Table 2

Estimation of CLint, in vivo from in vivo pharmacokinetic data for the model compounds in rats, dogs, and humans

CompoundsSpeciesCLoral or CLtotFafpRBCLint, in vivoEHReference
Well StirredParallel-TubeDispersion
ml/min/kg body weight ml/min/kg body weight
FK1052Rat8750.950.031.2127708.335785.607952.740.93In house data
Dog62.70.0170.823503.821802.282114.040.70
Human26.40.0160.781567.50945.951071.180.61
FK480Rat81.10.700.010.6265677.003358.323824.300.62In house data
Dog6.60.0060.6770.00687.51709.160.20
Human2.40.0050.6336.00315.14320.790.12
ZolpidemRat1060.890.130.89725.69405.00466.880.66 Ishibashi et al. (1993a,b)
Human7.10.040.66157.98129.84137.310.32 Kudo et al. (1990)
OmeprazoleRat7101.000.1250.785680.00985.691393.010.94 Watanabe et al. (1994)
Dog6.32-a 0.0970.6098.3879.3684.030.34 Regårdh et al. (1985)
Human22.20.0420.62528.57306.86350.730.63 Andersson et al. (1990)
NicardipineRat12121.000.0841.02-b 14428.572059.222992.550.96 Higuchi and Shiobara (1980a,b)
Dog5970.0621.02-b 9629.031500.952154.280.95
Human1310.0681.02-b 1926.47606.32779.700.86
NilvadipineRat28521.000.01170.922243760.6817589.9427932.160.98 Tokuma et al. (1987, 1988)
Dog360.0080.8364500.002818.313170.520.58 Terakawa et al. (1988)
Human1070.0130.7898230.772539.973277.200.87 Niwa et al. (1987); in house data
DiazepamRat103.81.000.1371.04757.66432.66496.310.64 Diaz-Garcia et al. (1992); Luurila et al. (1996)
Human0.70.0321.0421.8821.5321.530.03 Navia and Chaturvedi (1996); Sawada et al. (1985);Klotz et al. (1976)
DiltiazemRat300.21.000.1840.931631.52536.77684.980.85 Tsui et al. (1994); Etoh et al. (1983)
Dog201.60.2981.02-b 676.54209.27269.910.87 Kölle et al. (1983); Levet-Trafit et al. (1996)
Human64.20.221.0291.82132.79159.590.76 Lee et al. (1992); Piepho et al. (1982)
  • 2-a  CLtot.

  • 2-b  Assumed value.