Table
2. Pharmacokinetic parameters for
artesunate in humans
|
Dose
(mg/kg) |
Route |
Subjects
(n)* |
Cmax
(mg/l) |
tmax
(min) |
t½
(min) |
V
(l/kg) |
CL
(l/h/kg) |
Ref. |
|
3.8 |
i.v. |
4;
H |
39.0 |
- |
a
= 2.3
b
= 31 |
0.13 |
2.31 |
158
|
|
2.0
-
3.75 |
i.v. |
3;
H |
- |
- |
a
= 5
b
= 37 |
0.33
-
0.4 |
0.3
-
0.9 |
163
|
|
2.4 |
i.v. |
26;
PF |
11.3 |
2 |
2.7 |
0.14 |
2.33 |
17
|
|
2.5 |
i.v. |
12;
PV |
13.7 |
2 |
2.2 |
0.16 |
3.01 |
16,98 |
|
2.4 |
i.v. |
17,
H |
- |
- |
3.0 |
0.17 |
2.6 |
25
|
|
2.23 |
i.v. |
12;
PF
severe |
- |
- |
2.3 |
0.08 |
1.63 |
36 |
|
2.16 |
i.v. |
8;
PF
moderately
severe |
- |
- |
4.6 |
0.24 |
2.49 |
36 |
|
4.9 |
i.v.
infusion; 4h |
10;
PF
moderately
severe |
- |
- |
3.2 |
0.23 |
3.07 |
36
|
|
300
mg† |
oral |
8;
H |
397 |
15 |
a
= 11
b
= 32 |
- |
- |
98
|
|
300
mg†† |
oral |
8;
H |
194 |
19 |
a
= 10
b
= 34 |
- |
- |
98
|
|
1.8 |
rectal |
12;
CPF |
90 |
35 |
- |
- |
- |
50
|
|
3.1 |
oral
rectal |
12;
H |
0.26
0.45 |
40
86 |
29
57 |
|
|
102 |
*
H = healthy adult volunteers, PF = adult patients with falciparum malaria, PV =
adult patients with vivax malaria, CPF = child patients with falciparum malaria,
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
† Artesunate tablets from Guilin Pharmaceutical Factory, PRC; †† Artesunate tablets from Arenco, Belgium