Table 4

Pharmacokinetic parameters of CL and SSL DOX in humans

FormulationDoseT1/2AUCVdClReference
mg/m2 h mg ∗ h/l l l/h
SSL DOX253.2  (0.2–5.4)6094.10.08 Gabizon et al. (1994)
45.2  (20.8–59.1)(227–887)(3.0–6.5)(0.05–0.21)
501.4  (0.2–7.3)9025.90.09 Gabizon et al. (1994)
45.9  (29.3–74.0)(335–2497)(2.3–10.1)(0.03–0.24)
Free DOX250.07  (0.05–0.09)1.025445.3 Gabizon et al. (1994)
8.7  (3.6–13.3)(0.7–1.3)(126–393)(39.7–48.6)
500.06  (0.06–0.08)3.536525.3 Gabizon et al. (1994)
10.4  (5.4–26.8)(2.6–6.0)(131–501)(13.3–35.2)
SSL DOX20 5.65774.70.07 Working and Dayan (1996)
56.6
TLC D-99200.71 ± 0.3730.4 ± 32.521.4 ± 14.023.5 ± 15.6 Cowens et al. (1993)
8.2 ± 6.2
250.29 ± 0.0919.7 ± 17.718.8 ± 10.723.3 ± 15.7
6.68 ± 2.94
300.37 ± 0.1650.5 ± 44.98.2 ± 3.09.0 ± 7.8
25.0 ± 22.5
900.45 ± 0.6014.1 ± 16.614.6 ± 7.8 21.8 ± 15.5
13.5 ± 6.6 
TLC D-99300.2 ± 0.130.4 ± 25.87.1 ± 4.0 9.8 ± 10.7 Conley et al. (1993)
25.1 ± 35.5
DSPC/Chol (2:1)102.816.93.750.942 Gill et al. (1995)
 (daunorubicin)203.857.24.10.858
404.0120.13.70.630
608.3301.12.90.402
805.2375.32.90.396
Free daunorubicin800.7710.33105513.38   Forssen and Ross (1994)
DSPC:Chol (55:45) (VCR)2.01.95 ± 1.676.5 ± 0.64.35 ± 0.84 Embree et al. (1998)
22.5 ± 9.85
2.87.2 ± 4.840.2 ± 17.22.26 ± 0.47
99.3 ± 17.2
  • Errors are expressed as either a range (in parentheses) or as a S.D., depending on the source of the data. For expression of half-lives of elimination, the top value is the half-life associated with the first exponent of elimination, and the bottom value is the half-life associated with the second exponent of elimination.

  • T 1/2, half-life elimination of drug from the circulation; V d, volume of distribution; Cl, total plasma clearance.