Table 3.
Pharmacokinetics of S807 in Male and Female Sprague-Dawley Rats.
| Route | Dose (mg/kg bw) | Sex | Cmax (ng/mL) | AUClast (ng·hr/mL) | Tmax (hr) | t1/2 (hr) | Cmax Ratioa | AUClast Ratiob | %F |
|---|---|---|---|---|---|---|---|---|---|
| iv | 1 | M | 1110 ± 237 | 491 ± 33.3 | 0.033 | 3.02 ± 0.24 | – | – | – |
| F | 949 ± 222 | 342 ± 81.4 | 0.033 | 3.02 ± 0.92 | – | – | – | ||
| oral gavage | 20 | M | 174 ± 95.1 | 182 ± 70.5 | 0.313 | 1.14 ± 0.35 | 1 | 1 | 1.85% |
| F | 187 ± 87.6 | 166 ± 72.2 | 0.25 | 1.07 ± 0.67 | 1 | 1 | 2.43% | ||
| 50 | M | 1270 ± 1170 | 4890 ± 4960 | 1.50 | 1.83 ± 0.61 | 7.30 | 26.9 | 19.9% | |
| F | 529 ± 379 | 1410 ± 1020 | 1.0 | 1.17 ± 0.16 | 2.83 | 8.49 | 8.25% | ||
| 200 | M | 10500 ± 937 | 101000 ± 19500 | 4.0 | 2.49 ± 0.07 | 60.3 | 555 | 102.9% | |
| F | 9150 ± 2410 | 108000 ± 27900 | 3.0 | 2.62 ± 0.20 | 48.9 | 651 | 157.9% |
Male rat: CL = 30.7 mL/min/kg; Vss = 4630 mL/kg.
Female rat: CL = 47.2 mL/min/kg; Vss = 5610 mL/kg.
CL = clearance; Vss = steady-state volume of distribution; %F = bioavailability.
a
Cmax Ratio = Cmax/Cmax at 20 mg/kg bw dose.
b
AUClast Ratio = AUClast/AUClast at 20 mg/kg bw dose.