Excretion of methylproscillaridin in patients with a biliary fistula.

Abstract

Four patients with a biliary fistula received 0.5 mg 3H-methylproscillaridin as a single oral dose. 55% of the dose was excreted in bile, 16% in urine and 3% in faeces. More than 60% of the radioactivity excreted in bile and urine appeared within the first 24 hours. 78% of the radioactivity in bile consisted of CHCl3-insoluble metabolites of methylproscillaridin, incubation of which with beta-glucuronidase led to splitting off glucuronic acid from almost 80%. Methylproscillaridin can be regarded as the principal conjugated compound. TLC-separation of CHCl3-soluble compounds from bile showed identical running of radioactivity with methylproscillaridin, proscillaridin and scillarenin and three unknown metabolites P1, P2, and P3. In urine the CHCl3-soluble fraction averaged 16% to 34% of the total amount and was identified as methylproscillaridin, proscillaridin, scillarenin, P2 and P3. The relative composition of the total radioactivity in faeces amounted to 77% methylproscillardidin, 4% scillarenin and 12% polar metabolites.

• Authors: R Staud, N Rietbrock, H P Fassbender
• Journal: European journal of clinical pharmacology (Eur J Clin Pharmacol) Vol. 9 Issue 2-3 Pg. 99-103 (Dec 19 1975) ISSN: 0031-6970 [Print] Germany
• PMID: 1233271 (Publication Type: Journal Article)

Chemical References

• Bufanolides
• Glucuronates
• Proscillaridin

Topics

• Aged
• Bile (metabolism)
• Bile Ducts
• Bufanolides (metabolism)
• Catheterization
• Chromatography, Thin Layer
• Feces (analysis)
• Female
• Glucuronates (biosynthesis)
• Humans
• Male
• Middle Aged
• Proscillaridin (analogs & derivatives, metabolism)
• Time Factors