TABLE 2.
Pharmacokinetic parameters following oral administration of escalating doses of oral CRO formulation to ratsa
| Oral formulation | Cmax (μg/ml) | Tmax (h) | AUC0-8 h (μg · h/ml) | F (%) |
|---|---|---|---|---|
| CRO without CEA | ||||
| 50 mg/kg in PBS | 0.8 ± 0.3 | 0.5 | 0.9 ± 0.5 | 0.9 ± 0.5 |
| 50 mg/kg in 50% PG | 1.8 ± 0.3 | 0.5 | 4.6 ± 1.4 | 4.3 ± 1.3 |
| CRO/CEA in 50% PG | ||||
| 12.5 mg/kg | 3.5 ± 1.7 | 1.0 ± 0.3 | 7.7 ± 3.0 | 14.6 ± 5.7 |
| 25 mg/kg | 9.9 ± 3.9 | 1.1 ± 0.4 | 31.8 ± 15.1 | 30.3 ± 14.4 |
| 50 mg/kg | 22.9 ± 8.1 | 2.2 ± 1.0 | 118.0 ± 39.0 | 55.7 ± 18.7 |
a
Data are presented as means ± standard deviations (n = 5). Cmax, maximum concentration of drug in plasma; Tmax, time to maximum concentration of drug in plasma; AUC0-8 h, area under the concentration-time curve from 0 h to 8 h; F, oral bioavailability.