Table 7. Pharmacokinetic Parameters of 8 and Its Metabolites 2 and 17 Following a Single PO Dose of 300 mg/kg 8 With and Without PO Pre-treatment With 1000 mg/kg Mesalamine in Male Hamstersa.
| 300 mg/kg PO
(vehicle) |
300 mg/kg PO
(mesalamine) |
|||||
|---|---|---|---|---|---|---|
| PK parameter | 8 | 2 | 17 | 8 | 2 | 17 |
| AUC0–inf [ng*h/mL] | 464 ± 152 | b | 5820 ± 537 | 1090 ± 377 | 5580c | 9370c |
| AUC0–t [ng*h/mL] | 434 ± 158 | 4390 ± 1120 | 5520 ± 239 | 1030 ± 406 | 7030 ± 1556 | 7480 ± 328 |
| t1/2 [h] | 3.07 ± 1.08 | b | 5.24c | 4.97 ± 0.94 | 3.97c | 8.10c |
| tmax [h] | 0.19 ± 0.06 | 6.67 ± 0.67 | 4.67 ± 0.67 | 0.50 | 1.00 ± 0.50 | 6.00 ± 2.00 |
| Cmax [ng/mL] | 171 ± 90.5 | 476 ± 27.4 | 397 ± 41.3 | 372 ± 134 | 586 ± 19.0 | 483 ± 25.4 |
| MRTinf [h] | 4.07 ± 1.20 | b | 8.25c | 5.00 ± 0.65 | 6.73c | 11.7c |
a
Each value in the table is the mean of three experiments (n = 3), error is reported as SEM.
b
Not calculated; there was insufficient data to define the elimination phase.
c
SEM values were not calculated since AUC extrapolated was greater than 25% in one subject.