In Vitro Glucuronidation Ratesa | Glucuronide Excretionb | |||
---|---|---|---|---|
HLM | Hepatocytesc | Urine (0–168 h) | Bile (3–8 h) | |
pmol/(min · mg protein) | pmol/(min · 106 cells) | %dose | ||
Muraglitazar | 33 | 60 | 0.81 | 15 |
Peliglitazar | 32 | 49 | 0.24 | 16 |
↵a The substrate concentration was 5 and 10 μM, respectively, for hepatocyte and microsomal incubations.
↵b Excretion of muraglitazar AG and peliglitazar AG in humans after oral administration of 14C-labeled compounds (20 mg/subject, 100 μCi). Urinary elimination represented 2.13 and 1.24% of dose and biliary elimination represented 39.9 and 24.43% of dose, respectively, for muraglitazar and peliglitazar.