TABLE 1. Pharmacokinetics of S-1 in male Sprague-Dawley rats after i.v. and p.o. administration.
Pharmacokinetics | Unit | 0.1 mg/kg | 1 mg/kg | 10 mg/kg | 30 mg/kg |
---|---|---|---|---|---|
i.v. | |||||
t1/2 | min | 217 | 241 | 248 | 315 |
MRT | min | 301 ± 20 | 348 ± 49 | 363 ± 51 | 442 ± 170 |
AUC | min · μg/ml | 20.4 ± 0.7 | 228 ± 32 | 2549 ± 267 | 8738 ± 2053 |
CL | ml/min/kg | 5.2 ± 0.2 | 4.4 ± 0.7 | 4.0 ± 0.5 | 3.6 ± 0.7 |
Vss | ml/kg | 1564 ± 149 | 1532 ± 227 | 1458 ± 352 | 1512 ± 216 |
p.o. | 0.1 mg/kg | 1 mg/kg | 10 mg/kg | 30 mg/kg | |
t1/2 | min | 322 | 255 | 219 | 254 |
MRT | min | 685 ± 131 | 542 ± 28 | 481 ± 43 | 625 ± 39 |
Tmax | min | 347 ± 126 | 276 ± 138 | 288 ± 133 | 510 ± 151 |
Cmax | μg/ml | 0.014 ± 0.004 | 0.18 ± 0.06 | 2.12 ± 0.19 | 5.01 ± 0.72 |
AUC | min · μg/ml | 12 ± 4 | 136 ± 19 | 1412 ± 218 | 4771 ± 350 |
CL/F | ml/min/kg | 9.5 ± 3.3 | 7.6 ± 1.0 | 7.2 ± 1.0 | 6.3 ± 0.5 |
Vz/F | ml/kg | 4699 ± 2546 | 2840 ± 468 | 2294 ± 383 | 2361 ± 468 |
Bioavailability | % | 59.6 | 58.0 | 54.9 | 55.7 |