TABLE 1.
Parameter | Experimental data (mean value) for a dose (mg)/12 h of: |
Human dataa (n = 10) for a dose of 600 mg/12 h | |||||
---|---|---|---|---|---|---|---|
200 (n = 4) |
600 (n = 10) |
800 (n = 2) |
|||||
0-12b | 12-24 | 0-12 | 12-24 | 0-12 | 12-24 | ||
Cmax (μg/ml) | 4.38 | 4.79 | 13.4 | 14.6 | 19.2 | 19.5 | 14.1 ± 2.8 |
Tmax (h) | 0.5 | 0.5 | 0.5 | 0.5 | 0.5 | 0.5 | |
Cres (μg/ml) | 0.39 | 0.31 | 1.17 | 1.26 | 1.15 | 1.42 | |
t1/2β (h) | 6.72 | 6.27 | 6.54 | 6.18 | 5.01 | 5.2 | 5.1 ± 2.6 |
MRT (h) | 8.65 | 7.95 | 8.54 | 8.10 | 6.55 | 6.81 | |
AUC (h × μg/ml) | 10.1 | 10.1 | 32.4 | 35.4 | 38.2 | 47.7 | 88.1 ± 34.0c |
CLtot (liters/h) | 14.9 | 15.1 | 13.9 | 12.9 | 17.2 | 13.7 | |
V (liter)s | 140.7 | 136.7 | 129.7 | 114.9 | 124.5 | 102.2 | |
Vss (liters) | 119.7 | 116.9 | 112.1 | 100.2 | 103.9 | 89.3 | |
Correlation coefficient | 0.987 | 0.983 | 0.986 | 0.989 | 0.995 | 0.994 |