The Disposition and Metabolism of 3',4',7-Tri-O-(β-hydroxyethyl) rutoside and 7-Mono-O-(β-hydroxyethyl)rutoside in the Mouse

Abstract

1. Following intravenous administration of 3',4',7-tri-O-(β-hydroxy[¹⁴C₂]ethyl)rutoside or 7-mono-O-(β-hydroxy[¹⁴C₂]ethyl)rutoside to male mice, 68% of the dose of each is excreted in faeces as the corresponding hydroxyethyl-quercetin within 72 h of dosage. Mean urinary excretions of mono- and tri-hydroxyethylrutosides in 72 h were 27 and 21% respectively. Unchanged rutosides and their glucuronides were detected in urine.

2. In biliary-cannulated animals, the mean biliary excretion of both tri- and mono-hydroxyethylrutosides was 71%, in 24 h of dosage. In both cases most ¹⁴C was excreted in 3 h, as unchanged rutosides and glucuronide conjugates.

3. Fall of blood ¹⁴C concn. was rapid for both compounds. Neither compound was detected in brain but there was short-term accumulation in liver and kidney, and 2-3 h after dosage, most ¹⁴C for both compounds was associated with the gastro-intestinal contents.

4. Animals killed 72 h after dosage of either compound contained <7% of dose, mostly in the color and caecal contents.

5. Foetuses removed 3 h after dosage of either compound to the dams did not contain ¹⁴C; foetuses removed 5 min after dosage contained low levels of ¹⁴C, substantially below the maternal blood level and equiv. to <0·1% of dose in each case. No ¹⁴C was detected in amniotic fluid.