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2012 (v.20 no.2)

The Journal of Korean Society for Clinical Pharmacology and Therapeutics

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

  • Bioequivalence and Dose Proportionality of Olmesartan Medoxomil Formulations

    Sung Kweon Cho, Choon Ok Kim, Su Hyun Yu, Eun Sil Oh, Seong Bok Jang, Yoong Sik Park, Kyunghee Cho, Jae-Yong Chung

    J Korean Soc Clin Pharmacol Ther | v.20, no.2, pp.145-154, Dec, 2012

    Abstract

    Background: Olmesartan medoxomil is an angiotensin II receptor blocker commonly used in
    hypertension. First objective of this study was to evaluate the bioequivalence of two olmesartan
    formulations, Olmesartan 20 mg and 40 mg tablet (Yuhan, Pharmaceutical Corp. Seoul, Korea) as test
    drugs and Olmetec® 20 mg and 40 mg tablet (Daewoong, Pharmaceutical Corp. Seoul, Korea) as reference
    drugs. Second objective of this study was to evaluate the dose-proportionality of two formulations.
    Methods: Two studies (20 mg, 40 mg) were conducted as a randomized, open-label, 2-period, crossover
    design. Each subject received one 20 mg or 40 mg tablet of the reference or test formulation of
    olmesartan medoxomil in each study. Blood samples were obtained during the 48-hour period after the
    dose in each treatment period. Wash-out period was 1 week in each study. Concentrations of olmesartan
    medoxomil in plasma were analyzed using a liquid chromatography system with tandem
    mass-spectrometric detection (LC/MS/MS). The primary pharmacokinetic parameters were Cmax
    (maximum concentration) and AUCt (area under the concentration-time curve from time 0 to the last
    sampling time).
    Results: A total number of 40 healthy male volunteers participated in the study and 37 volunteers
    completed both treatment periods in 20 mg trial. All 40 participants completed both treatment periods in
    40 mg trial. The 90 % CIs for the geometric mean ratios of the pharmacokinetic parameters
    (test:reference drug) were 0.93 ~ 1.04 for AUCt and 0.97 ~ 1.08 for Cmax in 20 mg trial. The 90 CIs were
    0.94 ~ 1.02 for AUCt and 1.00 ~ 1.11 for Cmax in 40 mg trial. All parameters of two studies satisfy the
    range of bioequivalence criterion.
    Conclusion: The obtained results indicated that pharmacokinetic exposure to Olmesartan 20 mg and 40
    mg tablet was bioequivalent to that of Olmetec® 20 mg and 40 mg tablet, respectively.

    Keyword

    Olmesartan, Bioequivalence, Dose proportionality