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Table 1 Mean (CV%) pharmacokinetic parameters of artesunate (AS) by intravenous-infusion compartment modeling (CA) following multiple intravenous administrations of 2, 4, and 8 mg/kg daily for 3 days with a short-term infusion (2 min) in healthy volunteers (n = 6 per group)*

From: Pharmacokinetic profiles of artesunate following multiple intravenous doses of 2, 4, and 8 mg/kg in healthy volunteers: Phase 1b study

Date of dose PK Parameters 2 mg/kg (n = 6) 4 mg/kg (n = 6) 8 mg/kg (n = 6)
Day 1 Cmax (ng/ml) 28411 (59) 40574 (68) 63677 (55)
  Tmax (min) 2 2 2
  AUCinf (ng·h/ml) 2051 (66) 4640 (69) 6022 (48)
  t1/2 elimination (h) 0.16 (52) 0.21 (46) 0.20 (40)
  CL_obs (ml/min/kg) 21.19 (33) 19.39 (48) 27.87 (51)
  Vss_obs (ml/kg) 103.60 (48) 104.34 (80) 187.99 (89)
  MRT (h) 0.08 (47) 0.08 (38) 0.10 (37)
Day 2 Cmax (ng/ml) 17920 (57) 34387 (50) 74588 (45)
  Tmax (min) 2 2 2
  AUCinf (ng·h/ml) 1410 (49) 2628 (30) 6669 (47)
  t1/2 elimination (h) 0.19 (51) 0.23 (67) 0.19 (19)
  CL_obs (ml/min/kg) 29.50 (45) 27.26 (28) 26.66 (64)
  Vss_obs (ml/kg) 185.24 (57) 139.76 (51) 129.10 (68)
  MRT (h) 0.08 (35) 0.08 (29) 0.08 (8)
Day 3 Cmax (ng/ml) 16487 (42) 51164 (61) 67613 (83)
  Tmax (min) 2 2 2
  AUCinf (ng·h/ml) 1270 (26) 3518 (51) 5916 (61)
  t1/2 elimination (h) 0.15 (40) 0.20 (46) 0.20 (60)
  CL_obs (ml/min/kg) 27.87 (26) 23.02 (35) 28.91 (44)
  Vss_obs (ml/kg) 122.00 (42) 122.17 (49) 164.58 (55)
  MRT (h) 0.07 (18) 0.08 (42) 0.09 (24)
  Accumulation Index (AUCD3/D1) 0.81 (56) 0.91 (45) 1.01 (31)
  P value (T-Test, AUCD3:D1) 0.104 0.289 0.459
  Total AUCD1-D3 (ng·h/ml) 4731 (40) 10787 (17) 18606 (45)
  1. Data are presented as arithmetic mean (CV%); NCA = non-compartment analysis (WinNonlin 5.2 Version with non-compartment model 202, IV-infusion); CA = compartment analysis (WinNonlin 5.2 Version with compartment model 10, IV-infusion); MRT = mean residence time.