TABLE 4.
SAD study: Plasma pharmacokinetic parameters of GST-HG131 in healthy subjectsa
| PK parametes | 10 mg | 30 mg | 60 mg | 100 mg (fasted) | 100 mg (fed) | 150 mg | 200 mg | 250 mg | 300 mg |
|---|---|---|---|---|---|---|---|---|---|
| (N = 8) | (N = 8) | (N = 8) | (N = 16) | (N = 16) | (N = 8) | (N = 8) | (N = 8) | (N = 8) | |
| Tmax (h)b | 1.375 (0.25, 4.00) | 1.500 (0.75, 4.00) | 1.000 (0.50, 3.00) | 1.750 (0.25, 4.00) | 2.500 (1.25, 4.00) | 3.000 (1.00, 6.00) | 2.005 (1.00, 4.00) | 2.000 (0.50, 3.02) | 2.500 (1.25, 4.02) |
| Cmax (n*g/mL) | 223.3 ± 63.1 | 552.9 ± 121.3 | 1314.7 ± 352.2 | 2132.3 ± 595.2 | 1582.3 ± 291.3 | 2035.2 ± 881.7 | 3451.7 ± 820.3 | 4724.1 ± 1243.7 | 5375.7 ± 1682.9 |
| AUC0-t (h*ng/mL) | 1015.6 ± 419.0 | 2762.5 ± 1149.3 | 5908.8 ± 2212.9 | 11568.1 ± 2765.9 | 9791.9 ± 2002.6 | 12983.8 ± 4800.5 | 23737.5 ± 6020.9 | 27962.5 ± 9921.3 | 43337.5 ± 18315.3 |
| AUC0-∞ (h*ng/mL) | 1028.0 ± 422.3 | 2777.5 ± 1150.7 | 5945.0 ± 2209.5 | 11606.9 ± 2769.3 | 9845.6 ± 2004.0 | 13013.8 ± 4819.6 | 23762.5 ± 6036.5 | 28012.5 ± 9968.3 | 43525.0 ± 18383.2 |
| t1/2 (h) | 4.12 ± 1.65 | 4.06 ± 1.02 | 3.88 ± 1.22 | 7.71 ± 5.27 | 9.18 ± 10.9 | 5.63 ± 2.21 | 8.58 ± 4.80 | 11.6 ± 13.6 | 14.3 ± 22.3 |
| CL/F (mL/h) | 10842.5 ± 3316.3 | 12171.3 ± 3981.7 | 11753.8 ± 5777.5 | 9080.0 ± 2188.7 | 10529.4 ± 1989.5 | 14792.5 ± 11166.6 | 8960.0 ± 2503.4 | 9770.0 ± 2857.4 | 7996.3 ± 3274.3 |
| Vz/F (mL) | 58800 ± 10708 | 67300 ± 14679 | 60088 ± 17208 | 94131 ± 49143 | 142881 ± 178253 | 102463 ± 37626 | 107713 ± 59224 | 142925 ± 140744 | 128363 ± 158248 |
a
Data are expressed as mean ±SD unless otherwise specified. Tmax is expressed as median (range).
b
Tmax, time to peak plasma concentration; Cmax, peak plasma concentration; AUC0-t, area under the plasma concentration-time curve from time zero to time t; AUC0-∞, area under the plasma concentration-time curve from time zero to infinity; t1/2, terminal elimination half-life; CL/F, apparent clearance; Vz/F, apparent volume of distribution.