TABLE 4

CLint,vivo of statins versus with CLint determined by hepatocyte uptake, media loss, and metabolic stability assays

Data are presented as the mean ± S.E. for CLint,vivo and CLint,hepatocyte uptake assay and as the mean of two determinations for CLint,media-loss assay and CLint,metabolic stability assay.

RbfbCLint,vivoCLint,hepatocyte uptakeCLint,media-loss assayCLint,metabolic stability assay
ml/min/kg
Atorvastatin alone1.2a0.047a851 ± 1372480 ± 2384037.39
 +Rifampicin211 ± 35b663 ± 225c38.13.53
Pitavastatin alone0.65a0.021a571 ± 402940 ± 3273471.23
 +Rifampicin91.6 ± 10.3c1040 ± 101c1051.28
Pravastatin alone0.59a1.2a41.8 ± 11.774.3 ± 17.734.49.29
 +Rifampicin9.95 ± 2.040.147 ± 11.211b7.162.06
Rosuvastatin alone0.65d0.065d1480 ± 5621040 ± 905336.65
 +Rifampicin219 ± 20276 ± 12c1966.05
Cerivastatin alone0.7e0.083e169 ± 262930 ± 9342620.336
 +Rifampicin24.2 ± 2.0c1310 ± 7451740.310
Fluvastatin alone0.53a0.019a458 ± 35705 ± 10701942.90
 +Rifampicin98.9 ± 9.9c613 ± 572136<0
  • a Watanabe et al., 2010.

  • b P < 0.05 versus values in the absence of rifampicin.

  • c P < 0.01 versus values in the absence of rifampicin.

  • d Calculated from the PMDA-approved package data.

  • e Calculated from the unbound fraction in the plasma (fu,p) and the blood-to-plasma concentration ratio (Rb) data (Paine et al., 2008).