Table 5.
Estimated solubility limited absorbable dose (SLAD)
| Compound | Permeability | Solubility/dose | |||
|---|---|---|---|---|---|
| Predicted human Peff (10−4 cm/s) | Permeability classificationa | An | Ssi (µg/mL) | SLAD (mg) | |
| Ionized or partially ionized bases at physiological pH | |||||
| Doxycyclin | 0.70 | Intermediate | 1.0 | > 2000 | > 1000 |
| Pyronaridine | 1.4 | High | 1.6 | > 2000 | > 1610 |
| Proguanil | 0.71 | Intermediate | 1.0 | > 2000 | > 1000 |
| Primaquine | 3.0 | High | 3.6 | > 2000 | > 3560 |
| Chloroquine | 1.4 | High | 1.6 | > 2000 | > 1620 |
| Chlorproguanil | 1.5 | High | 1.8 | 1100 | 998 |
| Azithromycin | 0.16 | Low | 1.0 | 1440 | 720 |
| AQ-13 | 1.9 | High | 2.2 | > 2000 | > 2250 |
| Quinine | 3.7 | High | 4.4 | 1960 | 4280 |
| Clindamycin | 2.1 | High | 2.5 | > 2000 | > 2530 |
| KAF156 | 2.9 | High | 3.5 | 1600 | 2780 |
| M5717 | 3.4 | High | 4.0 | > 3000 | > 6050 |
| OZ277 | 2.7 | High | 3.2 | > 2000 | > 3240 |
| Mefloquine | 7.7 | High | 9.2 | 584 | 2690 |
| Amodiaquine | 4.7 | High | 5.6 | 1120 | 3130 |
| Ferroquine | 2.2 | High | 2.7 | 320 | 426 |
| Naphthoquine | 9.2 | High | 11 | 410 | 2250 |
| Tafenoquine | 11 | High | 13 | 15.8 | 105 |
| MMV253 | 6.8 | High | 8.1 | 569 | 2300 |
| MMV052 | 11 | High | 13 | 1140 | 7580 |
| Piperaquine | 11 | High | 13 | 103 | 685 |
| Halofantrine | 11 | High | 13 | 69.9 | 466 |
| TDD-E209 | 11 | High | 13 | 87.0 | 579 |
| Lumefantrine | CND | CND | CND | CND | CND |
| Ionized acids at physiological pH | |||||
| Sulfadoxine | 1.9 | High | 2.2 | 858 | 959 |
| Sulfamethoxazole | 0.85 | Intermediate | 1.0 | > 2000 | > 1000 |
| Artesunate | 0.66 | Intermediate | 1.0 | 1690 | 845 |
| Atovaquone | 11 | High | 13 | 1.83 | 12 |
| Zwitterionic or partially zwitterionic at physiological pH | |||||
| P218 | 0.24 | Low | 1.0 | 408 | 204 |
| JPC3210 | 11 | High | 13 | 7.60 | 51 |
| Neutral at physiological pH | |||||
| Dapsone | 4.1 | High | 4.9 | 323 | 786 |
| Dihydroartemisinin | 4.4 | High | 5.2 | 159 | 413 |
| DSM421 | 3.3 | High | 3.9 | 93.0 | 182 |
| Pyrimethamine | 4.9 | High | 5.9 | 111 | 326 |
| MMV048 | 3.8 | High | 4.5 | 6.70 | 15 |
| Artemisone | 5.0 | High | 6.0 | 115 | 345 |
| Artemether | 3.9 | High | 4.7 | 166 | 388 |
| SJ733 | 1.8 | High | 2.2 | 101 | 109 |
| DSM265 | 4.8 | High | 5.7 | 5.10 | 14 |
| KAE609 | 11 | High | 13 | 111 | 738 |
| OZ439 | 11 | High | 13 | 40.6 | 270 |
| ELQ300 | 11 | High | 13 | 0.520 | 3 |