Table 3. In vivo pharmacokinetic parameters.
| After IV administration of 10 mg/kg | After oral administration of 100 mg/kg | |||||||
| Compound | t½ (h) | CL (L/h/kg) | Vd (L/kg) | fe (%) | Cmax (mg/L) | Cmin,24 h (mg/L) | AUC0-∞ (mg h/L) | F (%) |
| 9a Ref | 10.3 (1.4) | 0.46 (0.07) | 6.72 (1.10) | 0.04 (0.01) | 0.85 (0.80) | 0.17 (0.16) | 10.2 (9.1) | 4.56 (4.06) |
| 9b | 2.48 (0.62) | 0.42 (0.15) | 1.53 (0.36) | 0.01 (0.00) | 2.31 (0.62) | 0.11 (0.11) | 15.1 (7.1) | 8.00 (3.93) |
| 9c | 5.60 (0.45) | 0.41 (0.06) | 1.69 (0.27) | 0.02 (0.00) | 0.15 (0.06) | 0.02 (0.02) | 1.61 (0.83) | 0.83 (0.57) |
Pharmacokinetic analysis of experimental compounds in rats.
Values represent means (% coefficient of variation).
Abbreviations: t½: half life; CL: clearance; Vd: volume of distribution; fe: fraction excreted unchanged in urine; Cmax: maximum plasma concentration; Cmin,24h: minimum plasma concentration within 24 hours after dosing; AUC0-∞: systematic exposure; F: oral bioavailability.