Table 1.
Pharmacokinetic parameters of 2-butyl-5-methyl-6-(pyridine-3-yl)-3-[2′-(1H-tetrazole-5-yl)-biphenyl-4-ylmethyl]-3H-imidazo[4,5-b]pyridine] (TM-25659). TM-25659 was administered i.v. or p.o. to rats at a dose of 10 mg·kg−1. Pharmacokinetic parameter values of TM-25659 were estimated using non-compartmental procedures
| Pharmacokinetic parameters | i.v. | p.o. |
|---|---|---|
| Tmax (h) | – | 0.33 ± 0.14 |
| Cmax (µg·mL−1) | – | 3.34 ± 0.73 |
| t 1/2 (h) | 6.78 ± 1.95 | 9.85 ± 3.15 |
| AUC0→t (µg·h·mL−1) | 43.72 ± 15.36 | 18.14 ± 3.89 |
| AUC0→∞ (µg·h·mL−1) | 52.99 ± 23.58 | 23.29 ± 0.60 |
| CL (L·h−1·kg−1) | 0.21 ± 0.09 | – |
| Vss (L·kg−1) | 1.91 ± 0.03 | – |
| MRT (h) | 5.64 ± 1.74 | 7.57 ± 1.73 |
| Ft (%) | – | 41.50 |
Results are mean ± SD (n = 6). AUC0→∞, The integral of the plasma concentration (Cp) after administration; AUC0→t, the area under time curve; CL, The volume of plasma cleared of the drug per unit time; Cmax, the peak plasma concentration of a drug after oral administration; F, the fraction of drug absorbed; MRT, mean residence time; Tmax, the time after administration of a drug when the maximum plasma concentration is reached; Vss, the apparent volume in which a drug is distributed and reaches steady-state.