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Table 2 Mean (CV%) PK parameters of dihydroartemisinin (DHA), an active metabolite of artesunate (AS), by non-compartment analysis (NCA) following multiple intravenous administrations of AS at dose 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) 1735 (31) 3015 (29) 6056 (40)
  Tmax (hr) 0.29 (45) 0.25 (55) 0.25 (59)
  AUCinf (ng·h/ml) 2121 (18) 4391 (22) 9697 (37)
  t1/2 elimination (h) 1.19 (16) 1.74 (59) 1.42 (21)
  CL/F (ml/min/kg) 16.18 (19) 15.92 (26) 15.51 (37)
  Vss/F (ml/kg) 1634 (14) 2377 (62) 1870 (39)
  MRT (h) 1.41 (12) 1.91 (22) 1.81 (16)
Day 2 Cmax (ng/ml) 1710 (41) 2923 (35) 5943 (35)
  Tmax (hr) 0.20 (63) 0.25 (55) 0.22 (69)
  AUCinf (ng·h/ml) 2012 (27) 3740 (28) 8732 (35)
  t1/2 elimination (h) 1.59 (55) 1.42 (22) 1.91 (60)
  CL/F (ml/min/kg) 17.55 (24) 19.37 (35) 16.96 (35)
  Vss/F (ml/kg) 2224 (31) 2249 (21) 2525 (35)
  MRT (h) 1.53 (24) 1.65 (20) 2.09 (36)
Day 3 Cmax (ng/ml) 2358 (26) 3018 (25) 5762 (59)
  Tmax (hr) 0.16 (63) 0.29 (45) 0.29 (45)
  AUCinf (ng·h/ml) 2385 (24) 3960 (19) 9205 (33)
  t1/2 elimination (h) 1.31 (16) 1.24 (20) 1.34 (12)
  CL/F (ml/min/kg) 14.63 (22) 17.49 (23) 15.60 (27)
  Vss/F (ml/kg) 1691 (33) 1895 (34) 1776 (25)
  MRT (h) 1.39 (6) 1.57 (16) 1.78 (11)
  Accumulation Index(AUCD3/D1) 1.14 (21) 0.93 (24) 0.98 (15)
  P value (T-Test, AUCD3:D1) 0.140 0.157 0.233
  Total AUCD1-D3 6520 (18) 12092 (20) 27635 (34)
  Ratio of AUCDHA/AUCAS 1.46 (23) 1.15 (28) 1.65 (39)
  Ratio of Cmax AS/Cmax DHA 3.08 (45) 3.71 (47) 3.78 (49)
  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.