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KMID : 0391020120200010042
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Journal of Korean Society for Clinical Pharmacology and Therapeutics
2012 Volume.20 No. 1 p.42 ~ p.50
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Comparison of Pharmacokinetic Characteristics and the Safety between Amlodipine Maleate Tablet 5mg and Amlodipine Besylate Tablet 5mg
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Choi Hee-Youn
Kim Jae-Woo
Lim Hyeong-Seok
Cho Sang-Heon
Ghim Jong-Lyul
Choe Sang-Min
Jung Jin-Ah
Im Jong-Lae
Bae Kyun-Seop
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Abstract
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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 and 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.
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KEYWORD
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Amlodipine maleate, Amlodipine besylate, Pharmacokinetic
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