TABLE 1.
E2072 plasma pharmacokinetic parameters in ratsa
Cmax | Tmax | AUClast | AUCinf | Clb | Vdb | t½ | %F | |
---|---|---|---|---|---|---|---|---|
ng/ml | h | ng · h/ml | l/h/kg | h | ||||
0.1 mg/kg i.v. | 1800 ± 927 | 1969 ± 1071 | 0.06 ± 0.03 | 0.20 ± 79 | 2.30 ± 0.23 | |||
0.1 mg/kg p.o. | 62.6 ± 43.0 | 0.83 ± 0.77 | 268 ± 267 | 605 ± 939 | 0.51 ± 0.40 | 2.98 ± 1.45 | 9.33 ± 14.9 | 17.4 ± 17.3 |
1 mg/kg i.v. | 12,675 ± 7417 | 12,989 ± 7511 | 0.05 ± 0.03 | 0.21 ± 0.11 | 3.25 ± 1.13 | |||
1 mg/kg p.o. | 1095 ± 1058 | 0.58 ± 0.44 | 2608 ± 818 | 3209 ± 776 | 0.33 ± 0.09 | 1.65 ± 0.69 | 3.72 ± 2.25 | 23.7 ± 6.6 |
10 mg/kg i.v. | 90,150 ± 88,864 | 90,622 ± 9043 | 0.27 ± 0.12 | 1.43 ± 0.82 | 3.55 ± 0.61 | |||
10 mg/kg p.o. | 7097 ± 5549 | 1.03 ± 0.57 | 33,448 ± 9737 | 33,762 ± 9867 | 0.32 ± 0.09 | 1.44 ± 0.46 | 3.17 ± 0.60 | 37.3 ± 10.9 |
30 mg/kg i.v. | 202,098 ± 86,045 | 204,159 ± 86,969 | 0.18 ± 0.08 | 1.08 ± 0.78 | 4.07 ± 0.98 | |||
30 mg/kg p.o. | 13,017 ± 6148 | 1.43 ± 0.35 | 76,062 ± 26,257 | 76,570 ± 26,341 | 0.51 ± 0.40 | 2.39 ± 2.18 | 3.15 ± 0.46 | 37.5 ± 12.9 |
Data are presented as mean ± S.D.; n = 4–9 rats per dose group.
For intravenous data, Cl and Vd are presented. For oral data, apparent clearance (Cl/F) and apparent volume (Vd/F) are presented.