Comperative pharmacokinetic and pharmacodynamic characteristics of amlodipine besylate and amlodipine nicotinate in healthy subjects

J. Y. Park, K. A. Kim, P. W. Park, O. J. Lee, J. S. Kim, G. H. Lee, M. C. Ha, J. H. Park, M. J. O, J. H. Ryu

Research output: Contribution to journalArticlepeer-review

12 Citations (Scopus)


Background and aim: Amlodipine, a dihydropyridine calcium antagonist, is prescribed for the management of angina and hypertension, and is sold as amlodipine besylate. However, a new salt formulation, amlodipine nicotinate, has recently been developed. Here, we evaluated the comparative pharmacokinetic and pharmacodynamic characteristics of the nicotinate and besylate forms of amlodipine. Subjects and methods: A randomized, 2-way crossover study was conducted in 18 healthy male volunteers to compare the pharmacokinetics and pharmacodynamics of these two forms, i.e. amlodipine nicotinate (test) and amlodipine besylate (reference), after administration of a single dose of 5 mg of each drug and a washout period between doses of 4 weeks. Blood samples for the pharmacokinetic analysis of amlodipine were obtained over the 144-hour period after administration. Systolic and diastolic blood pressures and pulse rates were recorded immediately prior to each blood sampling. Results: All participants completed both treatment periods, and no serious adverse events occurred during the study period. After administering a single dose of each formulation, mean AUC0-∞ and Cmax values were 190.91 ± 60.49 ng × h/ml and 3.87 ± 1.04 ng/ml for the test formulation and 203.15 ± 52.05 ng × h/ml and 4.01 ± 0.60 ng/ml for the reference formulation, respectively. The 90% confidence intervals of test/reference mean ratios for AUC0-∞ and Cmax fell within the predetermined equivalence range of 80 - 125%. Pharmacodynamic profiles including systolic and diastolic blood pressures and pulse rates exhibited no significant differences between the two formulations. Conclusion: The two amlodipine formulations showed similar pharmacokinetic and pharmacodynamic characteristics and the new amlodipine formulation, amlodipine nicotinate, was found to be equivalent for pharmacokinetics to the currently available amlodipine besylate with respect to the rate and extent of amlodipine absorption.

Original languageEnglish
Pages (from-to)641-647
Number of pages7
JournalInternational journal of clinical pharmacology and therapeutics
Issue number12
Publication statusPublished - 2006 Dec
Externally publishedYes


  • Amlodipine
  • Bioavailability
  • Pharmacodynamics
  • Pharmacokinetics
  • Salt substitution

ASJC Scopus subject areas

  • General Medicine


Dive into the research topics of 'Comperative pharmacokinetic and pharmacodynamic characteristics of amlodipine besylate and amlodipine nicotinate in healthy subjects'. Together they form a unique fingerprint.

Cite this