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KMID : 0391020130210020130
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Journal of Korean Society for Clinical Pharmacology and Therapeutics
2013 Volume.21 No. 2 p.130 ~ p.140
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Steady-State Pharmacokinetic Properties of Tamsulosin in Healthy Male Volunteers
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Seong Sook-Jin
Lee Hae-Won
Lee Joo-Mi
Lim Mi-Sun
Kim Eun-Hee
Park Sung-Min
Gwon Mi-Ri
Yoon Young-Ran
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Abstract
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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.
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KEYWORD
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Fasted state, Healthy volunteers, Multiple-dose, Pharmacokinetics, Tamsulosin
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