Transl Clin Pharmacol.  2020 Jun;28(2):92-101. 10.12793/tcp.2020.28.e8.

Pharmacokinetics and bioequivalence of fixed-dose combination of candesartan cilexetil/amlodipine besylate (16/10 mg) versus coadministration of individual formulations in healthy subjects

Affiliations
  • 1School of Medicine, Kyungpook National University and Department of Clinical Pharmacology, Kyungpook National University Hospital, Daegu 41566, Korea
  • 2Division of Cardiology, Department of Internal Medicine, Kyungpook National University Hospital, Daegu 41944, Korea
  • 3College of Nursing, Daegu Catholic University, Gyeongsan 38430, Korea
  • 4Analytical Research Division, Biocore Co. Ltd., Seoul 08511, Korea

Abstract

This study compared the pharmacokinetics of a fixed-dose combination (FDC) of candesartan (16 mg) and amlodipine (10 mg) versus coadministration of individual formulations to clarify the bioequivalence of the FDC. In this randomized, open-label, single-dose, 2-treatment, 2-way crossover study, healthy Korean volunteers received a single dose of candesartan (16 mg) with amlodipine (10 mg) as either an FDC or single agents concomitantly administered, with a 2-week washout period. Serial blood samples were collected up to 72 hours after dosing for each treatment period, and plasma concentrations of candesartan and amlodipine were measured using a validated liquid chromatography-tandem mass spectrometry method. A total of 39 subjects completed the study. The geometric mean ratios (GMRs) and 90% confidence intervals (CIs) for the area under the plasma concentration-time curve from time 0 to the last measurement (AUC0-t) and the peak plasma concentration (Cmax) for candesartan were 1.0182 (0.9562–1.0841) and 0.9492 (0.8726–1.0324), respectively. The GMR and 90% CI for the AUC0-t and Cmax for amlodipine were 1.0552 (1.0255–1.0857) and 1.0668 (1.0259–1.1094), respectively. In conclusion, the new FDC formulation of candesartan (16 mg) and amlodipine (10 mg) was bioequivalent to the concomitant administration of single agents. A single dose of candesartan/amlodipine as the FDC or as single agents was well tolerated.

Keyword

Hypertension; Pharmacokinetics; Bioequivalence; Candesartan; Amlodipine
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