Table 1.
Median (range) and mean (95% CI)a,b pharmacokinetic variables for oral administration of artesunate and artemether. Bioassay in DHA equivalents, except molar doses.
| Variable | Artesunatec | Artemetherc | P |
|---|---|---|---|
| Molar dose (nmol kg−1)a | 10 539 (10 146–10 932) | 13 578 (13 071–14 085) | < 0.0001 |
| tlag (h) | 0.25 (0.25) | 0.25 (0.25–1.50) | 0.06 |
| tmax (h) | 1.50 (0.50–4.00) | 2.0 (0.75–6.00) | 0.57 |
| Cmax (nmol l−1) | 8088 (4568–24 633) | 3454 (909–4663) | 0.006 |
| t½ (h) | 1.31 (0.55–4.71) | 2.98 (1.22–5.44) | 0.028 |
| λz (h−1) | 0.574 (0.147–1.263) | 0.236 (0.127–0.568) | 0.009 |
| AUC(0,∞) (nmol l−1 h)b | 18 867 (16 146–21 588) | 11 129 (9007–13 251) | 0.020 |
| Vz/F (l kg−1) | 1.31 (0.34–5.59) | 4.37 (1.73–13.85) | 0.004 |
| CL/F (l kg−1 h−1) | 0.65 (0.27–1.57) | 1.28 (0.69–2.55) | 0.004 |
| MRT (h) | 2.52 (1.18–5.11) | 3.97 (0.58–6.31) | 0.019 |
Abbreviations: Cmax (maximum observed concentration); tmax (observed time to Cmax); tlag (absorption lag time); t½ (elimination half-life); λz (elimination rate constant); Vz/F (total apparent volume of distribution kg−1 body weight); MRT (mean residence time); CL/F (clearance kg−1 body weight); AUC(0, ∞) (area under the antimalarial activity – time curve extrapolated to infinity).
Difference between the means (95% CI) = 3039 (2896, 3182) nmol kg−1
Difference between the means (95% CI) = 7738 (3568, 11908) h nmol l−1
To convert DHA equivalents nmol l−1 to ng ml−1 divide by 3.517.