TABLE 1.
Pharmacokinetic parameters of dihydroartemisinin and piperaquine in 24 healthy Vietnamese subjects following the administration of a single oral dose of 120 mg dihydroartemisinin and 960 mg piperaquine in the form of three Arterakine or three Artekin tablets (reference formulation)a
| Pharmacokinetic parameter | Dihydroartemisinin
|
Piperaquine
|
||
|---|---|---|---|---|
| Arterakine | Artekin | Arterakine | Artekin | |
| Cmax (ng/ml) | 198 (48-745) [240 ± 165] | 159 (65-359) [176 ± 81] | 232 (86-691) [276 ± 174] | 204 (78-841) [237 ± 159] |
| Tmax (h) | 1.0 (0.5-3.0) [1.2 ± 0.7] | 1.5 (0.5-3.0) [1.4 ± 0.6] | 3.0 (1.5-8.0) [3.1 ± 1.6] | 3.0 (1.0-10.0) [3.3 ± 1.9] |
| AUC0-last (ng · h/ml) | 442 (199-938) [482 ± 211] | 366 (180-761) [395 ± 157] | 13,431 (8,219-26,314) [13,984 ± 4,301] | 11,988 (5,361-24,514) [12,515 ± 3,809] |
| AUC0-∞ (ng · h/ml) | 444 (200-940) [484 ± 211] | 370 (182-716) [398 ± 159] | 23,308 (13,770-34,304) [24,168 ± 6,537]b | 19,929 (7,980-31,858) [20,942 ± 6,179] |
| AUCextrap (%)c | 0.5 ± 0.2 | 0.9 ± 0.7 | 41.5 ± 10.8 | 38.6 ± 12.8 |
| t1/2 (h) | 0.98 (0.73-1.28) [1.00 ± 0.21] | 1.01 (0.72-1.66) [1.05 ± 0.29] | 613 (273-1065) [647 ± 206] | 589 (221-1249) [643 ± 260] |
| CL/F (liters/h/kg) | 4.54 (2.28-10.34) [4.95 ± 2.10]b | 5.45 (2.49-11.02) [5.87 ± 2.31] | 0.40 (0.25-0.66) [0.42 ± 0.12]b | 0.47 (0.28-1.14) [0.50 ± 0.20] |
| V/F (liters/kg) | 6.31 (2.84-18.30) [7.00 ± 3.38]b | 7.97 (4.75-19.55) [8.02 ± 3.75] | 353 (135-627) [377 ± 125] | 394 (107-814) [428 ± 170] |
a
Data are presented as the geometric mean (range) [mean ± standard deviation].
b
Significant difference (paired t test, P < 0.05) from the reference formulation.
c
AUCextrap (%) = [(AUC0→∞ − AUC0→last)/AUC0→∞] × 100.