Pharmacokinetic parameters for taurocholate and rosuvastatin in humans and a comparison of human nonrenal (hepatic) clearance (CLH, vivo) with the biliary clearance in vitro predicted from the uptake clearance in SCHH (CLH, vitro)

CLH, PRBCLH, vivofBCLH,vitro (5 h)CLH,vitro (96 h)
ml · min1 · kg1ml · min1 · kg1ml · min1 · kg1 (CLH, vitro/CLH, vivo ratio)
Taurocholate0.6a20.7b0.4c9.50 (0.459)8.58 (0.415)10.9 (0.529)8.66 (0.418)10.4 (0.502)7.14 (0.345)
Rosuvastatin4.83d0.6a8.06d0.18d2.65 (0.329)2.99 (0.372)3.23 (0.401)2.74 (0.341)2.71 (0.337)1.99 (0.247)
  • CLH, P, the hepatic clearance in vivo based on the plasma concentration was assessed as the difference between the total plasma clearance and the renal plasma clearance for each compound; RB, ratio of the blood concentration to the plasma concentration of each compound; fB, unbound fraction of each compound in the total blood.

  • a Blood/plasma concentration ratio of these compounds in humans was assumed to be 0.6.

  • b Biliary clearance of taurocholate was assumed to be the same as the hepatic blood flow rate.

  • c There are no data for the blood unbound fraction of taurocholate in humans, so we used the value for rats (Inoue et al., 1985).

  • d These data were obtained from the interview form of CRESTOR.