TABLE 5.
Pharmacokinetic parameters and analysis for artemether, dihydroartemisinin (metabolite), and lumefantrine following administration of artemether-lumefantrine with or without tafenoquined
| Analyte and treatment group or parameter | Geometric mean AUC0–τ (ng · h/ml) | Geometric mean AUC0–last (ng · h/ml) | Geometric mean Cmax (ng/ml) | Geometric mean t1/2 (h) | Median Tmax (h) (range) |
|---|---|---|---|---|---|
| Artemether | |||||
| TQ + AL (n = 22) | 186.2a | 38.8 | 23.2 | 1.5a | 2.0 (1.0–6.0)c |
| AL (n = 21) | 103.0b | 37.7 | 22.4 | 2.0b | 2.0 (1.0–8.0) |
| CVb (%) | 62.8 | 216.2 | 80.9 | 76.3 | |
| Ratio (90% CI) | 1.81 (1.06, 3.10) | 1.03 (0.52, 2.04) | 1.03 (0.71, 1.49) | 0.76 (0.41, 1.44) | |
| Dihydroartemisinin (metabolite) | |||||
| TQ + AL (n = 22) | 226.8 | 239.3 | 86.8 | 1.8c | 1.9 (2.0–6.0) |
| AL (n = 21) | 294.6 | 293.3 | 103.3 | 2.2 | 2.0 (1.0–8.0) |
| CVb (%) | 45.0 | 46.8 | 53.5 | 32.9 | |
| Ratio (90% CI) | 0.77 (0.62, 0.96) | 0.82 (0.65, 1.02) | 0.84 (0.65, 1.09) | 0.85 (0.72, 1.00) | |
| Lumefantrine | |||||
| TQ + AL (n = 22) | 196,498.6 | 1,043,185.4 | 20,445.0 | 197.9 | 5.9 (0–12.0) |
| AL (n = 21) | 174,602.3 | 808,244.6 | 18,911.0 | 164.7 | 4.0 (0–12.0) |
| CVb (%) | 52.3 | 61.4 | 47.2 | 30.0 | |
| Ratio (90% CI) | 1.13 (0.87, 1.45) | 1.29 (0.97, 1.73) | 1.08 (0.86, 1.36) | 1.20 (1.03, 1.40) |
a
n = 5.
b
n = 12.
c
n = 21.
d
CVb, between-subject variability.