TABLE 3.
Predicted pharmacokinetic parameters of racemic and enantiomers of BUP and metabolites in healthy volunteers (n = 15) administered BUP (100 mg) to steady state
Values denote the geometric mean (90% confidence interval) or the percent coefficient of variation predicted using single-dose pharmacokinetic outcomes obtained from 15 subjects.
| Analyte | Accumulation Index | Cmax | AUCτ |
|---|---|---|---|
| nM | nM⋅ h | ||
| Enantiomer | |||
| R-BUP | 2.0 (1.8–2.4) | 324.4 (71) | 1158 (58) |
| S-BUP | 1.7 (1.4–2.0) | 53.2 (72) | 191 (72) |
| RR-OHBUP | 2.9 (2.7–3.1) | 3654.7 (50) | 37,447 (49) |
| SS-OHBUP | 2.3 (2.1–2.6) | 68.5 (61) | 577 (55) |
| RR-THRHBUP | 6.0 (5.1–7.1) | 490.4 (57) | 5399 (57) |
| SS-THRHBUP | 1.6 (1.4–1.8) | 231.7 (75) | 1433 (84) |
| SR-ERYHBUP | 3.5 (3.0–4.0) | 110.9 (57) | 1182 (60) |
| RS-ERYHBUP | 2.4 (2.0–2.9) | 21.4 (63) | 185 (71) |
| Racemic | |||
| BUP | 1.9 (1.7–2.2) | 375.4 (71) | 1331 (62) |
| OHBUP | 2.9 (2.7–3.1) | 3718.8 (50) | 37,993 (49) |
| THR | 4.3 (3.7–5.0) | 682.8 (45) | 6539 (44) |
| ERY | 3.2 (2.8–3.6) | 128.8 (54) | 1330 (57) |
AUCτ, partial area under the plasma concentration-time curve after the final simulated bupropion dose (300–312 hours).