Uesugi Takashi, Ikeda Mariko, K. Yoshiaki
Aug 15, 1974
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Journal
Biochemical Pharmacology
Abstract
Abstract Thiamphenicol (TP) or chloramphenicol (CP) administered intravenously (14 μmoles) to rats with ligated renal pedicles is rapidly excreted in bile mostly as the glucuronide (about 23 and 75 per cent in 7 hr respectively). Increasing the dose of either drug does not result in an increased excretion of glucuronide, indicating that the excretion process is saturable. TP glucuronide (TPG) or CP glucuronide (CPG) administered intravenously to rats with ligated renal pedicles is rapidly excreted into bile in high concentration as unchanged glucuronide. The maximal excretion rate of TPG or CPG (about 14.0 and 18.0 gmmoles/10 min respectively) when each glucuronide (100 μmoles) was administered is much higher than that (about 5.1 and 8.5 gmmoles/10 min respectively) when each aglycone (200 μmoles) was administered. The results suggest that the transport maxima (Tms) for the biliary excretion of TP and CP are due to a saturation of the conjugating process. CPG used in this study is isolated by a new method.