Table 2.
Median (range) and mean (95% CI)a–d pharmacokinetic variables after oral administration of artesunate and artemether on the 1st and 2nd day. Bioassay in DHA equivalents, except molar dose. Abbreviations as in Table 1.
| Variable | Artesunate | Artemether | ||||
|---|---|---|---|---|---|---|
| Day 1 | Day 2 | P | Day 1 | Day 2 | P | |
| Dose (nmol kg−1 body weight) | 10 272 (10 026–10518) | 10 806 (10 085–11 527)a | 0.2 | 13 922 (12 994–14 850) | 13 234 (12 917–13 551)b | 0.2 |
| tlag (h) | 0.25 (0.25–0.25) | 0.25 (0.25–0.25) | 1.0 | 0.25 (0.25–0.25) | 0.50 (0.25–1.50) | 0.03 |
| tmax (h) | 2.00 (0.50–4.00) | 1.13 (0.50–4.00) | 0.5 | 1.0 (0.75–4.00) | 2.00 (1.00–6.00) | 0.2 |
| Cmax (nmol l−1) | 5118 (3178–8359) | 16 998 (4791–24 633) | 0.08 | 3091 (909–4663) | 3454 (1480–4339) | 0.9 |
| t½ (h) | 0.75 (0.49–2.30) | 2.59 (0.55–4.71) | 0.2 | 3.34 (1.30–5.44) | 2.05 (1.22–4.32) | 0.2 |
| AUC(0,∞) (nmol l−1 h) | 14 184 (10 336–18 032) | 23 551 (15 764–31 338)c | 0.06 | 9274 (6370–12 178) | 12 984 (10 400–15 568)d | 0.09 |
| Vz/F (l kg−1) | 0.78 (0.52–3.15) | 1.94 (0.34–5.59) | 0.7 | 9.46 (3.80–13.85) | 2.84 (1.73–6.40) | 0.017 |
| CL/F (l kg −1 h−1) | 0.72 (0.49–1.57) | 0.43 (0.27–1.00) | 0.2 | 1.72 (0.79–2.55) | 1.08 (0.69–1.38) | 0.1 |
| MRT (h) | 2.71 (1.52–5.11) | 2.34 (1.18–4.39) | 0.8 | 3.65 (0.58–6.31) | 4.29 (2.96–6.89) | 0.5 |
Difference between means (95% CI):
534 (145, 923)
688 (187, 1189) nmol kg−1 body weight
9367 (4935–13799)
3710 (1726–5694) nmol l−1 h.