J Korean Soc Clin Pharmacol Ther.  2012 Jun;20(1):42-50.

Comparison of Pharmacokinetic Characteristics and the Safety between Amlodipine Maleate Tablet 5 mg and Amlodipine Besylate Tablet 5 mg

Affiliations
  • 1Department of Clinical Pharmacology and Therapeutics, Asan Medical Center, Seoul, Korea. ksbae@amc.seoul.kr
  • 2University of Ulsan College of Medicine, Korea.
  • 3School of Military Medicine, The First Republic of Korea Army, Korea.
  • 4Department of Clinical Pharmacology and Therapeutics, Inje University Pusan Paik Hospital, Pusan, Korea.
  • 5Division of Clinical Pharmacology, Clinical Trials Center, Pusan National University Hospital, Korea.
  • 6Division of Clinical Pharmacology, Clinical Trial Center, Samsung Medical Center, Korea.
  • 7Technical research center, CKD research institute, Chong Kun Dang Pharmaceutical Co, Ltd, Korea.

Abstract

BACKGROUND
Amlodipine is a third-generation dihydropyridine calcium channel blocker for treating hypertension. Though marketed primarily as a besylate salt, there have been some efforts to find other comparable salts. Among them, maleate is the salt that has been considered favorable for many drugs. The aim of this study was to compare the pharmacokinetics, as well as safety and tolerability of amlodipine maleate with amlodipine besylate.
METHODS
This study was open, randomized, two-period crossover design investigated in twelve healthy male volunteers over a 144 h period after administrating two forms of amlodipine 5 mg, respectively. Each period was separated with 2 weeks. Plasma concentrations of amlodipine were determined by liquid chromatography-tandem mass spectrometry. Safety profiles were assessed by vital signs, physical examinations, electrocardiograms, laboratory testing and adverse events monitoring.
RESULTS
All subjects were completed this study. Geometric mean ratios (GMRs) of amlodipine maleate/amlodipine besylate of Cmax and AUClast for amlodipine were 0.92 (90 % confidence interval, 0.81 ~ 1.05) and 1.05 (0.96 ~ 1.16), respectively. No serious adverse events were reported, and no clinically relevant changes were observed in safety profiles during this trial.
CONCLUSION
Pharmacokinetics, tolerability and the safety were comparable between amlodipine maleate and amlodipine besylate in healthy individuals.

Keyword

Amlodipine maleate; Amlodipine besylate; Pharmacokinetics

MeSH Terms

Amlodipine
Calcium Channels
Cross-Over Studies
Dihydropyridines
Electrocardiography
gamma-Aminobutyric Acid
Humans
Hypertension
Male
Maleates
Mass Spectrometry
Physical Examination
Plasma
Salts
Vital Signs
Amlodipine
Calcium Channels
Dihydropyridines
Maleates
Salts
gamma-Aminobutyric Acid
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