Table 4.
Summary pharmacokinetic parameters for total irinotecan in rats after each administration of either irinotecan or Irinophore C™ at 170 mg/kg on day 1 then 160 mg/kg on day 2
| Parameter | Irinotecan | Irinophore C | ||
|---|---|---|---|---|
| Day 1 | Day 2 | Day 1 | Day 2 | |
| Dose (mg/kg) | 170 | 160 | 170 | 160 |
| Cmax observed (μg/mL) | 30.0 | 22.1 | 3,197 | 3,172 |
| T½ (Elim.)* (h) | 4.6 | 9.1 | ||
| AUC0–24 (μg∙h/mL) | 171.5 | – | 33,083 | – |
| AUC24–48 (μg∙h/mL) | – | 203.4 | – | 42,548 |
| AUC0-∞ (μg∙h/mL) | 378 | 86,630 | ||
| Vd** (mL/kg) | 5820.1 | 50.02 | ||
| CL** (mL/h/kg) | 873.0 | 3.8 | ||
* Estimated from the clearance curves after the second day of dosing, i.e., from 24 h to 72 h (irinotecan) or 96 h (Irinophore C™) after the study start
** Calculated based on AUC0-∞