Parameter

Non-Fixed Formulation

Fixed Formulation

Artesunate

AUClast (µg.hr/L)

419 ± 670

310 ± 324

Cmax (µg/L)

451 ± 440

255 ± 272

Tmax (hr)

0.925 ± 0.563 (0.750)

0.833 ± 0.702 (0.500)

Artesunate, Dose-Normalised to 200 mg Artesunate

Dose-Normalised AUClast (µg.hr/L)

430 ± 707

310 ± 324

Dose-Normalised Cmax (µg/L)

448 ± 381

255 ± 272 *

Dihydroartemisinin

AUClast (µg.hr/L)

3633 ± 1367

3027 ± 2491

AUCinf (µg.hr/L)

3745 ± 1371

3138 ± 2491

Cmax (µg/L)

2043 ± 949

1234 ± 857

Tmax (hr)

1.41 ± 0.714 (1.50)

1.99 ± 1.12 (2.00)

Dihydroartemisinin, Dose-Normalised to 200 mg Artesunate

Dose-Normalised AUClast (µg.hr/L)

3695 ± 1424

3027 ± 2491

Dose-Normalised AUCinf (µg.hr/L)

3812 ± 1443

3138 ± 2491

Dose-Normalised Cmax (µg/L)

2059 ± 941

1234 ± 857 *

Mefloquine

AUClast (µg.hr/L)

782607 ± 224234

810835 ± 364880

AUCinf (µg.hr/L)

1062533 ± 365937

1149417 ± 758992

Cmax (µg/L)

3239 ± 734

3279 ± 1252

Tmax (hr)

70.9 ± 13.5 (72.0)

71.3 ± 17.3 (72.0)

Mefloquine, Dose-Normalised to 400 mg Mefloquine

Dose-Normalised AUClast (µg.hr/L)

763147 ± 232259

810835 ± 364880

Dose-Normalised AUCinf (µg.hr/L)

1029264 ± 351032

1149417 ± 758992

Dose-Normalised Cmax (µg/L)

3184 ± 934

3279 ± 1252


*p < 0.05 compared to Non-Fixed formulation data; statistical analysis not conducted on non-dose-normalised data.
Table 3: Derived artesunate, dihydroartemisinin and mefloquine pharmacokinetic parameters for uncomplicated falciparum malaria patients administered artesunate and mefloquine as a Fixed formulation (200 mg artesunate/400 mg mefloquine daily for 3 days) or a Non-Fixed formulation (4 mg/kg artesunate + 0 mg/kg mefloquine on Day 1; 4 mg/kg artesunate + 15 mg/kg mefloquine on Day 2; 4 mg/kg artesunate + 10 mg/kg mefloquine on Day 3) (Fixed: n=20; Non-Fixed: n=23). Data expressed as mean ± standard deviation (median).
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