Table 2.
Pharmacokinetic parameters
| Parameters, mean (SD) | Canagliflozin | |||
|---|---|---|---|---|
| 25 mg (n = 12) | 100 mg (n = 12) | 200 mg (n = 14) | 400 mg (n = 13) | |
| Day 1 | ||||
| C max (ng/mL) | 248 (55) | 1126 (228) | 2304 (539) | 5028 (1733) |
| AUC0–24h (ng·h/mL) | 1295 (240) | 5468 (899) | 11,991 (3042) | 21,836 (4983) |
| t max (h)a | 1.0 [1.0–2.0] | 1.0 [1.0–1.5] | 1.0 [1.0–1.5] | 1.0 [1.0–3.0] |
| t 1/2 (h) | 10.70 (1.76) | 10.22 (1.89) | 13.26 (4.96) | 12.15 (2.34) |
| Urinary excretion rate (%)b | 0.387 (0.070) | 0.384 (0.084) | 0.424 (0.107) | 0.385 (0.097) |
| Day 16 | ||||
| C max (ng/mL) | 263 (91) | 1136 (330) | 2688 (805) | 5236 (1123) |
| AUC0–24h (ng·h/mL) | 1556 (387) | 6635 (1367) | 16,716 (5464) | 30,766 (7916) |
| t max (h)a | 1.0 [1.0–3.0] | 1.0 [1.0–1.5] | 1.3 [1.0–1.5] | 1.0 [1.0–1.5] |
| t 1/2 (h) | 14.21 (7.46) | 11.81 (3.22) | 16.16 (5.87)c | 15.76 (5.56)d |
| Urinary excretion rate (%)b | 0.599 (0.183) | 0.641 (0.204) | 0.614 (0.195) | 0.495 (0.153) |
| AR | 1.19 (0.12) | 1.21 (0.12) | 1.38 (0.17) | 1.42 (0.29) |
AR accumulation ratio, AUC 0–24h area under the concentration–time curve from time zero to 24 h, C max maximum concentration, SD standard deviation, t 1/2 elimination half-life, t max time to maximum concentration
aMedian [Min–Max]
b0–24 h
c n = 13
d n = 12