Table 4.
Pharmacokinetic parameters of methylprednisolone, calculated from 0–72 h
| Dose (mg) | Cohort | Compound | Cmax (ng ml –1 ) (SD) | Tmax (h) (SD) | AUC_0_inf (ng h l –1 ) (SD) | Ka (h –1 ) (SD) | T ½ (h) (SD) |
|---|---|---|---|---|---|---|---|
| 150 | 1 (n = 6) | 2B3–201 | 138 (37.1) | 4.56 (1.3) | 4370 (1000) | 0.029 (0.0045) | 24.4 (3.9) |
| 300 | 2 (n = 6) | 2B3–201 | 375 (96.6) | 4.48 (1.4) | 13 400 (3220) | 0.028 (0.0032) | 25 (2.5) |
| 300 | 5 (n = 6) | 2B3–201 | 282 (35) | 4.19 (0.9) | 14 800 (4060) | 0.025 (0.0086) | 31 (9.5) |
| 450 | 3 (n = 6) | 2B3–201 | 501 (144) | 4.85 (0.75) | 17 900 (2690) | 0.024 (0.0029) | 29.2 (3.5) |
| 450 | 4 (n = 6) | 2B3–201 | 360 (57.5) | 5.12 (1.4) | 17 400 (4020) | 0.024 (0.0034) | 28.9 (4.3) |
| 450 | 7 (n = 6) | 2B3–201 | 545 (99.7) | 5.90 (2.9) | 31 800 (15500) | 0.0250 (0.010) | 37.0 (29) |
| 300 | 2 (n = 6) | Free MP | 2140 (371) | 2.67 (0.20) | 11 900 (2490) | 0.258 (0.039) | 2.74 (0.44) |
| 1000 | 1 (n = 6) | Free MP | 5930 (580) | 2.16 (0.37) | 27 800 (7370) | 0.286 (0.041) | 2.47 (0.38) |
| 1000 | 3 (n = 6) | Free MP | 5120(1120) | 3.95 (0.029) | 28 800 (10800) | 0.286 (0.032) | 2.45 (0.30) |
| 1000 | 7 (n = 6) | Free MP | 7290 (1740) | 4.20 (0.26) | 42 900 (13400) | 0.208 (0.082) | 3.81 (1.6) |
SD, standard deviation