TABLE 1

Bupropion and hydroxybupropion observational pharmacokinetic parameters in plasma and brain ECF after a subcutaneous 10-mg/kg dose of bupropion or a 2-mg/kg dose of hydroxybupropion by the same route

Results for AUC, Cmax, and AUCECF/AUCplasma,u ratio are presented as means (S.E.M.). Results for half-lives are presented as the geometric mean. There were a total of six rats in the bupropion administration group (five for plasma and five for brain), and four rats in the hydroxybupropion administration group.

DrugPlasmaBrain ECFAUCECF/
AUCplasma,u
AUC0–∞CmaxHalf-LifeAUC0–∞CmaxHalf-Life
nM·minnMminnM·minnMmin
Bupropion46,205 (5768.6)198 (27.1)13298,616 (8552.2)607 (74.3)1092.1 (0.18)
Hydroxybupropion (formed)2637 (309.8)15 (1.8)1014249 (225.7)23 (1.3)941.8 (0.10)
Hydroxybupropion (preformed)46,026 (10,737.6)496 (145.6)5056,683 (5779.6)492 (70.8)451.5 (0.21)