Mean ± S.D. (n = 8) pharmacokinetic parameters determined using [14C]CPT-11-related radioactivity in whole blood and plasma and plasma concentrations of CPT-11, SN-38, SN-38G, and APC determined using fluorescence HPLC
| Parameter | Total Radioactivity | |
|---|---|---|
| Whole blood | Plasma | |
| Tmax(h) | 1.5 ± 0 | 1.50 ± 0 |
| Cmax (μg-eq/g) | 2.34 ± 0.314 | 2.14 ± 0.359 |
| AUC0–25.5(μg-eq · h/g) | 13.7 ± 3.88 | 14.2 ± 6.66 |
| AUC0–49.5 (μg-eq · h/g) | 15.7 ± 5.80 | 16.1 ± 9.20 |
| t½ (h)5-152 | 13.6 | 8.7 |
| Parameter | CPT-11—Plasma | SN-38—Plasma | SN-38G—Plasma | APC—Plasma |
|---|---|---|---|---|
| Tmax (h) | 1.50 ± 0.00 | 2.32 ± 1.02 | 2.81 ± 0.458 | 3.44 ± 1.78 |
| Cmax (ng/ml) | 1534 ± 143 | 27.1 ± 11.6 | 87.9 ± 42.5 | 203 ± 184 |
| AUC0–25.5(ng · h/ml) | 7765 ± 1876 | 228 ± 149 | 1047 ± 847 | 2400 ± 2460 |
| AUC0–∞(ng · h/ml) | 8808 ± 2215 | 400 ± 242 | 1745 ± 1417 | 3271 ± 3481 |
| CL (l/h/m2) | 12.4 ± 3.02 | N.D. | N.D. | N.D. |
| Vz (l/m2) | 297 ± 119 | N.D. | N.D. | N.D. |
| t½ (h)5-152 | 14.6 | 28.5 | 35.5 | 17.8 |
N.D., not done, only patient 5 was bile-exteriorized.
↵5-152 harmonic mean.