Comparison of mean triglyceride (TG) transport and drug transport rates in lymph of dogs and rats after oral coadministration of MU or halofantrine with different lipid loads
| Species/Drug | Formulation or Lipid Load | Maximum Rate of TG Transport in Lymph | Total TG Transported in Lymph over 8/10 h | Maximum Rate of Drug Transport in Lymph per Gram TG | Total Drug Transported in Lymph per Gram Lymph TG over 8/10 h |
|---|---|---|---|---|---|
| mg/h | g | mg drug/g TG | mg drug/g TG | ||
| Dog | |||||
| MU | 0 g of lipid (fasted) | 461 | 1.4 | 0.27 | 0.07 |
| 5 g of lipid | 745 | 4.1 | 0.94 | 0.19 | |
| 7.5 g of lipid | 1374 | 5.2 | 1.12 | 0.45 | |
| 10 g of lipid | 2791 | 7.0 | 1.51 | 0.62 | |
| 15 g of lipid | 2101 | 11.7 | 0.93 | 0.25 | |
| 34 g of lipid | 5015 | 20.45 | 0.77 | 0.23 | |
| Halofantrinea | ME/LC (fasted) | 850 | 3.4 | 12.29 | 4.2 |
| ME/MC (fasted) | 178 | 0.9 | 5.14 | 2.8 | |
| PEG melt (fasted) | N.M. | 0.5 | 4.81 | 2.6 | |
| PEG melt (34 g of lipid) | N.M. | 32.6 | 6.21 | 1.7 | |
| Ratb | |||||
| MU | Lipid-free | 2.88 | 0.017 | 0.55 | 0.16 |
| 4 mg of OA + LPC + BS | 3.18 | 0.017 | 0.52 | 0.11 | |
| 4 mg of CO/PGL + LPC + BS | 3.41 | 0.020 | 1.25 | 0.15 | |
| 40 mg of CO/PGL in Tween | 5.72 | 0.028 | 1.03 | 0.41 | |
| 40 mg of OA + LPC + BS | 9.94 | 0.034 | 0.60 | 0.52 | |
| 40 mg of OA in Tween | 10.22 | 0.041 | 0.77 | 0.38 | |
| 100 mg of lipid predose | 16.97 | 0.072 | 0.56 | 0.32 |
N.M., not measured.
↵a Data reproduced from Khoo et al. (2003). ME/LC, long-chain triglyceride microemulsion; LC/MC, medium-chain triglyceride microemulsion; PEG melt, lipid-free amorphous PEG 600 solid dispersion.