TABLE 5.
Summary of the mean (S.D.) pharmacokinetic parameters of oseltamivir and oseltamivir carboxylate after a single oral dose of oseltamivir (150 mg) to healthy volunteers (n = 18) under fasting conditions and with food
Statistical analysis was performed on pharmacokinetic parameters; data for fasted volunteers were compared with those receiving food.
| Pharmacokinetic Parameter | Oseltamivir |
Oseltamivir Carboxylate |
||||
|---|---|---|---|---|---|---|
| Fasted | Fed | Ratio (%) Fed/Fasted | Fasted | Fed | Ratio (%) Fed/Fasted | |
| Cmax, μg/l | 124 (63.2) | 101 (32.2) | 81.4 | 551 (204) | 441 (142)*** | 80.0 |
| tmax, h | 0.806 (0.572) | 2.06 (0.937)*** | 256 | 4.37 (1.21) | 5.42 (0.772)** | 124 |
| tβ, h | 1.61 (0.529) | 2.15 (1.17) | 134 | 6.87 (1.39) | 8.20 (1.63)*** | 120 |
| CL/F, l/min | 13.0 (11.1) | 9.54 (3.96) | 73.4 | 0.371 (0.0427) | 0.385 (0.0665) | 103.9 |
| AUC0–24h, μg/l · h | 238 (82.0) | 280 (71.4)*** | 118 | 5543 (688) | 5064 (865)** | 91.3 |
| AUC0-∞, μg/l · h | 244 (81.9) | 287 (71.6)*** | 118 | 6218 (756) | 6069 (1029) | 97.6 |
| fe, % | 3.09 (1.22) | 4.32 (1.53)*** | 140 | 58.5 (10.9) | 55.5 (9.59) | 94.9 |
| CLR, l/h | 20.4 (7.20) | 23.1 (5.95) | 113 | 13.4 (2.76) | 13.1 (2.65) | 97.7 |
CL/F, clearance as a function of bioavailability; fe, fraction excreted unchanged in urine; CLR, renal clearance.
**
, p < 0.01;
***
, p < 0.001.