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. 2012 Dec;40(12):2315–2323. doi: 10.1124/dmd.112.046821

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
a

Data are presented as mean ± S.D.; n = 4–9 rats per dose group.

b

For intravenous data, Cl and Vd are presented. For oral data, apparent clearance (Cl/F) and apparent volume (Vd/F) are presented.