Table 5.
Pharmacokinetic parameters of darunavir in brain and plasma after administration by nasal (optimized in situ gel, 30 µL, 2.4 mg/kg) and intravenous (solution, 0.4 mL, 2.4 mg/kg) routes in Sprague Dawley rats. The data presented are the average of six animals at every time point.
| Parameters | Brain | Plasma | ||
|---|---|---|---|---|
| Nasal | Intravenous | Nasal | Intravenous | |
| Tmax a | 1 h | 2 h | 2 h | - |
| Cmax b | 260.02 ± 17.71 * (ng/g) | 70.10 ± 5.07 (ng/g) | 64.99 ± 14.28 * (ng/mL) | 390.59 ± 32.61 (ng/mL) |
| AUC0-α c | 1127.08 ± 267.72 * (ng·h/g) | 325.84 ± 88.21 (ng·h/g) | 414.25 ± 128.87 * (ng·h/mL) | 1403.39 ± 303.82 (ng·h/mL) |
| AUC brain/AUC plasma | 2.72 | 0.23 | - | - |
* Significant difference (p < 0.0001) detected in darunavir level in the nasal group compared to intravenous. a time to reach maximum plasma concentration; b maximum plasma drug concentration; c area under the plasma drug concentration–time profile curve.