Table 5

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

ParameterTotal Radioactivity
Whole bloodPlasma
Tmax(h)1.5  ± 01.50  ± 0
Cmax (μg-eq/g)2.34  ± 0.3142.14  ± 0.359
AUC0–25.5(μg-eq · h/g)13.7  ± 3.8814.2  ± 6.66
AUC0–49.5 (μg-eq · h/g)15.7  ± 5.8016.1  ± 9.20
t½ (h)5-152 13.68.7
ParameterCPT-11—PlasmaSN-38—PlasmaSN-38G—PlasmaAPC—Plasma
Tmax (h)1.50  ± 0.002.32  ± 1.022.81  ± 0.4583.44  ± 1.78
Cmax (ng/ml)1534  ± 14327.1  ± 11.687.9  ± 42.5203  ± 184
AUC0–25.5(ng · h/ml)7765  ± 1876228  ± 1491047  ± 8472400  ± 2460
AUC0–∞(ng · h/ml)8808  ± 2215400  ± 2421745  ± 14173271  ± 3481
CL (l/h/m2)12.4  ± 3.02N.D.N.D.N.D.
Vz (l/m2)297  ± 119N.D.N.D.N.D.
t½ (h)5-152 14.628.535.517.8
  • N.D., not done, only patient 5 was bile-exteriorized.

  • 5-152  harmonic mean.