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. 2022 Mar 18;65(7):5606–5624. doi: 10.1021/acs.jmedchem.1c02104

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
a

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.