TABLE 3.
Pharmacokinetic parameters of GST-HG171 of the multiple ascending dose study in each treatment group in the fasted state at day 5 (mean ± SD)
| PK parameter | GST-HG171 (300 mg) BID (N = 6) | GST-HG171 (150 mg)/RTV (100 mg) BID (N = 6) | GST-HG171 (300 mg) TID (N = 6) | GST-HG171 (300 mg)/RTV (100 mg) (N = 6) |
|---|---|---|---|---|
| C max,ss (ng/mL) | 2272.81 ± 519.89 | 5019.08 ± 1106.20 | 2037.05 ± 696.16 | 7276.06 ± 1311.29 |
| Trough concentration (ng/mL) | 65.02 ± 45.02 | 854.79 ± 245.95 | 129.15 ± 53.44 | 1892.21 ± 656.96 |
| AUC0–t,ss (h × ng/mL) | 8561.44 ± 2886.72 | 35992.89 ± 5834.64 | 8874.28 ± 3607.54 | 61752.17 ± 7744.63 |
| AUC0–∞,ss (h × ng/mL) | 8733.43 ± 2986.66 | 36564.86 ± 5979.17 | 9521.77 ± 4901.67 | 62441.62 ± 8046.32 |
| t 1/2,ss (h) | 4.13 ± 3.75 | 3.84 ± 0.29 | 6.56 ± 10.77 | 3.85 ± 0.87 |
| T max,ss (h) | 1.13 (0.500, 1.500) | 1.50 (1.000, 3.001) | 0.63 (0.250, 3.000) | 2.25 (1.500, 3.000) |
| DF (%) | 336.78 ± 68.58 | 162.69 ± 23.66 | 210.94 ± 69.24 | 125.53 ± 28.96 |
| CL,ss
(L/h) |
39642.31 ± 11059.76 | 4998.38 ± 781.51 | 42443.87 ± 6223.18 | 5863.32 ± 868.12 |
| R cmax (%) | 99.72 ± 34.45 | 140.54 ± 33.27 | 89.93 ± 35.30 | 123.06 ± 21.18 |
| R auc(%) | 85.71 ± 8.24 | 139.02 ± 23.03 | 87.55 ± 16.73 | 133.71 ± 20.79 |
a
Median (min–max); R cmax, accumulation index for C max; R auc, accumulation index for AUC; DF, degree of fluctuation.