Parameters | SACa | NAc-SACa | SACSa | NAc-SACSa | |
---|---|---|---|---|---|
i.v. | Oral | i.v. | i.v. | i.v. | |
Cmax (mg/l) | 3.2 ± 0.025 | 2.1 ± 0.14 | 9.7 ± 2.1 | 12 ± 3.3 | 11 ± 1.0 |
tmax (h) | — | 1.3 ± 0.58 | — | — | — |
t1/2 (h) | 12 ± 0.39 | 12 ± 1.2 | 11 ± 1.5 | 6.0 ± 0.28 | 3.9 ± 0.85 |
CL (l/h/kg) | 0.048 ± 0.006 | — | 0.11 ± 0.031 | 0.074 ± 0.010 | 0.20 ± 0.009 |
CLr (l/h/kg) | 0.0002 | — | 0.0019 | 0.0042 | 0.17 |
Vss (l/kg) | 0.83 ± 0.10 | — | 1.3 ± 0.10 | 0.51 ± 0.059 | 0.32 ± 0.023 |
Bioavailability (%) | — | 92.0 | — | — | — |
AUC (mg⋅h/l) | |||||
SAC | 42.1 ± 4.96 | 38.7 ± 3.46 | 27.6 ± 4.46 | n.d. | n.d. |
NAc-SAC | 24.4 ± 6.09 | 22.7 ± 2.82 | 19.4 ± 4.87 | n.d. | n.d. |
SACS | 5.90 ± 0.59 | 4.92 ± 0.26 | 3.52 ± 1.14 | 27.2 ± 3.43 | 2.32 ± 0.21 |
NAc-SACS | 2.85 ± 0.56 | 2.27 ± 0.31 | 1.95 ± 0.53 | 3.70 ± 0.18 | 9.94 ± 0.44 |
GSAC | 0.34 ± 0.064 | 0.28 ± 0.024 | 0.23 ± 0.059 | n.d. | n.d. |
n.d., not detected; tmax, time to reach Cmax; Vss, distribution volume at steady state.
↵a A single oral or i.v. dose (2 mg/kg) of SAC, NAc-SAC, SACS, and NAc-SACS was administered to dogs.