| Intravenous Administration (iv) |
| Compound |
Cpa (mg/mL) |
tmax (h) |
AUClast (h•µg/mL) |
AUCinf (h•µg/mL) |
MRTlast (h) |
Cl (mL/h/kg) |
V (L/kg) |
t½ (h) |
| Free acid |
134 ± 29 |
0.14 ± 0.10 |
102 ± 34 |
102 ± 34 |
0.89 ± 0.13 |
435 ± 165 |
0.48 ± 0.21 |
0.76 ± 0.06 |
| Citric acid salt |
177 ± 40 |
0.08 ± 0.00 |
122 ± 24 |
122 ± 24 |
0.76 ± 0.06 |
340 ± 65 |
0.34 ± 0.08 |
0.69 ± 0.06 |
| Gentisic acid salt |
116 ± 9 |
0.08 ± 0.00 |
99 ± 23 |
99 ± 23 |
0.81 ± 0.11 |
424 ± 104 |
0.40 ± 0.08 |
0.65 ± 0.06 |
| Meglumine saltb |
192 |
0.08 |
149 |
149 |
0.60 |
273 |
0.27 |
0.69 |
| Tromethamine salt |
184 ± 54 |
0.08 ± 0.00 |
131 ± 23 |
131 ± 23 |
0.74 ± 0.07 |
317 ± 52 |
0.34 ± 0.07 |
0.75 ± 0.05 |
| Oral Administration (po) |
| Compound |
Cmax(mg/mL) |
tmax (h) |
AUClast(h•µg/mL) |
AUCinf (h•µg/mL) |
MRTlast (h) |
Cc (mL/h/kg) |
Vc (L/kg) |
t½ (h) |
Fd (%) |
| Free acid |
1.7 ± 2.0 |
0.50 ± 0.00 |
3.8 ± 4.6 |
4.0 ± 4.6 |
1.66 ± 0.08 |
405 ± 6 |
0.71 ± 0.06 |
1.22 ± 0.10 |
3.9 ± 4.5 |
| Citric acid salt |
2.8 ±3.3 |
1.17 ± 0.76 |
3.9 ± 4.1 |
4.1 ± 4.1 |
1.46 ± 0.29 |
334 ± 7 |
0.47 ± 0.20 |
0.97 ± 0.41 |
3.3 ± 3.4 |
| Gentisic acid salt |
0.8 ± 0.2 |
0.83 ± 0.29 |
1.5 ± 0.3 |
1.6 ± 0.3 |
1.53 ± 0.46 |
411 ± 3 |
0.67 ± 0.33 |
1.13 ± 0.55 |
1.6 ± 0.3 |
| Meglumine salt |
3.7 ± 5.3 |
0.83 ± 0.29 |
6.3 ± 9.0 |
6.5 ± 9.1 |
1.40 ± 0.66 |
267 ± 9 |
0.50 ± 0.22 |
1.27 ± 0.54 |
4.3 ± 6.1 |
| Tromethamine salt |
2.7 ± 3.5 |
0.50 ± 0.00 |
3.6 ± 4.0 |
3.7 ± 4.0 |
1.24 ± 0.35 |
318 ± 6 |
0.57 ± 0.36 |
1.23 ± 0.77 |
2.8 ± 3.0 |
aCp is the first measurable concentration in plasma after dose administration.
bOne rat died immediately after iv dose administration, and results are derived from samples collected in two animals; no standard deviation is available.
cFor po administrations, V and Cl were calculated from V/F•F and Cl/F•F, respectively.
dThe bioavailability F is expressed as a percentage. |
