Steady-State Pharmacokinetic Properties of Tamsulosin in Healthy Male Volunteers.
10.12793/jkscpt.2013.21.2.130
- Author:
Sook Jin SEONG
1
;
Hae Won LEE
;
Joomi LEE
;
Mi Sun LIM
;
Eun Hee KIM
;
Sung Min PARK
;
Mi Ri GWON
;
Young Ran YOON
Author Information
1. Department of Clinical Trial Center, Kyungpook National University Hospital, Daegu, Korea. yry@knu.ac.kr
- Publication Type:Original Article ; Randomized Controlled Trial
- Keywords:
Fasted state;
Healthy volunteers;
Multiple-dose;
Pharmacokinetics;
Tamsulosin
- MeSH:
Administration, Oral;
Cross-Over Studies;
Healthy Volunteers;
Humans;
Male*;
Pharmacokinetics;
Plasma;
Therapeutic Equivalency
- From:Journal of Korean Society for Clinical Pharmacology and Therapeutics
2013;21(2):130-140
- CountryRepublic of Korea
- Language:English
-
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.
