Table 2.
Summary of saxagliptin pharmacokinetic parameters following administration of a single oral dose of saxagliptin 5 mg to healthy subjects with and without rifampicin (600 mg once daily for 6 days)
| Pharmacokinetic parameter | Saxagliptin 5 mg (n = 13) (reference) | Saxagliptin 5 mg with rifampicin 600 mg (n = 13) (test) | Test : reference ratio (%) | 90% CI |
|---|---|---|---|---|
| Cmax (ng ml−1) | ||||
| Geometric mean (CV%) | 20 (47) | 9 (25) | 47 | 38, 57 |
| tmax (h) | ||||
| Median (min, max) | 0.48 (0.48, 2.02) | 0.48 (0.48, 1.98) | NC | NC |
| AUC0–∞ (ng·h ml−1) | ||||
| Geometric mean (CV%) | 73 (26) | 17 (24) | 24 | 21, 27 |
| t1/2 (h) | ||||
| Mean (SD) | 3.02 (0.64) | 1.70 (0.57) | NC | NC |
| Urinary recovery (%) | ||||
| Mean (SD) | 17 (4) | 4 (1) | NC | NC |
| CLR (ml min−1) | ||||
| Geometric mean (CV%) | 180 (29) | 197 (15) | NC | NC |
AUC0–∞, area under the plasma concentration−time curve from time 0 to infinity; CI, confidence interval; CLR, apparent renal clearance; Cmax, maximum plasma concentration; CV%, coefficient of variation %; NC, not calculated; t1/2, terminal elimination half-life; tmax, time to reach the Cmax.