Pharmacokinetics and urinary excretion of eprosartan in Chinese healthy volunteers of different gender.
The study aims to evaluate the pharmacokinetics and urinary excretion of eprosartan in Chinese healthy volunteers and to study the effect of gender on pharmacokinetics of eprosartan. Twenty healthy volunteers (ten men and ten women) were recruited for an open trial and received a single dose of 600 mg eprosartan. Using a validated LC/MS/MS method, plasma and urinary concentrations of eprosartan were determined. The following pharmacokinetic parameters were elucidated after administration: the area under the plasma concentration versus time curve from 0 to 32 h (AUC0-32h) 14818.75 +/- 7312.11 ng x h/mL, the area under the plasma concentration versus time curve from 0 to infinite (AUC(0-infinity)) 15081.62 +/- 7379.63 ng x h/mL, peak plasma concentration (Cmax) 3664.25 x 1653.94 ng x h/mL, time to Cmax (Tmax) 1.63 +/- 0.46 h, elimination half-life (t(1/2)) 8.03 +/- 4.04 h, apparent clearance (CL/F) 47.84 +/- 19.21 L/h, apparent volume of distribution of the central compartment (V/F) 537.21 +/- 287.91 L, renal clearance (CLr) 1.33 +/- 0.41 L/h, amount of unchanged eprosartan excreted into urine 18.44 +/- 6.43 mg and fraction of unchanged eprosartan excreted into urine 3.07 +/- 1.07%. Our results also indicated that no gender differences were observed in the pharmacokinetics of eprosartan in Chinese healthy volunteers.
Xu
H R
HR
Department of Clinical Pharmacology, ZhongShan Hospital, Fudan University, 180 Fen Lin Road, Shanghai 200032, PR China. hrongxu@sohu.com
Chen
W L
WL
Li
X N
XN
Liu
G Y
GY
Chu
N N
NN
Yu
C
C
D000179:Acrylates / Q000493:pharmacokinetics* / Q000652:urine; D000328:Adult; D000959:Antihypertensive Agents / Q000493:pharmacokinetics* / Q000652:urine; D019540:Area Under Curve; D004562:Electrocardiography; D005260:Female; D006207:Half-Life; D006801:Humans; D007093:Imidazoles / Q000493:pharmacokinetics* / Q000652:urine; D008297:Male; D012727:Sex Characteristics; D013876:Thiophenes / Q000493:pharmacokinetics* / Q000652:urine
D000179:Acrylates; D000959:Antihypertensive Agents; D007093:Imidazoles; D013876:Thiophenes; C068373:eprosartan