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Arzneimittelforschung 2008; 58(7): 323-327
DOI: 10.1055/s-0031-1296514
Cardiac Drugs · Cardiac Stimulants · Coronary Drugs
Editio Cantor Verlag Aulendorf (Germany)

Comparative Pharmacokinetics of a Single Oral Dose of Two Formulations of Amlodipine

A randomized, single-blind, two-period, two-sequence, crossover study
Jose Carlos Pico
1   Clinical Pharmacology Unit, Hospital de Clínicas, Medical School, Buenos Aires University, Buenos Aires, Argentina
,
Graciela Domínguez
1   Clinical Pharmacology Unit, Hospital de Clínicas, Medical School, Buenos Aires University, Buenos Aires, Argentina
,
Armando Luis Negri
2   Medical Research Department, Laboratorios Casasco, Buenos Aires, Argentina
,
Juan Carlos Caubet
2   Medical Research Department, Laboratorios Casasco, Buenos Aires, Argentina
,
Norberto Antonio Terragno
1   Clinical Pharmacology Unit, Hospital de Clínicas, Medical School, Buenos Aires University, Buenos Aires, Argentina
› Author Affiliations
Further Information

Publication History

Publication Date:
15 December 2011 (online)

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Abstract

Amlodipine, a long acting dihydropyridine calcium channel antagonist, is prescribed worldwide for the treatment of angina and hypertension. The objective of this study was to compare the pharmacokinetics and to establish bioequivalence of two formulations of amlodipine. The study was performed at the Clinical Pharmacology Unit, Hospital de Clínicas, Medical School of Buenos Aires University. This randomized, single blind, two-period, two-sequence, comparative crossover study was conducted in 24 Caucasian healthy volunteers. A single oral 10 mg dose of amlodipine besylate (CAS 111470-99-6) test formulation and reference formulation were administered to the volunteers separated by a 3-week washout period in a crossover manner. Blood samples for pharmacokinetic analysis were collected over a period of 144 h after drug administration. Amlodipine was measured in plasma samples using a validated HPLC method with LC-MS-MS detection. A non-compartmental method was used for pharmacokinetic analysis. Bioequivalence between test and reference amlodipine samples were demonstrated as the calculated 90% confidence interval for the corresponding ratios of log transformed pharmacokinetic parameters (AUCt, AUC∞ and Cmax) fell within the 80–125% range, the predetermined criterion for pharmacokinetic equivalence.

Key words

Amlodipine besylate, bioequivalence, pharmacokinetics - Calcium channel antagonists, dihydropyridine - CAS 111470-99-6
 

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