Metabolism of the Hydroxyethylrutosides Biliary and Urinary Excretion of 3′,4′,5-[Hydroxyethyl-¹⁴C], 7-Tetra-<i>O</i>-(β-Hydroxyethyl)-rutoside in Rats and Monkeys after Parenteral Administration

Abstract

1. 3′,4′,5-[Hydroxyethyl-*C],7-tetra-O-(β-hydroxyethyl)rutosideis rapidly excreted unchanged, in both urine (42–71% dose in 24 h) and in bile (15–39% in 24 h) following parenteral administration of a single dose (3–8 mg/kg body wt.). Biliary excretion is max. within the first 3 h and virtually complete by 24 h at this dosage.2. Excretion of the glycoside in the urine of non-cannulated rats amounted to 32–70% dose in 24 h. Between 14–23% of the parenterally administered dose was extracted from the faeces of non-cannulated rats, mostly as the [14C] aglycone.3. Following intravenous administration of the glycoside to non-cannulated rhesus monkeys 50–58% dose was excreted in the urine and 19–27% was found to be excreted into the gall bladder.