Table 2.
PK parameters of AD16 in SAD group
| PK parameters | 5 mg N = 8 |
10 mg N = 8 |
20 mg N = 8 |
30 mg N = 8 |
40 mg N = 8 |
60 mg N = 4 |
|
|---|---|---|---|---|---|---|---|
| Tmax (h) | Median (range) | 0.50 (0.25–2.00) | 0.50 (0.25–2.00) | 1.00 (0.33–2.00) | 0.75 (0.33–2.00) | 0.50 (0.33–1.00) | 0.87 (0.50–1.00) |
| T1/2z (h) | Mean ± SD (CV%) | 6.46 ± 2.05 (31.80) | 6.51 ± 1.16 (17.90) | 6.34 ± 1.32 (20.88) | 6.43 ± 1.46 (22.77) | 6.47 ± 1.38 (21.42) | 5.85 ± 1.20 (20.48) |
| Median (range) | 5.42 (4.70–10.44) | 6.38 (4.77–8.35) | 6.58 (4.67–8.19) | 6.27 (4.64–9.02) | 6.94 (4.06–7.93) | 5.54 (4.76–7.55) | |
| Cmax (ng/mL) | Mean ± SD (CV%) | 181.6 ± 52.17 (28.73) | 324.8 ± 67.70 (20.85) | 582.0 ± 190.06 (32.66) | 823.1 ± 164.87 (20.03) | 1139.9 ± 174.69 (15.32) | 1392.5 ± 404.34 (29.04) |
| Median (range) | 209.50 (111–236) | 355.50 (224–389) | 511.50 (411–943) | 856.00 (564–1000) | 1190.00 (913–1420) | 1385.00 (1010–1790) | |
| AUC0-t (h*ng/mL) | Mean ± SD (CV%) | 974.23 ± 227.30 (23.33) | 1876.42 ± 443.64 (23.64) | 3991.79 ± 962.47 (24.11) | 5672.23 ± 1715.99 (30.25) | 6808.53 ± 2167.28 (31.83) | 9726.83 ± 1577.54 (16.22) |
| Median (range) | 934.84 (745.97–1294.06) | 1820.15 (1302.29–2741.21) | 3812.11 (2742.19–5444.71) | 5193.31 (3921.47–8449.84) | 6154.08 (4077.52–10,528.26) | 9455.22 (8108.47–11,888.39) | |
| AUC0-∞ (h*ng/mL) | Mean ± SD (CV%) | 999.52 ± 229.69 (22.98) | 1942.97 ± 439.23 (22.61) | 4056.10 ± 948.02 (23.37) | 5772.89 ± 1715.49 (29.72) | 6881.45 ± 2184.89 (31.75) | 9771.35 ± 1632.07 (16.70) |
| Median (range) | 965.56 (763.69–1317.42) | 1883.37 (1337.48 –2789.17) | 3833.06 (2817.34–5524.11) | 5274.72 (4021.40–8646.43) | 6186.26 (4129.88–10,620.99) | 9472.10 (8121.11–12,020.10) | |
| CL/F (mL/h) | Mean ± SD (CV%) | 5231.05 ± 1148.84 (21.96) | 5371.31 ± 1173.65 (21.85) | 5166.19 ± 1174.41 (22.73) | 5587.49 ± 1531.42 (27.41) | 6336.59 ± 1956.32 (30.87) | 6262.70 ± 984.38 (15.72) |
| Median (range) | 5201.73 (3795.29–6547.13) | 5321.49 (3585.30–7476.74) | 5217.85 (3620.49–7098.89) | 5760.56 (3469.64–7460.09) | 6558.11 (3766.13–9685.51) | 6335.51 (4991.64–7388.16) | |
| Vd/F (mL) | Mean ± SD (CV%) | 46,201.74 ± 6459.12 (13.98) | 48,804.92 ± 3816.97 (7.82) | 45,467.84 ± 4745.20 (10.44) | 49,491.16 ± 7854.11 (15.87) | 56,108.07 ± 9536.99 (17.00) | 51,801.38 ± 5651.42 (10.91) |
| Median (range) | 45,646.41 (38,311.17–57,183.13) | 48,397.36 (43,203.97–54,977.22) | 47,202.23 (38,391.01–50,999.27) | 47,556.53 (37,375.58–60,281.43) | 55,361.62 (38,758.73–71,727.88) | 52,900.10 (44,111.04–57,292.49) | |
| MRT0-t (h) | Mean ± SD (CV%) | 7.02 ± 2.62 (37.32) | 7.07 ± 1.68 (23.70) | 7.71 ± 1.63 (21.10) | 7.73 ± 1.84 (23.76) | 7.49 ± 2.10 (28.03) | 7.96 ± 1.66 (20.83) |
| Median (range) | 5.65 (4.82–11.04) | 6.37 (5.4–10.18) | 7.95 (5.72–9.85) | 7.96 (5.15–10.68) | 7.49 (4.39–10.20) | 7.81 (6.45–10.53) | |