Table 1.
i.v. | s.c.b. | s.c.i. | |
---|---|---|---|
†Appearance t½ (h) | – | 0.08 ± 0.03 | 1.53 ± 0.74 ** |
Elimination t½ (h) | 2.2 ± 1.0 | 2.1 ± 0.4 | 2.2 ± 0.8 |
Apparent CL (ml min−1) | 1584 ± 408 | 1385 ± 259 | 2125 ± 860 |
Apparent Vd (l) | 276 ± 72 | 248 ± 74 | 406 ± 229 |
Cmax (nmol l−1) | 283 ± 74 | 262 ± 49 | 46 ± 8***### |
tmax (h) | 0.08 (0.08-0.08) | 0.25 (0.17-0.25)*** | 4.0 (3.5-5.0)***### |
AUC(0,t) (nmol l−1 h) | 269 ± 62 | 303 ± 55 | 198 ± 55 # |
AUC(0,∞) (nmol l−1 h) | 290 ± 67 | 323 ± 60 | 225 ± 49 # |
Bioavailability (%) | 100 | 113.6 ± 16.9 | 83.2 ± 34.6 |
Data standardized to 10 mg dose to 70 kg subject.
Results are mean±s.d. except tmax which is median (range).
i.v. = intravenous; s.c.b. = subcutaneous bolus; s.c.i. = subcutaneous infusion
Equivalent to absorption half-life for the parent drug
*P < 0.05 compared with i.v.
P < 0.01 compared with i.v.
P < 0.001 compared with i.v.
= P < 0.05 compared with s.c. b.
= P < 0.01 compared with s.c. b
= P < 0.001 compared with s.c.b.
N.B. Paired t-tests used throughout, except for appearance t½ and tmax for M3G for which the Wilcoxon Signed-Ranks test was used as the data were not normally distributed.