Table 1 The main pharmacokinetic parameters of dihydroartemisinin (DHA) and its metabolite (DHA-Glu) in healthy Chinese subjects (n = 16) after four recommended oral doses of DHA (80 mg/dose)

DHA

1st dose

0.32 ± 0.10

648.37 ± 264.69

1.6 (1.0-2.5)

0.9 ± 0.2

3.33 ± 1.06

4.08 ± 1.36

2nd dose

0.24 ± 0.07**

442.34 ± 156.17**

1.9 (1.0-4.0)

0.9 ± 0.3

4.35 ± 1.33**

5.26 ± 1.98**

3rd dose

0.26 ± 0.09**

569.48 ± 240.80

1.8 (0.5-3.0)

0.9 ± 0.1

4.13 ± 1.35*

4.97 ± 1.53**

4th dose

0.21 ± 0.06**

410.78 ± 151.93**

2.1 (1.0-4.0)

1.1 ± 0.6

4.65 ± 1.37**

6.65 ± 2.60**

DHA-Glu

1st dose

1.51 ± 0.42

2495.27 ± 756.66

1.6 (1.0-2.5)

1.2 ± 0.3

N.A.

1.11 ± 0.43

2nd dose

1.63 ± 0.41

2779.61 ± 809.14

2.1 (1.0-4.0)

1.2 ± 0.4

N.A.

0.99 ± 0.39

3rd dose

1.39 ± 0.33

2395.57 ± 697.35

2.1 (1.0-3.0)

1.2 ± 0.1

N.A.

1.17 ± 0.27

4th dose

1.61 ± 0.31

2624.44 ± 903.36

2.2 (1.5-4.0)

1.1 ± 0.2

N.A.

1.01 ± 0.39

Geometric mean ratios for DHA (90% CI)

2nd/1st dose

0.77 (0.73-0.81)**

0.73 (0.64-0.83)**

N.A.

1.00 (0.90-1.09)

1.31 (1.24-1.38)**

1.32 (1.17-1.46)**

3rd/1st dose

0.83 (0.74-0.91)**

0.95 (0.75-1.15)

N.A.

0.98 (0.91-1.05)

1.27 (1.11-1.43)*

1.24 (1.09-1.38)**

4th/1st dose

0.73 (0.66-0.80)**

0.70 (0.55-0.85)**

N.A.

1.22 (0.95-1.49)

1.42 (1.28-1.55)**

1.65 (1.37-1.93)**

AUC _DHA-Glu /AUC _DHA (90% CI)

2nd/1st dose

1.49 (1.30-1.69)*

N.A.

N.A.

N.A.

N.A.

N.A.

3rd/1st dose

1.18 (1.05-1.31)

N.A.

N.A.

N.A.

N.A.

N.A.

4th/1st dose

1.66 (1.46-1.85)**

N.A.

N.A.

N.A.

N.A.

N.A.