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Table 2 Pharmacokinetic parameter estimates for artemether and dihydroartemisinin in different ethnic populations after artemether administration

From: Pharmacokinetics of artemether and dihydroartemisinin in healthy Pakistani male volunteers treated with artemether-lumefantrine

 

Pakistani male healthy volunteers (n = 12).

Oral single dose of 80 mg artemether a,b

[present study]

Caucasian male and female healthy volunteers

(n = 16).

Oral single dose of 80 mg artemether a,b[19]

Thai male healthy volunteers (n = 6).

Oral single dose of 200 mg artemether c[20]

Malaysian male healthy volunteers

(n = 6).

Oral single dose of 200 mg artemether c[22]

Chinese male and female patients with malaria

(n = 11).

Oral multiple doses of 80 mg artemether c,d[21]

Chinese male and female patients with malaria

(n = 11).

Oral multiple doses of 80 mg artemether a,c,d[21]

Artemether

      

CMAX (ng/mL)

184 ± 100

104 ± 40

118 (112-127)

310 ± 150

157 ± 93 e

133 ± 49 e

TMAX (hr)

1.56 ± 0.68

2.00 (1.00-4.00)

3.00 (1.00-10.0)

1.88 ± 0.21

1.73 ± 0.46 e

2.13 ± 0.49 e

CL/F (L/hr)

257 ± 140

-

-

365 ± 190

-

-

V/F (L)

666 ± 220

-

-

988 ± 520

543 ± 950 e

189 ± 130 e

T1/2 (hr)

2.00 ± 0.71

1.90 ± 0.80

3.10 (1.00-9.60)

2.00 ± 0.59

1.16 ± 0.44

0.860 ± 0.26

TLAG (hr)

0.130 ± 0.23

-

-

0.330 ± 0.13

0.480 ± 0.24 e

0.830 ± 0.37 e

AUC0-∞/dose (hr × ng/mL/mg)

4.82 ± 2.2

4.00 ± 1.7

5.50 (1.65-22.2)

3.36 ± 1.4

5.73 ± 3.1

6.36 ± 2.5

AUC0-∞ (hr × ng/mL)

385 ± 170

320 ± 140

1100 (330-4440)

671 ± 270

1830 ± 1000

2040 ± 800

Dihydro-artemisinin

      

CMAX (ng/mL)

126 ± 46

104 ± 45

379 (162-702)

273 ± 64

161 ± 63 e

105 ± 42 e

TMAX (hr)

1.69 ± 0.59

2.50 (1.00-4.00)

6.00 (2.00-12.0)

1.92 ± 0.13

1.86 ± 0.45 e

2.44 ± 0.44 e

CL/F (L/hr)

269 ± 57

-

-

-

-

-

V/F (L)

702 ± 220

-

-

-

275 ± 230 e

246 ± 99 e

T1/2 (hr)

1.80 ± 0.31

2.10 ± 0.90

10.6 (4.70-19.2)

-

0.950 ± 0.42

1.06 ± 0.25

TLAG (hr)

0.250 ± 0.24

-

-

0.290 ± 0.10

0.350 ± 0.28 e

0.820 ± 0.54 e

AUC0-∞/dose (hr × ng/mL/mg)

3.86 ± 0.76

4.33 ± 1.5

34.5 (4.35-202)

3.94 ± 1.2

9.14 ± 2.0

9.80 ± 4.5

AUC0-∞ (hr × ng/mL)

294 ± 58

331 ± 110

6590 (830-38700)

753 ± 230

2930 ± 640

3140 ± 1400

  1. a Fixed oral combination of 80 mg artemether and 120 mg lumefantrine
  2. b administered together with a high-fat meal
  3. c administered on an empty stomach
  4. d administered at 0, 8, 24 and 48 hours
  5. e pharmacokinetic parameter estimates based on the first dose
  6. Values are reported as mean ± SD or as median (range).
  7. Dose normalized exposures were calculated using the published mean or median value for total exposure divided with the mean or median dose.
  8. CMAX = maximum observed plasma drug concentration, TMAX = observed time to reach CMAX, CL/F = oral clearance, V/F = apparent oral volume of distribution, T1/2 = terminal elimination half-life, TLAG = absorption lag time, and AUC0-∞ = area under the plasma concentration time curve after the first dose to infinity.