J Korean Soc Clin Pharmacol Ther.  2013 Dec;21(2):130-140. 10.12793/jkscpt.2013.21.2.130.

Steady-State Pharmacokinetic Properties of Tamsulosin in Healthy Male Volunteers

• Seong SJ
• Lee HW
• Lee J
• Lim MS
• Kim EH
• Park SM
• Gwon MR
• Yoon YR

• KMID: 2203226
• DOI: http://doi.org/10.12793/jkscpt.2013.21.2.130

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; AUCtau, 93.7 (31.5) and 88.2 (29.3) ng x h/mL; and t(1/2), 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 AUCtau (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 AUCtau 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

MeSH Terms

Administration, Oral
Cross-Over Studies
Healthy Volunteers
Humans
Male*
Pharmacokinetics
Plasma
Therapeutic Equivalency

Figure

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  Figure 1. Chemical structure of tamsulosin.

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  Figure 2. Mean (SD) plasma tamsulosin concentration-time profiles after administration of multiple 0.2-mg/day doses of two formulations of tamsulosin in 41 healthy Korean male volunteers.

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