Table 5.
Pharmacokinetics of tadalafil and its major metabolite following administration of 20 mg every 24 h for 10 days to 15 healthy subjects
| Geometric mean (CV%) | |||
|---|---|---|---|
| Parameter | Day 1 N = 15 | Day 5 N = 15 | Day 10 N = 13 |
| Tadalafil | |||
| AUCτ (µg h l−1) | 4950 (23) | 7692 (31) | 7389 (38) |
| Cmax (µg l−1) | 352 (25) | 514 (27) | 481 (31) |
| tmax (h)a | 2.0 (1.0–3.0) | 2.0 (1.0–4.0) | 2.0 (1.0–3.0) |
| t1/2 (h) | – | – | 18.7 (40) |
| CL/F (l h−1) | – | 2.6 (31) | 2.71 (38) |
| Vz/F (l) | – | – | 73.1 (23) |
| Accumulation ratio for AUCτ | – | 1.58 | 1.55 |
| Methylcatechol glucuronideb | |||
| AUCτ (µg h l−1) | 2863 (34) | 9967 (35) | 9397 (46) |
| Cmax (µg l−1) | 179 (35) | 469 (34) | 442 (44) |
| tmax (h)a | 24 (24–24) | 3.0 (0–8.0) | 3.0 (0–24) |
| t1/2 (h) | – | – | 23.2 (25) |
| Accumulation ratio for AUCτ | – | 3.58 | 3.38 |
a
Median (min – max).
b
Quantified as total methylcatechol in hydrolysed plasma.