Journal of Korean Society for Clinical Pharmacology and Therapeutics (임상약리학회지)

Korean Society for Clinical Pharmacology and Therapeutics (대한임상약리학회)
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Comparison of Pharmacokinetic Characteristics and the Safety between Amlodipine Maleate Tablet 5 mg and Amlodipine Besylate Tablet 5 mg

말레인산 암로디핀 정 5 mg과 베실산 암로디핀 정 5 mg의 약동학 특성 및 안전성 비교

  • Choi, Hee-Youn (Department of Clinical Pharmacology and Therapeutics, Asan Medical Center) ;
  • Kim, Jae-Woo (Department of Clinical Pharmacology and Therapeutics, Asan Medical Center) ;
  • Lim, Hyeong-Seok (Department of Clinical Pharmacology and Therapeutics, Asan Medical Center) ;
  • Cho, Sang-Heon (School of Military Medicine, The First Republic of Korea Army) ;
  • Ghim, Jong-Lyul (Department of Clinical Pharmacology and Therapeutics, Inje University Pusan Paik Hospital) ;
  • Choe, Sang-Min (Division of Clinical Pharmacology, Clinical Trials Center, Pusan National University Hospital) ;
  • Jung, Jin-Ah (Division of Clinical Pharmacology, Clinical Trial Center, Samsung Medical Center) ;
  • Lim, Jong-Lae (Technical research center, CKD research institute, Chong Kun Dang Pharmaceutical Co., Ltd.) ;
  • Bae, Kyun-Seop (Department of Clinical Pharmacology and Therapeutics, Asan Medical Center)
  • 최희연 (서울아산병원 임상약리학과) ;
  • 김재우 (서울아산병원 임상약리학과) ;
  • 임형석 (서울아산병원 임상약리학과) ;
  • 조상헌 (국군의무학교) ;
  • 김종률 (인제대학교 부산백병원 임상약리학과) ;
  • 최상민 (부산대학교병원 임상시험센터 임상약리실) ;
  • 정진아 (삼성서울병원 임상시험센터 임상약리학과) ;
  • 임종래 (종근당 효종연구소) ;
  • 배균섭 (서울아산병원 임상약리학과)
  • Received : 2011.12.01
  • Accepted : 2012.05.12
  • Published : 2012.06.30
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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 $C_{max}$ and $AUC_{last}$ 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.

Keywords

Acknowledgement

Supported by : 종근당(주)

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