Table 1.
Pharmacokinetic variables of a single 150-mg oral dose of aliskiren in 12 healthy volunteers during orange juice, apple juice and water phases
| Variable | Water phase (control) | Orange juice phase | Geometric mean ratio (orange juice/water; 95% CI) | Apple juice phase | Geometric mean ratio (apple juice/water; 95% CI) |
|---|---|---|---|---|---|
| Aliskiren | |||||
| Cmax (ng ml−1) | 110 (67, 182) | 22 (12, 40)* | 0.20 (0.11, 0.37) | 18 (11, 28)* | 0.16 (0.09, 0.28) |
| tmax (h) | 0.5 (0.5–5) | 1 (0.5–5) | 1 (0.5–2) | ||
| t1/2 (h) | 28 (27, 31) | 28 (25, 30) | 0.97 (0.86, 1.09) | 26 (24, 29) | 0.92 (0.83, 1.02) |
| AUC(0–72 h; ng ml−1 h−1) | 441 (276, 704) | 162 (122, 216)* | 0.37 (0.27, 0.51) | 161 (126, 207)* | 0.37 (0.25, 0.53) |
| AUC(0–∞; ng ml−1 h−1) | 481 (302, 767) | 183 (138, 243)* | 0.38 (0.28, 0.53) | 180 (142, 229)* | 0.37 (0.26, 0.54) |
| Ae (mg) | 0.405 (0.281, 0.582) | 0.132 (0.110, 0.158)* | 0.33 (0.24, 0.44) | 0.127 (0.102, 0.157)* | 0.31 (0.22, 0.45) |
| CLR (l h−1) | 1.34 (1.07, 1.66) | 1.54 (1.32, 1.81) | 1.16 (0.97, 1.38) | 1.47 (1.24, 1.75) | 1.10 (0.89, 1.37) |
The volunteers ingested 200 ml of orange juice, apple juice or water three times a day for 5 days and a single 150-mg dose of aliskiren on day 3, together with the first orange juice, apple juice or water dose of the day. Data are given as geometric mean (95% CI) and geometric mean ratio (95% CI), except for tmax, which is given as median (range). Ae, amount excreted into urine within 12 h; AUC(0–72 h), area under the plasma concentration–time curve from 0 to 72 h; AUC(0–∞), area under the plasma concentration–time curve from time 0 to infinity; CI, confidence interval; CLR, renal clearance; Cmax, peak plasma concentration; t1/2, elimination half-life; tmax, time to Cmax.
P < 0.001 compared with water phase.