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 | ||
Vz = Volume of distribution based on the terminal phase; MRT = mean residence time, D = Day.