Table 4.  Pharmacokinetic parameters for artemether in humans

 

Dose (mg/kg)

Route

Subjects

(n)*

Cmax (µg/l)

tmax

(h)

t½

(h)

ka

(1/h)

V/F

(l/kg)

CL/F

(l/h/kg)

Ref.

3.5

oral

6; H

310

1.88

2

-

17.4

6.42

94

3.7

oral

6; H

352

3

3.1

-

-

-

100

3.4

oral

8; P

689

3

4.2

-

-

-

100

5

oral

8;H

1211

1.7

2.6

-

-

-

132

5

oral

8;H

499

2

5.5

-

9.6

2.26

131

5

rectal

8;H

755

3.1

-

-

-

-

132

5

i.m.

8;H

1754

8.7

-

-

-

-

132

6

i.m.

6; H

432

5.2

7.7

2.6

-

2.31

163

6

oral

50;P

138-158

6

-

-

-

-

63

6

oral

13;P

351

2

2.2

-

10.9

3.55

62

10

i.m.

6; H

668

6.3

11.1

2.0

-

1.94

163

3.2

i.m.

26; PC

40-73

1.3-2.1

-

-

-

-

96

4.6 - 6.7

oral

8; H

474

2

2.8

1.1

-

-

66

4.6 - 6.7

i.m.

8; H

540

3.9

6.9

2.0

-

-

66

 

* H = healthy adult volunteers, P = adult patients, PC = child patients, Cmax=maximum plasma concentration; tmax=time of maximum concentration; t1/2=elimination half-life; ka=first order absorption rate constant; V/F= volume of distribution after non-i.v. administration; CL/F=clearance after non-i.v. administration.