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2013 (v.21 no.2)

The Journal of Korean Society for Clinical Pharmacology and Therapeutics

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

  • Steady-State Pharmacokinetic Properties of Tamsulosin in Healthy Male Volunteers

    Sook Jin Seong, Hae Won Lee, Joomi Lee, Mi-sun Lim, Eun Hee Kim, Sung Min Park, Mi-Ri Gwon, Young-Ran Yoon

    J Korean Soc Clin Pharmacol Ther | v.21, no.2, pp.130-140, Dec, 2013

    Abstract

    Background: To evaluate the pharmacokinetic properties of daily oral doses of tamsulosin administered
    to fasted healthy Korean male volunteers for 5 days.
    Methods: In a randomized, open-label, multiple-dose, two-period, crossover study, all 44 subjects were
    randomly assigned in a 1:1 ratio to receive a newly developed generic capsule formulation (test) or a
    branded capsule formulation (reference) of tamsulosin 0.2 mg, followed by a 10-day washout period and
    administration of the other formulation. Plasma concentrations of tamsulosin were assessed after
    administration of five-day multiple doses, using HPLC-MS/MS. Clinical and laboratory adverse events
    (AE) were assessed.
    Results: The mean (SD) pharmacokinetic properties with the test and reference formulations were as
    follows: Css, max , 9.0 (2.9) and 8.4 (2.6) ng/mL, respectively; median (range) tmax, 4 (2-6) and 5 (2-7)
    hours; AUCτ, 93.7 (31.5) and 88.2 (29.3) ng × h/mL; and t½, 9.5 (2.6) and 10.0 (2.7) hours. The volume
    of distribution and clearance after oral administration of tamsulosin were 0.5 L/kg, and 0.04 L/h/kg,
    respectively. The accumulation ratios for 0.2 mg once-daily dosing regimen were 1.2. The 90% CIs of the
    geometric mean ratios for the log-transformed AUCτ (1.005-1.131) and Css, max (1.000-1.136) values were
    within the acceptable range for bioequivalence. No serious AE was reported during the study. Both
    formulations were well tolerated.
    Conclusion: The results demonstrate that the Css, max and AUCτ values in the fasted subjects were
    higher than those in the fed from other study, with a shorter tmax values.

    Keyword

    Fasted state, Healthy volunteers, Multiple-dose, Pharmacokinetics, Tamsulosin