TABLE 2

Pharmacokinetic parameters for repaglinide and inhibition parameters

ParametersUnitsValuesSources
Bioavailability0.625Hatorp, 2002
CLtot (plasma)l/h32.6Hatorp, 2002
CLtot (blood)l/h52.6CLtot (plasma) / Rb
fe0.001van Heiningen et al., 1999
CLh (blood)l/h52.6Assuming CLr = 0
Fh0.401-CLh/Qh
FaFg1Bioavailability > Fh
fp0.015Hatorp, 2002
fb0.025fp / Rb
Rb0.6van Heiningen et al., 1999
Doseμg250Niemi et al., 2003a
kah−14.51 ± 1.87*
Lagh1.20 ± 0.06*
Vbl8.38 ± 9.02*
fh·CLintl/h5.63 ± 4.88*
fb·PSinfl/h192 ± 127*
fh·PSeffl/h15.4Yabe et al., 2011; Ménochet et al., 2012; Jones et al., 2012
k12h−12.62 ± 3.60*
k21h−11.23 ± 0.30*
fm2C80.801 ± 0.049*
Ki,3A4,iczμg/l0.0477 ± 0.0365*
Ki,app,2C8μM20Ogilvie et al., 2006
kinact,2C8h−112.6Ogilvie et al., 2006
kdeg,2C8h−10.03013Yang et al., 2008
Ki,1B1,gemμg/l3,560 ± 2,530*
Ki,1B1,glu/Ki,1B1,gem0.385Shitara et al., 2004; Nakagomi-Hagihara et al., 2007
  • * Optimized by fitting analysis.