Table 5.
Pharmacokinetic parameters of the TXY436 prodrug and the PC190723 product following a single intravenous or peroral administration of TXY436 to male BALB/c micea
| Compound | Route | Dose (mg/kg) | tmax (h) | C0b (ng/liter) | AUClast (ng/liter·h) | t1/2 (h) | CL (ml/min·kg) | Vss (liters/kg) | %Fc |
|---|---|---|---|---|---|---|---|---|---|
| TXY436 | i.v. | 5 | NA | 878 | 252 | 0.26 | 312 | 5.77 | NA |
| p.o. | 10 | 0.50 | 178 | 164 | NA | NA | NA | 33 | |
| PC190723 | i.v. | NA | NA | 978 | 923 | 0.96 | 86.0 | 5.39 | NA |
| p.o. | NA | 0.50 | 343 | 1340 | NA | NA | NA | 73 |
a
Parameters were calculated by analysis of the plasma concentration versus time plots shown in Fig. 8 using the sparse sampling mode in the noncompartmental analysis (NCA) module of the Phoenix WinNonlin version 6.3 software package. NA, not applicable.; i.v., intravenous; p.o., peroral.
b
An extrapolated concentration was used for the i.v. group.
c
The AUClast value was used to calculate the %F value.