Table 3. Pharmacokinetic Parameters of 8, 2, and 17 After Administration of 8 in SD Ratsa.
| 5 mg/kg IV |
300 mg/kg PO |
|||||
|---|---|---|---|---|---|---|
| PK parameter | 8 | 2 | 17 | 8 | 2 | 17 |
| AUC0–inf [ng*h/mL] | 499 ± 30.4 | 509 ± 36.6 | 1070 ± 36.06 | 577 ± 116 | 9560b | 13,700b |
| AUC0–t [ng*h/mL] | 493 ± 31.5 | 502 ± 34.9 | 1052 ± 41.74 | 513 ± 119 | 8023 ± 991 | 12,330 ± 3001 |
| t1/2 [h] | 0.14 ± 0.02 | 0.35 ± 0.02 | 0.84 ± 0.18 | 1.54 ± 0.28 | 3.66b | 3.03b |
| tmax [h] | 0.08 | 0.25 | 0.25 | 0.25 | 2.0 ± 1.0 | |
| Cmax [ng/mL] | 1180 ± 37.86 | 640 ± 48.7 | 219 ± 39.4 | 2950 ± 241 | 1290 ± 86.6 | |
| C0 [ng/mL] | 3537 ± 231 | |||||
| CL [mL/min/kg] | 169 ± 8.41 | |||||
| MRTinf [h] | 0.13 ± 0.01 | 0.36 ± 0.03 | 1.2 ± 0.2 | 2.85 ± 0.86 | 4.41b | 5.76b |
| Vdss | 1.3 ± 0.1 | |||||
| F [%] | 31.4b | |||||
Each value in the table is the mean of three experiments (n = 3), error is reported as SEM.
SEM values were not calculated since AUC extrapolated was greater than 25% in one subject.