Table 2.
Comparison of pharmacokinetic parameters of artemether, dihydroartemisinin and lumefantrine
| Parameter | Artemether/lumefantrine(N = 13), median (range) | Artemether/lumefantrine plus lopinavir/ritonavir(N = 16), median (range) | P value |
|---|---|---|---|
| Artemether | |||
| Cmax (ng/mL) | 112 (20–362) | 56 (17–236) | 0.03 |
| Tmax (h) | 1 (1–4) | 2 (1–4) | 0.38 |
| CL/F (L/h) | 295 (69–817) | 492 (129–1805) | <0.01 |
| V/F (L) | 1072 (593–2651) | 1487 (762–3485) | 0.02 |
| t1/2 (h) | 2 (1–5) | 1 (1–6) | 0.04 |
| AUC0-last (ng · h/mL) | 264 (92–1129) | 151 (38–606) | <0.01 |
| AUC0-∞ (ng · h/mL) | 271 (97–1150) | 162 (44–618) | <0.01 |
| Dihydroartemisinin | |||
| Cmax (ng/mL) | 66 (10–111) | 73 (31–224) | 0.55 |
| Tmax (h) | 2 (1–4) | 2 (1–4) | 0.89 |
| CL/F (L/h) | 350 (210–942) | 424 (280–626) | 0.23 |
| V/F (L) | 922 (498–4779) | 876 (734–1315) | 1 |
| t1/2 (h) | 1 (1–3) | 1 (1–2) | 0.06 |
| AUC0-last (ng · h/mL) | 213 (68–343) | 175 (118–262) | 0.27 |
| AUC0-∞ (ng · h/mL) | 217 (81–363) | 180 (121–272) | 0.23 |
| Lumefantrine | |||
| Tlag (h) | 1 (0–4) | 1 (0–1) | 0.16 |
| Cmax (ng/mL) | 2532 (1071–5957) | 7097 (2396–9462) | <0.01 |
| Tmax (h) | 8 (3–12) | 8 (4–12) | 0.26 |
| CL/F (L/h) | 10 (3–32) | 1 (1–5) | <0.01 |
| V/F (L) | 179 (53–860) | 86 (59–219) | 0.01 |
| t1/2 (h) | 23 (6–51) | 31 (24–43) | <0.01 |
| AUC0-last (ng · h/mL) | 41 119 (12 850–125 200) | 199 678 (71 205–251 015) | <0.01 |
| AUC0-∞ (ng · h/mL) | 46 925 (14 559–136 297) | 267 386 (84 845–344 468) | <0.01 |