TABLE 1

Clearance parameters from the literature and calculated Clint and Clh values (ml/min/kg) for the 27 compounds analyzed

CLin vivoaCLint,in vivobfuBcRBdSuspended CLinteSuspended CLhRelay Method CLintgRelay Method CLhPlated CLinthPlated CLhHepatoPac ClintiHepatoPac CLh
With BindingfWithout BindingfWith BindingfWithout BindingfWith BindingfWithout BindingfWith BindingfWithout Bindingf
ml/min/kgml/min/kg
Alprazolam0.5911.60.3810.7612.10.771.94.01.43.3
Antipyrine0.5720.600.9720.670.630.651.31.21.2
Atazanavir8.711080.1411.01142.310.218.1
Atomoxetine3.912050.02410.55170.91.516.0
Diazepam0.38118.30.02110.7116.60.145.015.00.318.72.810.062.512.20.267.7
Diclofenac4.215830.00910.55186.80.7616.7294.02.419.3
Disopyramide0.936.30.1531.224.80.703.9
Flecanide9.1137.10.4410.8912.51.12.3
Glimepiride0.62170.30.00910.5519.40.096.572.20.6416.1
Ketoprofen1.2274.90.017211.00.197.217.00.299.3
Lidocaine9.2146.40.3610.84115.34.38.829.16.912.1
Meloxicam0.15130.70.00511.22 14.60.023.8
Metroprolol13.3246.50.8025.33.54.2
Midazolam4.612040.02920.6911383.418.058.221.615.3238.45.219.0
Naproxen0.1116.10.01821.40.031.318.00.329.6
Prednisolone2.429.70.2811.01306.012.26.71.75.1
Ranitidine2.924.40.7723.02.12.63.12.12.7
Riluzole3.513610.01211.7196.01.117.0
Risperidone3.6126.20.1610.67134.14.412.9
Theophylline1.112.30.4810.8512.61.22.32.81.32.53.21.42.8
Timolol11248.90.4824.41.93.614.05.18.4
Tolbutamide0.1711.60.1110.5510.380.040.377.40.755.51.110.121.14.60.473.8
Verapamil13.323100.12233.43.412.8
Voriconazole3.8111.10.4211.0325.37.011.4
Warfarin0.04512.50.01810.5514.20.083.53.60.063.0
Zolmitriptan6.7113.010.7541.013.52.33.0
Zolpidem4.3231.90.1728.01.35.8
  • a The superscript numbers represent the following references: 1, Chan et al. (2013); 2, Hallifax et al. (2010); 3, Di et al. (2012).

  • b Clint in vivo back-calculated from Cltotal using eq. 3, except for zolmitriptan; the superscript number 1 represents Di et al. (2012).

  • c Data from the literature or calculated from reported fu and Rb (fub = fu/Rb). The superscript numbers represent the following: 1, fu from Chan et al. (2013); 2, fub referenced in Hallifax et al. (2010); 3, Aitio (1981); 4, Dixon and Warrander (1997).

  • d The superscript numbers represent the following references: 1, Chan et al. (2013); 2, Hinderling et al. (1974); or 3, not available (assumed to be 1).

  • e Represents results from Hallifax et al. (2010).

  • f Clh calculated using the well-stirred model (eq. 2) either with or without fub.

  • g Represents results from Di et al. (2012, 2013).

  • h The superscript numbers represent the following references: 1, Smith et al. (2012); 2, Blanchard et al. (2005) (scaled in vitro data using eq. 1).

  • i In vitro Clint value obtained from back-calculated in vitro scaled CLh (Chan et al., 2013) using the well-stirred model (modified eq. 3).

  • —, no data available.