in human volunteers / Cainazzo, Maria Michela; Pinetti, Diego; G., Savino; M., Bartiromo; A., Forgione; Bertolini, Alfio. - In: DRUGS UNDER EXPERIMENTAL AND CLINICAL RESEARCH. - ISSN 0378-6501. - STAMPA. - 31 (3):(2005), pp. 115-121.

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

CAINAZZO, Maria Michela;PINETTI, Diego;BERTOLINI, Alfio
2005

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(infinity): 409.99 +/- 61.08 ng/h/ml; A(half-life): 2.26 +/- 0.36 h; Dhalf-life: 2.43 +/- 0.44 h; Ehalf-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.
31 (3)
115
121
Pharmacokinetics of a new extended-release nifedipine formulation following a single oral dose, in human volunteers / Cainazzo, Maria Michela; Pinetti, Diego; G., Savino; M., Bartiromo; A., Forgione; Bertolini, Alfio. - In: DRUGS UNDER EXPERIMENTAL AND CLINICAL RESEARCH. - ISSN 0378-6501. - STAMPA. - 31 (3):(2005), pp. 115-121.
Cainazzo, Maria Michela; Pinetti, Diego; G., Savino; M., Bartiromo; A., Forgione; Bertolini, Alfio
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11380/305408
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