TABLE 5

Pharmacokinetic parameters of SAC, NAc-SAC, SACS, and NAc-SACS in dogs after oral and i.v. administration

Data represent mean ± S.D. of three dogs

ParametersSACaNAc-SACaSACSaNAc-SACSa
i.v.Orali.v.i.v.i.v.
Cmax (mg/l)3.2 ± 0.0252.1 ± 0.149.7 ± 2.112 ± 3.311 ± 1.0
tmax (h)1.3 ± 0.58
t1/2 (h)12 ± 0.3912 ± 1.211 ± 1.56.0 ± 0.283.9 ± 0.85
CL (l/h/kg)0.048 ± 0.0060.11 ± 0.0310.074 ± 0.0100.20 ± 0.009
CLr (l/h/kg)0.00020.00190.00420.17
Vss (l/kg)0.83 ± 0.101.3 ± 0.100.51 ± 0.0590.32 ± 0.023
Bioavailability (%)92.0
AUC (mg⋅h/l)
SAC42.1 ± 4.9638.7 ± 3.4627.6 ± 4.46n.d.n.d.
NAc-SAC24.4 ± 6.0922.7 ± 2.8219.4 ± 4.87n.d.n.d.
SACS5.90 ± 0.594.92 ± 0.263.52 ± 1.1427.2 ± 3.432.32 ± 0.21
NAc-SACS2.85 ± 0.562.27 ± 0.311.95 ± 0.533.70 ± 0.189.94 ± 0.44
GSAC0.34 ± 0.0640.28 ± 0.0240.23 ± 0.059n.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.