Table 2 Pharmacokinetic comparison of tafenoquine (TQ) and primaquine (PQ) in plasma and liver tissue following single intravenous at dose of 5 mg/kg and intragastric at dose of 20 mg/kg administrations in male mice (n = 3)
PK parameters | Tafenoquine (TQ) | Primaquine (PQ) | ||
|---|---|---|---|---|
Plasma | Liver | Plasma | Liver | |
Intravenous (5 mg/kg) | ||||
Cmax (μg/mL or g) | 0.66 ± 0.13 | 44.76 ± 29.95 | 1.21 ± 0.21 | 3.99 ± 0.53 |
Tmax (hours) | 1.36 ± 1.11 | 3.69 ± 2.29 | 0.08 ± 0.0 | 0.39 ± 0.53 |
AUClast (μg · h/mL or g) | 29.63 ± 6.74 | 2493.82 ± 1361.10 | 1.20 ± 0.13 | 6.06 ± 1.39 |
AUCinfininty (μg · h/mL or g) | 30.14 ± 6.65 | 2544.96 ± 1348.03 | 1.26 ± 0.14 | 6.14 ± 1.38 |
t1/2 elimination (h) | 66.28 ± 10.32 | 70.02 ± 4.35 | 0.63 ± 0.08 | 1.32 ± 0.06 |
Vz (liter/kg) | 16.76 ± 6.44 | - | 3.85 ± 0.71 | - |
Cl (liter/h/kg) | 0.17 ± 0.04 | - | 4.19 ± 0.42 | - |
MRT (h) | 55.92 ± 3.86 | 66.11 ± 19.19 | 0.68 ± 0.02 | 1.27 ± 0.11 |
AUCinf ratio (liver/plasma) | - | 87.24 ± 44.29 | - | 3.91 ± 0.54 |
Intragastric (20 mg/kg) | ||||
Cmax (μg/mL) | 2.04 ± 0.59 | 56.90 ± 26.09 | 0.53 ± 0.07 | 8.15 ± 0.29 |
Tmax (hours) | 11.33 ± 5.37 | 1.17 ± 0.76 | 0.50 ± 0.0 | 0.50 ± 0.0 |
AUClast (μg · h/mL) | 137.91 ± 24.38 | 5140.52 ± 1794.60 | 1.26 ± 0.40 | 27.45 ± 1.84 |
AUCinfininty (μg · h/mL) | 139.18 ± 24.92 | 5391.86 ± 1898.51 | 1.31 ± 0.41 | 27.67 ± 1.75 |
t1/2 elimination (h) | 50.87 ± 4.23 | 75.48 ± 12.06 | 1.84 ± 0.45 | 4.28 ± 1.30 |
Vz (liter/kg) | 10.60 ± 1.22 | - | 154.66 ± 61.83 | - |
Cl (liter/h/kg) | 0.15 ± 0.03 | - | 57.94 ± 20.52 | - |
MRT (h) | 62.08 ± 2.30 | 88.67 ± 12.98 | 2.28 ± 0.10 | 4.49 ± 0.25 |
AUCinf ratio (liver/plasma) | - | 48.91 ± 22.67 | - | 22.26 ± 6.73 |
Absolute bioavailability (%) | 100.77 ± 37.49 | 28.32 ± 6.93 | ||