TABLE 3.
Plasma pharmacokinetic parameters in rats after intravenous administration of E2072 and E2072-homodisulfidea
Dose | Cmax | Tmax | AUClast | AUCinf | Cl | Vd | t½,β |
---|---|---|---|---|---|---|---|
ng/ml | h | ng · h/ml | l/h/kg | l/kg | h | ||
E2072 (10 mg/kg) | |||||||
E2072 | 57,226 ± 12,077 | 0.11 ± 0.08 | 86,652 ± 22,279 | 86,973 ± 222,349 | 0.12 ± 0.26 | 19.0 ± 9.9 | 105 ± 40 |
E2072-homodisulfide | 3134 ± 838 | 0.48 ± 0.48 | 120,303 ± 30,237 | 253,322 ± 108,052 | – | – | 208 ± 81 |
E2072-homodisulfide (5 mg/kg) | |||||||
E2072 | 242 ± 173 | 3.33 ± 1.03 | 9149 ± 4386 | 12,177 ± 5214 | – | – | 102 ± 27 |
E2072-homodisulfide | 103,952 ± 24,100 | 0.11 ± 0.08 | 2,492,590 ± 480,442 | 3,537,275 ± 1,052,897 | 0.0015 ± 0.0005 | 209 ± 52 | 101 ± 35 |
Data are presented as mean ± S.D.; n = 5–6 rats per dose group.