Pharmacokinetic parameters and urinary excretion1-a of penciclovir and M4 following single oral administrations of SK18991-b and famciclovir1-c
| Compound | Rat | Dog | |||||
|---|---|---|---|---|---|---|---|
| Famciclovir | SK1899 | Famciclovir | SK1899 | ||||
| 0.2 | 0.2 | 2 | 0.034 | 0.034 | 0.68 | ||
| T max (h) | Penciclovir | 0.5 ± 0.01-d | 0.5 ± 0.0 | 1.4 ± 0.3 | 2.0 ± 0.01-d | 2.7 ± 0.6 | 4.0 ± 0.0 |
| M4 | 0.3 ± 0.1 | 0.4 ± 0.1 | 0.8 ± 0.5 | 0.7 ± 0.3 | 1.0 ± 0.0 | 2.2 ± 0.8 | |
| C max(μM) | Penciclovir | 34.0 ± 3.8 | 39.5 ± 5.2 | 113.1 ± 17.5 | 5.0 ± 1.2 | 4.5 ± 1.3 | 29.1 ± 9.1 |
| M4 | 46.8 ± 10.6 | 49.9 ± 5.4 | 302.8 ± 73.1 | 23.8 ± 3.6 | 30.1 ± 6.1 | 588.1 ± 86.3 | |
| AUC0-∞ (μM·h) | Penciclovir | 54.5 ± 6.2 | 57.5 ± 7.7 | 369.3 ± 83.6 | 27.9 ± 9.6 | 28.2 ± 11.1 | 236.4 ± 88.1 |
| M4 | 36.7 ± 3.5 | 36.6 ± 1.9 | 682.2 ± 154.4 | 54.2 ± 1.1 | 65.1 ± 6.6 | 2226.2 ± 330.1 | |
| t 1/2 (h) | Penciclovir | 0.9 ± 0.1 | 0.8 ± 0.1 | 2.1 ± 0.5 | 2.0 ± 0.3 | 2.1 ± 0.3 | 3.1 ± 1.0 |
| M4 | 0.3 ± 0.1 | 0.3 ± 0.0 | 0.9 ± 0.2 | 1.1 ± 0.2 | 1.0 ± 0.1 | 1.2 ± 0.2 | |
| Excretion (% dose) | Penciclovir | 35.5 ± 0.7 | 36.1 ± 0.8 | 23.2 ± 2.7 | 38.0 ± 3.2 | 36.3 ± 3.4 | 14.1 ± 1.2 |
| M4 | 24.0 ± 3.3 | 26.5 ± 2.4 | 40.2 ± 1.8 | 30.2 ± 2.4 | 33.3 ± 2.6 | 52.8 ± 2.3 | |
↵1-a Urine was collected for 24 h after dosing and analyzed by HPLC.
↵1-b SK1899 was administered at 0.2 or 2 mmol/kg to rats and 0.034 or 0.68 mmol/kg to dogs.
↵1-c Famciclovir was administered at 0.2 and 0.034 mmol/kg to rats and dogs, respectively.
↵1-d Each value represents the mean ± S.D. of four animals for the rat and three animals for the dog.