Pharmacokinetic parameters of enantiomers of primaquine (PQ) and carboxyprimaquine (cPQ) after a single oral dose of 45-mg primaquine (base, administered as diphosphate) racemate in healthy human volunteers
| Enantiomer | Mean | Maximum | Minimum | S.D. | P value |
|---|---|---|---|---|---|
| (−)-PQ | |||||
| Cmax (ng/ml) | 163.35 | 221.60 | 121.30 | 37.64 | 0.017 (S)a |
| Tmax (h) | 3.00 | 4.00 | 2.00 | 1.09 | 0.500 (N.S.)a |
| AUC0–24 h (ng.hr/ml) | 2231.00 | 2778.60 | 1768.70 | 374.64 | 0.022 (S)a |
| kel | 0.085 | 0.043 | 0.114 | 0.025 | 0.782 (N.S.)a |
| T1/2 (h) | 9.00 | 16.00 | 6.05 | 3.65 | 0.991 (N.S.)a |
| CL/F (l/h) | 168.1 | 212.0 | 135.0 | 28.3 | 0.010 (S)a |
| (+)-PQ | |||||
| Cmax (ng/ml) | 234.66 | 299.2 | 168.8 | 48.9 | |
| Tmax (h) | 2.67 | 4.00 | 2.00 | 1.03 | |
| AUC0–24 h (ng.h/ml) | 3221.55 | 4546 | 2359.5 | 813.9 | |
| kel | 0.081 | 0.056 | 0.102 | 0.019 | |
| T1/2 (h) | 8.98 | 12.32 | 6.82 | 2.36 | |
| CL/F (l/h) | 116.4 | 158.9 | 82.5 | 28.6 | |
| Total PQ | |||||
| Cmax (ng/ml) | 394.93 | 520.8 | 292.0 | 85.14 | |
| Tmax (h) | 2.67 | 4.00 | 2.00 | 1.03 | |
| AUC0–24 h (ng.h/ml) | 5402.55 | 7324.6 | 4021.2 | 1233.12 | |
| kel | 0.079 | 0.043 | 0.099 | 0.0201 | |
| T1/2 (h) | 9.39 | 15.90 | 7.00 | 3.31 | |
| (−)-cPQ | |||||
| Cmax (ng/ml) | 1398.66 | 1756 | 1104 | 277.97 | <0.001 (S)b |
| Tmax (h) | 13.33 | 1440 | 480 | 495.74 | 0.406 (N.S.)b |
| AUC0–24 h (ng.h/ml) | 28,033.96 | 33,827.7 | 23,573.1 | 4502.43 | <0.001 (S)b |
| (+)-cPQ | |||||
| Cmax (ng/ml) | 23.416 | 36.88 | 15.8 | 8.41 | |
| Tmax (min) | 1056 | 1440 | 480 | 525.81 | |
| AUC0–24 h (ng.h/ml) | 312.2 | 489.4 | 198.4 | 115.86 | |
| Total cPQ | |||||
| Cmax (ng/ml) | 1396.16 | 1771.8 | 1069.2 | 302.47 | |
| Tmax (min) | 800 | 1440 | 480 | 495.74 | |
| AUC0–24 h (ng.h/ml) | 28,283.76 | 34,026.1 | 23,755.1 | 4461.47 |