Table 2. Pharmacokinetic Parameters of Compounds 1 and 2 Following IV or IM of Free Base to Male Fresian-Holstein Cattlea.
compound | 1 | 2 |
---|---|---|
IV dose | 2.5 mg/kg; n = 4 | 2 mg/kg; n = 3 |
Clb (mL/min/kg) | 20 ± 4 | 15 ± 5 |
Vdss (L/kg) | 2.4 ± 0.8 | 2.3 ± 0.6 |
half-life (h) | 1.8 ± 0.5 | 4 ± 2 |
AUC 0-∞ (ng-min/mL) | 130,000 ± 30,000 | 140,000 ± 40,000 |
IM dose | 5 mg/kg; n = 4 | 10 mg/kg; n = 3 |
Cmax (ng/mL) | 130 ± 60 | 1700 ± 800 |
Tmax (h) | 0.44 ± 0.13 | 1.3 ± 0.6 |
AUC 0-∞ (ng-min/mL) | 21,000 ± 5000 | 500,000 ± 30,000 |
F (%) | 8.8 ± 2.1 | 73 ± 6 |
Data are mean ± SD; for compound 1, formulation IV was 2.5% NMP, 30% PEG400, 37.5% propylene glycol, and 30% water by volume; formulation IM was 10% NMP, 40% 2-pyrrolidone, 30% PEG400, and 20% water by volume; for compound 2, formulation was 40% 0.3 M acetate buffer, 20% Kolliphor EL, 20% glycerol formal, and 20% 2-pyrrolidone.