Table 2.
Typical pharmacokinetic parameter values for artemisinin and associated interoccasional (IOV) and interindividual (IIV) variability in 33 healthy subjects and 54 malaria patients
| Parameter | Estimate (RSE%) | IOV (RSE%) | IIV (RSE%) |
|---|---|---|---|
| t1/2, ENZ (h) | 94 (27) | NE | NE |
| SIND (1/ng) | 0.045 (32) | NE | NE |
| CLint,0 (l h−1) | 1760 (35) | NE | 0.38 (24) |
| Vp (l) | 26.1 (15) | NE | 1.2 (32) |
| ka (h−1) | 0.09 (13) | 0.64 (23) | NE |
| MIT (h) | 2.0 (43) | NE | NE |
| Km (ng ml−1) | 434 (50) | NE | NE |
| fu | 0.14 (FIXED) | NE | NE |
| Residual error | 0.54 (4.7) | NE | NE |
t1/2, ENZ: enzyme elimination half-life,. SIND: slope of the inducing effect of artemisinin hepatic concentration on the production rate of enzyme precursor, CLint,0: intrinsic clearance in the pre-induced state, Vp: volume of sampling compartment, ka: absorption rate constant, fu: plasma unbound fraction, MIT: mean induction time, Km: hepatic artemisinin concentration resulting in 50% of maximum intrinsic clearance, RSE%: relative standard error in per cent, NE: not estimated.