Table 5. Pharmacokinetic Properties of 24 and 25a.
| Compound | Species | Dose (mg/kg) | Route | C0 (ng/mL) | AUC0-t (h × ng/mL) | VD (mL/kg) | CL (mL/h/kg) | T1/2 (h) | Cmax (ng/mL) | AUC0-t (h × ng/mL) | Tmax (h) | %F |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 24 | Mice | 3 | iv | 7482 | 5274 | 661 | 556 | 2.6 | ||||
| 25 | 788 | 928 | 5573 | 3134 | 0.8 | |||||||
| 24 | 10 | po | 6618 | 12464 | 0.5 | 71 | ||||||
| 25 | 2531 | 4489 | 0.3 | 100 | ||||||||
| 24 | Rat | 3 | iv | 27659 | 111567 | 2000 | 24 | 5.3 | ||||
| 24 | 10 | po | 22147 | 171258 | 1.2 | 46 | ||||||
| 24 | Dog | 1 | iv | 1963 | 6064 | 500 | 186 | 2.6 | ||||
| 24 | 10 | po | 12823 | 86465 | 1.17 | 100 |
a
Values represented as mean with sparse sampling technique. iv formulation (solution) includes 10% v/v ethanol, 30% v/v PEG, and 60% v/v water. po formulation (suspension) contains 50 parts of 1% v/v Tween 20 in water and 50 parts of 0.5% w/v hydroxy ethyl cellulose.