Table 7.
Brain Penetration Analysisa
| route | time (h) | brain conc. (ng/g) | plasma conc. (ng/g) | brain/plasma ratio |
|---|---|---|---|---|
| 15b IV | 0.25 | 198 ± 32 | 3668 ± 845 | 0.05 ± 0.01 |
| 1 | 62 ± 20 | 1175 ± 526 | 0.06 ± 0.04 | |
| 24f IV | 0.25 | 124 ± 26 | 6103 ± 265 | 0.02 ± 0.003 |
| 1 | 9.0 ± 0.8 | 376 ± 26 | 0.02 ± 0.001 |
a
Values are mean ± SD from n = 3 biological replicates.
Concentrations of compounds 15b and 24f in the brain and plasma were determined at 0.25 and 1 h after a single dose of 10 mg/kg by IV. Formulation: DMSO:20% HP-β-CD in saline = 1:9.