Table 3.
Pharmacokinetic parameters of chloroquine in the different formulations (median values and range).
| Cmax (mol/l) | AUC0–21 (mmolh/l) | tmax (h) | t1/2 (h) | Vd (l/kg) | CL (ml/h/kg) | ka (h-1) | Relative Bioavailabilitya (90%CI) | AUCrest %d | |
| Formulation | |||||||||
| CQa | 760 | 34 | 2 | 155 | 113 | 0.50 | 1.8 | 1.00 (Reference) | 7.3 |
| n=8 | (466–1186) | (19–54) | (1–4) | (87–232) | (55–257) | (0.39–0.77) | (0.27–3.4) | (1.9–21) | |
| Fansidar+CQ | 731 | 43 | 3 | 162 | 105 | 0.44 | 0.47 | 1.26 | 7.9 |
| n=8 | (449–1194) | (26–70) | (1–3) | (102–395) | (79–203) | (0.28–0.72) | (0.24–3.3) | (1.03 – 1.36) | (2.9 – 30) |
| Homapak | 700 | 33 | 2 | 151 | 117 | 0.55 | 1.2 | 0.97 | 6.8 |
| n=7 | (495–813) | (17–45) | (1–4) | (93–325) | (69–548) | (0.38–1.2) | (0.19–7.8) | (0.89 – 1.20) | (1.7 – 24) |
a
The acceptable value should be within 0.85 – 1.25 at 90% Confidence Interval
b
AUCrest is derived from AUC0–8 – AUC0–21 as a percentage of the observed AUC0–8