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 parameterDihydroartemisininPiperaquine
ArterakineArtekinArterakineArtekin
C max (ng/ml)198 (48-745) [240 ± 165]159 (65-359) [176 ± 81]232 (86-691) [276 ± 174]204 (78-841) [237 ± 159]
T max (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]b19,929 (7,980-31,858) [20,942 ± 6,179]
AUCextrap (%)c0.5 ± 0.20.9 ± 0.741.5 ± 10.838.6 ± 12.8
t 1/2 (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]b5.45 (2.49-11.02) [5.87 ± 2.31]0.40 (0.25-0.66) [0.42 ± 0.12]b0.47 (0.28-1.14) [0.50 ± 0.20]
V/F (liters/kg)6.31 (2.84-18.30) [7.00 ± 3.38]b7.97 (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.