Comparison of Pharmacokinetic Characteristics and the Safety between Amlodipine Maleate Tablet 5 mg and Amlodipine Besylate Tablet 5 mg.
10.12793/jkscpt.2012.20.1.42
- Author:
Hee Youn CHOI
1
;
Jae Woo KIM
;
Hyeong Seok LIM
;
Sang Heon CHO
;
Jong Lyul GHIM
;
Sangmin CHOE
;
Jin Ah JUNG
;
Jonglae LIM
;
Kyun Seop BAE
Author Information
1. Department of Clinical Pharmacology and Therapeutics, Asan Medical Center, Seoul, Korea. ksbae@amc.seoul.kr
- Publication Type:Original Article ; Randomized Controlled Trial
- Keywords:
Amlodipine maleate;
Amlodipine besylate;
Pharmacokinetics
- MeSH:
Amlodipine;
Calcium Channels;
Cross-Over Studies;
Dihydropyridines;
Electrocardiography;
gamma-Aminobutyric Acid;
Humans;
Hypertension;
Male;
Maleates;
Mass Spectrometry;
Physical Examination;
Plasma;
Salts;
Vital Signs
- From:Journal of Korean Society for Clinical Pharmacology and Therapeutics
2012;20(1):42-50
- CountryRepublic of Korea
- Language:Korean
-
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.
