Plasma pharmacokinetics (data presented as means ± S.D.) following a bolus i.v. (1 mg/kg) and p.o. (5 mg/kg) administration to Sprague Dawley rats (n = 3/group)
Intravenous parameters include total clearance (CL), volume of distribution (Vss), half-life (t1/2), and brain uptake over time (Kin). Oral parameters include maximal plasma concentration (Cmax), area under the curve (AUC), time to maximal plasma concentration (Tmax), and percentage oral availability (F).
| Test article | i.v. | p.o. | ||||||
|---|---|---|---|---|---|---|---|---|
| CL | Vss | t1/2 | Kin | Cmax | AUCinf | Tmax | F | |
| ml/min/kg | l/kg | h | ml/min | ng/ml | min*ng/ml | h | % | |
| Oxycodone | 49.2 ± 7.1 | 1.72 ± 0.25 | 0.76 ± 0.25 | 0.124 | 53.9 ± 45.1 | 75.6 ± 64.0 | 0.3 ± 0.1 | 4.40 ± 3.7 |
| NKTR-181 | 59.3 ± 8.1 | 4.19 ± 0.70 | 4.53 ± 1.10 | 0.007 | 100.7 ± 18.4 | 483.3 ± 97.9 | 1.8 ± 1.3 | 34.0 ± 6.9 |