Metabolism of the Hydroxyethylrutosides. II. Excretion and Metabolism of 3',4',7-Tri-<i>O</i>-(β-hydroxyethyl)rutoside and Related Compounds in Laboratory Animals after Parenteral Administration

Abstract

Abstract1. Following intravenous administration of 3',4',7-tri-O-(β-hydroxyethyl)-rutoside, 4'7-di-O-(β-hydroxyethyl)rutoside or 7-O-(β-hydroxyethyl)rutoside approximately two-thirds of the dose of each is excreted in the bile of cannulated rats in 24 h. Urinary excretion does not exceed 25% of the dose in this time. At doses up to 10 mg/kg, biliary excretion is maximal within 3 h, but at higher doses (40–100 mg/kg it is prolonged and variable. Intraperitoneal administration of these rutosides results in higher excretion in the bile. The hydroxyethylrutosides are excreted in bile and urine unchanged, and as glucuronide conjugates.2. In non-cannulated rats the major route of excretion of 3',4',7-tri-O-(β-hydroxyethyl)-rutoside and 4'7-di-O-(β-hydroxyethyl)rutoside is via the faeces, as the corresponding aglycone. 7-O-(β-hydroxyethyl)rutoside is similarly metabolized to the aglycone, which is then degraded by intestinal microflora to a compound which is absorbed and excreted in urine.3. Following intravenous administration of 3',4',7-tri-O-(β-hydroxyethyl)-rutoside to non-cannulated rabbits and rhesus monkeys, urinary excretion did not exceed 20% of the dose in 72 h. Between 13–16% of the glycoside was detected in the gall-bile of monkeys within 3 h of administration.