TABLE 2

Effects of dosing vehicle on pharmacokinetic parameters of S-1 at the dose level of 10 mg/kg in male Sprague-Dawley rats (n = 5/dose group)

Dosing Vehicle
Unit
10 mg/kg
10% Ethanol in PEG-300
5% DMSO in PEG-300
i.v.
    t1/2 min 330 248
    MRT min 434 ± 63 363 ± 51
    AUC min · μg/ml 2009 ± 413 2549 ± 267
    CL ml/min/kg 5.1 ± 1.1 4.4 ± 0.5
    Vss
ml/kg
2214 ± 486
1458 ± 352
10 mg/kg
5% Ethanol in PEG-300
5% DMSO in PEG-300
p.o.
    t1/2 min 283 219
    MRT min 502 ± 88 481 ± 43
    Tmax min 106 ± 89 288 ± 133
    Cmax μg/ml 2.97 ± 0.15 2.12 ± 0.19
    AUC min · μg/ml 1860 ± 249 1412 ± 218
    CL/F ml/min/kg 5.3 ± 0.7 7.2 ± 1.0
    Vz/F ml/kg 2155 ± 179 2294 ± 383
Bioavailability
%
95.9
54.9