Table 2a.
Summary of pharmacokinetic parameters for saxagliptin, 5-hydroxy saxagliptin, simvastatin, and simvastatin acid
| Treatment | Saxagliptin | Point estimate (90% CI) | 5-Hydroxy saxagliptin | Point estimate (90% CI) | Simvastatin | Point estimate (90% CI) | Simvastatin acid | Point estimate (90% CI) | ||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| SAXA (n = 23) | SAXA + SIMVA (n = 23) | SAXA + SIMVA/SAXA | SAXA (n = 23) | SAXA + SIMVA (n = 23) | SAXA + SIMVA/SAXA | SIMVA (n = 23) | SAXA + SIMVA (n = 23) | SAXA + SIMVA/SIMVA | SIMVA ACID | SAXA + SIMVA ACID | SAXA + SIMVA ACID/SIMVA ACID | |
| Cmax, ng/mLa | 44 (32) | 54 (39) | 1.21 (1.11, 1.31) | 96 (33) | 103 (29) | 1.08 (1.02, 1.14) | 7.4 (57) | 6.5 (49) | 0.88 (0.74, 1.06) | 1.8 (71) | 1.8 (54) | 1.00 (0.89, 1.13) |
| AUCτ, ng · h/mLa | 153 (19) | 172 (17) | 1.12 (1.09, 1.15) | 529 (26) | 538 (24) | 1.02 (0.99, 1.05) | 30 (44) | 32 (41) | 1.04 (0.94, 1.15) | 17.9 (76) | 20.8 (56) | 1.16 (1.04, 1.29) |
| Tmax, hb | 1.00 (0.50, 2.00) | 0.50 (0.25, 2.00) | – | 1.50 (1.00, 3.00) | 1.50 (1.00, 2.00) | – | 1.5 (0.50, 3.00) | 1.5 (0.50, 6.00) | – | 4.00 (2.00, 8.00) | 4.00 (2.50, 10.0) | – |
a
Notes: Geometric mean (CV%);
b
Median (minimum, maximum). Treatment SAXA, saxagliptin 10 mg administered alone (day 4); Treatment SIMVA, simvastatin 40 mg administered alone (day 8); Treatment SAXA + SIMVA, saxagliptin 10 mg + simvastatin 40 mg (day 12).
Abbreviations: AUCτ, area under the concentration-time curve during a dosing interval; CI, confidence interval; Cmax, maximum observed concentration; CV, covariance; SAXA, saxagliptin; SIMVA, simvastatin; Tmax, time of maximum observed concentration.