In vitro parameters
Compound | kmem | Rat fmed, ss | Dog fmed, ss | fuinc | fuL | Dog PPB | Rat PPB | Dog B/P | Rat B/P |
---|---|---|---|---|---|---|---|---|---|
Ibuprofen | 0 | 0.98 | 0.98 | 0.97 | 0.25 | 98.8 | 97.7 | 0.6 | 0.6 |
Indomethacin | 0.20 | 0.65 | 0.70 | 0.78 | 0.08 | 99.2 | 99.7 | 0.6 | 0.6 |
Losartan | 0.05 | 0.32 | 0.67 | 0.87 | 0.08 | 95.2 | 98.5 | 1 | 0.8 |
Ramatroban | 0.22 | 0.42 | 0.58 | 0.71 | 0.08 | 95.5 | 96.3 | 0.6 | 0.8 |
Sulfisoxazole | 0.05 | 0.84 | 0.80 | 0.77 | 0.51 | 86.6 | 98.4 | 0.6 | 0.6 |
Telmisartan | 0.004 | 0.33 | 0.41 | 0.51 | 0.04 | 97.9 | 99.4 | 0.9 | 0.9 |
Tolmetin | 0.04 | 0.96 | 0.96 | 0.96 | 0.31 | 95.0 | 97.1 | 1.1 | 1 |
AZ1 | 0.14 | 0.27 | 0.45 | 0.80 | 0.08 | 99.7 | 99.7 | 0.6 | 0.7 |
AZ2 | 0.08 | 0.25 | 0.42 | 0.90 | 0.06 | 99.6 | 99.6 | 0.6 | 0.6 |
fmed, ss, fraction in the medium at steady state; fuinc, fraction unbound in the incubation; fuL, fraction unbound in liver tissue; PPB, plasma protein binding; B/P, blood/plasma ratio.