Biopharmaceutical Study of the Hepatobiliary Transport of Drugs. VI. Inhibition of Active Biliary Excretion of Organic Cations by Retrograde Infusion

概要

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The new method employed to organic anions was applied to investigate the active excretory process of organic cations from liver cells to bile canaliculi. Biliary excretion of acetyl procaineamide ethobromide (APAEB) and quinine in rats was studied after infusing retrogradely a solution of various reagents from the cannulated common bile duct into the biliary trees. Among the tested reagents, surfactants, sulfhydryl reagents and aminoreactive agents remarkably inhibited the active biliary excretion of organic cations. The concentrations in bile, the amounts excreted for 30 minutes and the bile/plasma ratios of APAEB were decreased to about 1/2-1/3 of their values at the sham operation by the treatment with these reagents. Because of the intensive decrease in the B/L ratios compared to the L/P ratios, the reagents are supposed to act locally on the bile canalicular site of the liver plasma membrane and to inhibit the active excretory process of organic cations. As compared with organic anions, the biliary excretion of organic cations was more sensitive to the treatment with sulfhydryl reagents and less sensitive to the solubilizing effect of surfactants and organic solvents.
公益社団法人日本薬学会の論文
1977-03-25