Mean ± S.D. steady-state pharmacokinetic parameters of CP-615,003 and CP-900,725 in plasma and CSF in healthy human volunteers on day 3 of multiple-dose administration of CP-615,003 at 100 mg b.i.d.
Pharmacokinetic Parameter | CP-615,003 | CP-900,725 |
|---|---|---|
| Plasma Cmax (ng/ml) | 173 ± 56 | 34.6 ± 5.4 |
| Plasma Tmax (h)a | 3.00 (2.00-4.00) | 4.00 (3.00-6.00) |
| Plasma AUC0-12 h (h · ng/ml) | 1052 ± 305 | 277 ± 63 |
| Plasma C4 h (ng/ml) | 140 ± 62 | 33.2 ± 6.3 |
| CSF C4 h (ng/ml) | 3.1 ± 0.7 | 0.529 ± 0.066 |
| CSF/Plasma Ratio | 0.024 ± 0.006 | 0.0166 ± 0.0047 |
| Ex Vivo Plasma fu | 0.233 ± 0.031 | 0.148 ± 0.029 |
| CSF/Cu | 0.104 ± 0.029*** | 0.116 ± 0.039*** |