Hepatobiliary elimination of bendamustin (Cytostasan) in rats. |
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Authors: | S Bezek V Scasnár T Trnovec R Grupe |
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Institution: | Institute of Experimental Pharmacology, Slovak Academy of Sciences, Bratislava, CSFR. |
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Abstract: | Biliary excretion of bendamustin (Cytostasan, 5-bis(2-chloroethyl)amino]-i-methylbenzimidazole-2-butyric acid; 1) and its metabolites was studied in rats after i.v. administration of 14C-1. The most significant finding was the rapid excretion of 1 related radioactivity in the bile occurring shortly after injection. While radioactivity eliminated by bile within 2 h was 41.8%, in the course of subsequent 22 h it amounted only to 3.2%. Bile samples analyzed by TLC indicated that the total amount of radioactivity was excreted in the form of conjugates and two hydroxy metabolites. A significant amount of radioactivity was excreted in urine. The diversion of bile by cannulation of the bile duct led to a significant decrease of elimination by feces. |
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