Table 2.
The hepatic disposition parameters of the parent MP, DMP-1, and DMP-5 and the MP regenerated from DMP-1 or DMP-5 after single 5 mg/kg (MP equivalent) intravenous doses of the parent drug or the prodrugs
Injected Drug | MP | DMP-1 | DMP-5 | ||
---|---|---|---|---|---|
Measured Analyte | MP | MP | DMP-1 | MP | DMP-5 |
Cmax, μg/g | 1.14 ± 0.45 | 1.02 ± 0.41 | 35.6 ± 4.49a | 1.09 ± 0.69 | 18.1 ± 1.44a |
Tmax, h | 0 | 1.5 | 1.5 | 3 | 1.5 |
AUClast, μg h/g | 0.927 ± 0.088b | 7.63 ± 1.10b | 560 ± 42a | 9.57 ± 0.87b | 143 ± 6 a |
AUC0-∞, μg h/g | 1.10 | 15.0 | 842 | 10.8 | 239 |
Liver:Plasma AUC Ratio | 2.29 | -c | 8.40 | -c | 2.98 |
MRT, h | 1.02 | 17.2 | 21.6 | 9.79 | 13.0 |
T1/2, h | 0.708 | 12.3 | 15.0 | 7.47 | 9.07 |
Significant difference between DMP-1 and DMP-5.
Significant differences between parent MP and MP regenerated from DMP-1 or between parent MP and MP regenerated from DMP-5.
Not estimated because of the lack of accurate estimate of plasma AUC.