Table 2.
Estimated biliary excretion pharmacokinetic parameters of Rho-123 (0.2 mg/kg, i.v.) in rats. Five groups were established in both studies: sham RT + Rho-123 (0.2 mg/kg, i.v.); concurrent regimen, RT2Gy + Rho-123 (0.2 mg/kg, i.v.) 10 min later; sequential regimen, RT2Gy + Rho-123 (0.2 mg/kg, i.v.) 24 hr later; concurrent regimen, RT9Gy + Rho-123 (0.2 mg/kg, i.v.) 10 min later; and sequential regimen, RT9Gy + Rho-123 (0.2 mg/kg i.v.) 24 hr later. The data are expressed as the mean ± SEM values (n = 6 per group).
| Pharmacokinetic parameter | Rho-123 (0.2 mg/kg) | RT2Gy | RT9Gy | ||
|---|---|---|---|---|---|
| After 10 min + Rho-123 (0.2 mg/kg) | After 24 hr +Rho-123 (0.2 mg/kg) | After 10 min + Rho-123 0.2 mg/kg | After 24 hr + Rho-123 (0.2 mg/kg) | ||
| AUC0-T (min*µg/mL) | 112.64 ± 23.51 | 190.38 ± 63.61a | 115.23 ± 33.31b,g | 162.42 ± 38.13c,e | 99.48 ± 27.16d,f,h |
| Cmax (µg/mL) | 2.01 ± 0.60 | 3.56 ± 1.93 | 2.24 ± 0.57 | 2.86 ± 0.83 | 2.07 ± 0.75 |
| Tmax (min) | 14 ± 4 | 11 ± 5 | 9 ± 5 | 11 ± 5 | 13 ± 4 |
| t½ (min) | 42 ± 13 | 46 ± 13 | 32 ± 8 | 43 ± 6 | 34 ± 9 |
| Cl (mL/min/kg) | 1.56 ± 0.30 | 0.92 ± 0.23 | 1.73 ± 0.61 | 1.07 ± 0.33 | 1.91 ± 0.56 |
| MRT (min) | 61 ± 14 | 66 ± 24 | 47 ± 12 | 66 ± 8 | 50 ± 13 |
AUC, area under the concentration vs. time curve; Tmax, the time at which Cmax is observed; Cmax, peak plasma concentration of the drug after administration.
aRT2Gy (wait 10 min) + Rho-123 (0.2 mg/kg) vs. Rho-123 (0.2 mg/kg) only, p = 0.013.
bRT2Gy (wait 24 hr) + Rho-123 (0.2 mg/kg) vs. Rho-123 (0.2 mg/kg) only, p = 0.877.
cRT9Gy (wait 10 min) + Rho-123 (0.2 mg/kg) vs. Rho-123 (0.2 mg/kg) only, p = 0.018.
dRT9Gy (wait 24 hr) + Rho-123 (0.2 mg/kg) vs. Rho-123 (0.2 mg/kg) only, p = 0.391.
eRT2Gy (wait 10 min) + Rho-123 (0.2 mg/kg) vs. RT9Gy (wait 10 min) + Rho-123 (0.2 mg/kg), p = 0.424.
fRT2Gy (wait 24 hr) + Rho-123 (0.2 mg/kg) vs. RT9Gy (wait 24 hr) + Rho-123 (0.2 mg/kg), p = 0.436.
gRT2Gy (wait 10 min) + Rho-123 (0.2 mg/kg) vs. RT2Gy (wait 24 hr) + Rho-123 (0.2 mg/kg), p = 0.047.
hRT9Gy (wait 10 min) + Rho-123 (0.2 mg/kg) vs. RT9Gy (wait 24 hr) + Rho-123 (0.2 mg/kg), p = 0.017.