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2012 (v.20 no.1)

The Journal of Korean Society for Clinical Pharmacology and Therapeutics

Korean Society for Clinical Pharmacology and Therapeutics
ISSN: 1225-5467

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

    Hee Youn Choi, Jae Woo Kim, Hyeong-Seok Lim, Sang-Heon Cho, Jong-Lyul Ghim, Sangmin Choe, Jin Ah Jung, Jonglae Lim, Kyun-Seop Bae

    J Korean Soc Clin Pharmacol Ther | v.20, no.1, pp.42-50, Jun, 2012


    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.


    Amlodipine maleate, Amlodipine besylate, Pharmacokinetics