Table 4.
Summary of the pharmacokinetic parameters of MW33 by dose group.
| Statistics | 4 mg/kg group (n = 2) | 10 mg/kg group (n = 8) | 20 mg/kg group (n = 8) | 40 mg/kg group (n = 8) | 60 mg/kg group (n = 8) |
|---|---|---|---|---|---|
| Cmax (μg/mL) | |||||
| Mean ± SD | 113.3 ± 7.2 | 336.3 ± 26.5 | 716.6 ± 65.1 | 1597.0 ± 314.8 | 2338.1 ± 402.1 |
| CV% | 6.38 | 7.88 | 9.09 | 19.71 | 17.20 |
| Range | 108.2–118.5 | 299.4–371.1 | 623.8–810.0 | 1122.0–2225.0 | 1961.0–2898.9 |
| AUC0–t (h*μg/mL) | |||||
| Mean ± SD | 49,023.9 | 134,560.7 ± 16,263.9 | 280,948.8 ± 35,075.1 | 583,651.0 ± 62,067.9 | 831,047.1 ± 51,956.5 |
| CV% | 12.09 | 12.48 | 10.63 | 6.25 | |
| Range | 49,023.9–49,023.9 | 111,910.6–154,088.3 | 237,188.4–334,225.8 | 499,530.5–698,153.7 | 749,453.9–902,886.9 |
| AUC0–∞ (h*μg/mL) | |||||
| Mean ± SD | 54,829.9 | 147,635.0 ± 21,311.1 | 313,295.4 ± 46,334.3 | 636,815.3 ± 72,588.2 | 898,312.6 ± 65,473.9 |
| CV% | 14.43 | 14.79 | 11.40 | 7.29 | |
| Range | 54,829.9–54,829.9 | 118,130.9–175,027.5 | 254,574.8–390,663.9 | 531,850.0–767,327.6 | 795,364.0–984,779.2 |
| t1/2 (days) | |||||
| Mean ± SD | 28.1 | 24.8 ± 3.6 | 26.0 ± 3.3 | 24.8 ± 2.8 | 22.2 ± 1.3 |
| CV% | 14.68 | 12.78 | 11.23 | 5.72 | |
| Range | 20.4–30.6 | 21.1–3.3 | 20.5–28.0 | 20.7–23.8 | |
| λZ (1/h) | |||||
| Mean ± SD | 0.0010 | 0.0012 ± 0.0002 | 0.0011 ± 0.0002 | 0.0012 ± 0.0001 | 0.0013 ± 0.0001 |
| CV% | 14.37 | 13.45 | 12.08 | 5.75 | |
| Range | 0.0010–0.0010 | 0.0009–0.0014 | 0.0009–0.0014 | 0.0010–0.0014 | 0.0012–0.0014 |
| Tmax (h) | |||||
| Mean ± SD | 1.52 ± 0.68 | 1.22 ± 0.47 | 1.61 ± 0.52 | 1.97 ± 1.70 | 1.74 ± 0.49 |
| CV% | 45.09 | 38.59 | 32.27 | 86.68 | 28.24 |
| Range | 1.033–2 | 0.933–1.983 | 0.95–2 | 0.9–5.983 | 0.933–2 |
| Vz (mL/kg) | |||||
| Mean ± SD | 72.04 ± 1.61 | 56.91 ± 5.29 | 57.81 ± 5.77 | 53.82 ± 5.62 | 50.59 ± 3.47 |
| CV% | 2.24 | 9.29 | 9.98 | 10.44 | 6.86 |
| Range | 70.90–73.18 | 47.48–62.09 | 49.28–68.43 | 44.80–61.95 | 44.34–55.37 |
| CL (mL/h/kg) | |||||
| Mean ± SD | 0.07 ± 0.00 | 0.07 ± 0.01 | 0.07 ± 0.01 | 0.06 ± 0.01 | 0.07 ± 0.01 |
| CV% | 3.16 | 14.84 | 14.56 | 13.77 | 10.38 |
| Range | 0.07–0.08 | 0.06–0.08 | 0.05–0.08 | 0.05–0.08 | 0.05–0.08 |
Notes: Serum concentrations at 1008, 1680 and 2016 h post-dose were missing for S0102; serum concentrations at 1344, 1680 and 2016 h post-dose were missing for S0209; serum concentrations at 672 and 1680 h post-dose were missing for S0507; serum concentrations at 1344 h post-dose were missing for S0409. Considering that all the above blood sampling points were missing at the end of the elimination phase and had little effect on PK parameters, the PK parameters were still calculated, and AUC, t1/2 and λz parameters were not statistically described.