Rb | fb | CLint,vivo | CLint,hepatocyte uptake | CLint,media-loss assay | CLint,metabolic stability assay | |
---|---|---|---|---|---|---|
ml/min/kg | ||||||
Atorvastatin alone | 1.2a | 0.047a | 851 ± 137 | 2480 ± 238 | 403 | 7.39 |
+Rifampicin | 211 ± 35b | 663 ± 225c | 38.1 | 3.53 | ||
Pitavastatin alone | 0.65a | 0.021a | 571 ± 40 | 2940 ± 327 | 347 | 1.23 |
+Rifampicin | 91.6 ± 10.3c | 1040 ± 101c | 105 | 1.28 | ||
Pravastatin alone | 0.59a | 1.2a | 41.8 ± 11.7 | 74.3 ± 17.7 | 34.4 | 9.29 |
+Rifampicin | 9.95 ± 2.04 | 0.147 ± 11.211b | 7.16 | 2.06 | ||
Rosuvastatin alone | 0.65d | 0.065d | 1480 ± 562 | 1040 ± 90 | 533 | 6.65 |
+Rifampicin | 219 ± 20 | 276 ± 12c | 196 | 6.05 | ||
Cerivastatin alone | 0.7e | 0.083e | 169 ± 26 | 2930 ± 934 | 262 | 0.336 |
+Rifampicin | 24.2 ± 2.0c | 1310 ± 745 | 174 | 0.310 | ||
Fluvastatin alone | 0.53a | 0.019a | 458 ± 35 | 705 ± 1070 | 194 | 2.90 |
+Rifampicin | 98.9 ± 9.9c | 613 ± 572 | 136 | <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).