Table 1.
Mean (±SD) pharmacokinetic parameters of fospropofol following fospropofol administration in rats
| Route | Dose (mg/kg) | Cmax (µg/mL) | AUC(0−t) (µg h/mL) | AUC0−∞ (µg h/mL) | T1/2 (h) | Vd (L/kg) | CLp (L/h/kg) | Fa (%) |
|---|---|---|---|---|---|---|---|---|
| IV | 5 | 16.3 (±1.80) | 3.15 (±0.29) | 3.15 (±0.28) | 0.49 (±0.28) | 1.02 (±0.66) | 1.38 (±0.125) | – |
| PO | 20 | 0.23 (±0.07) | 0.05 (±0.008) | 0.06 (±0.007) | 0.19 (±0.27) | – | – | 0.448 |
| PO | 100 | 9.23 (±4.09) | 2.16 (±0.99) | 2.18 (±0.99) | 0.49 (±0.24) | – | – | 3.46 |
| ID | 30 | 0.17b | 0.044 | 0.05 | 0.21nd | – | – | 0.264 |
| ID | 100 | 3.74 (±2.12) | 0.644 (±0.38) | 0.65 (±0.39) | 0.23 (±0.1) | – | – | 1.03 |
nd not determined as only one rat showed terminal elimination.
aRatio of mean of AUC(0−∞) to reference treatment of 5 mg/kg IV fospropofol.
bN = 1.