Pharmacokinetic parameters of unchanged saquinavir in male Sprague-Dawley rats with a portal-vein catheter after single oral administration of saquinavir at 20 mg/kg
SQV | SQV + GF | SQV + MK | SQV + MDZ | SQV + GF + MK | SQV + GF + MDZ | |
|---|---|---|---|---|---|---|
| Cmax (μg/ml) | ||||||
| Mean ± S.D. | 0.102 ± 0.113 | 1.85 ± 0.49* | 0.188 ± 0.171 | 0.472 ± 0.528 | 1.29 ± 0.54* | 1.64 ± 0.58* |
| Geometric mean | 0.0681 | 1.80 | 0.176 | 0.308 | 1.21 | 1.55 |
| 90% CI | 0.0327–0.142 | 1.42–2.27 | 0.068–0.453 | 0.132–0.717 | 0.800–1.83 | 1.05–2.29 |
| Tmax (min) | ||||||
| Mean ± S.D. | 15.0 ± 12.2 | 15.0 ± 5.8 | 46.0 ± 75.0 | 15.0 ± 5.8 | 30.0 ± 17.3 | 33.3 ± 23.1 |
| AUC0–t (μg · min/ml) | ||||||
| Mean ± S.D. | 6.84 ± 7.21 | 143 ± 45* | 15.2 ± 11.8 | 26.2 ± 30.6 | 89.7 ± 30.4* | 72.9 ± 19.7* |
| Geometric mean | 4.86 | 138 | 13.7 | 16.8 | 86.3 | 71.0 |
| 90% CI | 2.31–10.2 | 105–180 | 5.22–35.8 | 7.20–39.2 | 62.3–119 | 53.9–93.6 |
| AUC0–∞ (μg · min/ml) | ||||||
| Mean ± S.D. | 11.9 ± 12.1 | 157 ± 44* | 21.0 ± 16.0 | 27.8 ± 31.3 | 117 ± 64 | 74.4 ± 19.5* |
| Geometric mean | 6.83 | 152 | 17.8 | 18.7 | 107 | 72.5 |
| 90% CI | 3.16–14.8 | 118–195 | 6.85–46.0 | 8.52–41.1 | 66.6–173 | 55.6–94.6 |
| Vd/F (liters/kg) | ||||||
| Mean ± S.D. | 539 ± 536 | 21.8 ± 13.6* | 696 ± 843 | 340 ± 362 | 77.9 ± 80.2 | 33.0 ± 10.0 |
| CL/F (liters/min/kg) | ||||||
| Mean ± S.D. | 5.29 ± 6.21 | 0.137 ± 0.045* | 3.10 ± 4.17 | 1.38 ± 0.87 | 0.201 ± 0.085* | 0.283 ± 0.083* |
| t1/2 (min) | ||||||
| Mean ± S.D. | 118 ± 99 | 98.5 ± 30.9** | 176 ± 37 | 141 ± 78 | 253 ± 180 | 80.6 ± 1.6** |
|
n
| 7 | 4 | 5 | 4 | 3 | 3 |