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In order to clarify the relationship between biliary excretion of antibiotics and bile acid, the concentrations of Cefoperazone (CPZ) and bile acid in bile were measured by HPLC in 8 patients, 4 with T-tube drainage and 4 with percutaneous transhepatic biliary drainage.The biliary excretion rate of CPZ in 6h at the time of jaundice release (more than 3 weeks after the biliary drainage had started) was extremely low, 0.03-1.4% of the intravenously injected dose of 1.0g. The biliary excretion of CPZ after the administration of ursodeoxy cholate rose to 1.1 to 28 times the preadministration level. After reopening of the enterohepatic circulation of bile acid by surgical bypass, it was 1.3 to 41 times the preadministration level. Especially the marked increase was observed in the patients without severe hepatic dysfunction. There was a significant correlation between biliary excretion of total bile acid and the total biliary excretion of CPZ in 6h. We conclude that the concentration of biliary bile acid is one of the factors affecting the transfer of injected CPZ to bile. This fact is important with respect to the treatment of biliary infections.

Clinical study of the relationship between the biliary excretion of antibiotics and bile acid.