TABLE 2.
Pharmacokinetics of RFB and of desRFB after administration of RFB alone (treatment B) and in combination with DRV/r (treatment C)
| Drug, parameter | Pharmacokinetics [mean ± SD or Tmaxa median (range)] with treatment: |
LS means ratio (90% CI) | |
|---|---|---|---|
| B (RFB) | C (DRV/r + RFB) | ||
| RFB | |||
| No. of volunteers | 15 | 11 | |
| Tmax (h) | 2.5 (1.0-6.0) | 4.0 (2.0-5.0) | |
| C0h (ng/ml) | 67.54 ± 19.82 | 116.0 ± 31.92 | 1.730 (1.536-1.948) |
| Cmin (ng/ml) | 61.99 ± 14.23 | 111.8 ± 34.62 | 1.637 (1.481-1.808) |
| Cmax (ng/ml) | 565.2 ± 132.5 | 619.7 ± 242.3 | 0.717 (0.550-0.935) |
| AUCτb,c (ng·h/ml) | 4,659 ± 968.9 | 10,790 ± 3,171 | 0.933 (0.796-1.093) |
| desRFB | |||
| No. of volunteers | 15 | 11 | |
| Tmax (h) | 2.5 (1.5-6.0) | 5.0 (2.5-12.0) | |
| C0h (ng/ml) | 4.147 ± 1.133 | 121.0 ± 23.93 | 28.97 (23.90-35.11) |
| Cmin (ng/ml) | 3.684 ± 1.110 | 112.4 ± 26.62 | 27.10 (22.20-33.20) |
| Cmax (ng/ml) | 40.98 ± 15.83 | 236.5 ± 74.53 | 4.767 (4.040-5.625) |
| AUCτb,c (ng·h/ml) | 339.1 ± 116.7 | 7,497 ± 2,044 | 9.812 (8.087-11.90) |
| AUCτ,par+met (ng·h/ml)d | 5,016 ± 1,043 | 18,670 ± 4,623 | 1.55 (1.326-1.811) |
| Percentage ratio (AUCτ,par+met) | 7.315 ± 2.060 | 72.96 ± 19.51 | |
a
Tmax, time to maximum plasma concentration.
b
AUCτ is AUC24h for treatment B and AUC48h for treatment C.
c
τ (dosing interval) is 24 h for treatment B and 48 h for treatment C, before statistical analysis. AUCτ was corrected for the difference in dosage interval. All other PK parameters shown are absolute values.
d
n = 9 volunteers for both test and reference arms.