Characterization of metabolites of Δ8,9-dehydroestrone in dogs

✍ Scribed by A. Chandrasekaran; M. Osman; P. Raveendranath; K. Chan; J. A. Scatina; S. F. Sisenwine

• Publisher: John Wiley and Sons
• Year: 1995
• Tongue: English
• Weight: 527 KB
• Volume: 30
• Category: Article
• ISSN: 1076-5174
• DOI: 10.1002/jms.1190301017

✦ Synopsis

Abstract

Δ^8,9^‐Dehydroestrone is the fifth most abundant component in the conjugated equine estrogen preparation Premarin®, representing about 2 to 6% of the total steroids in the tablet. The metabolism of this estrogen has been determined in female beagle dogs after acute peroral administration. 17β‐Dihydro‐Δ^8,9^‐dehydroestrone(17β‐Δ^8,9^‐dehydroestradiol) and 17α‐dihydro‐Δ^8,9^dehydroestrone(17α‐Δ^8,9^‐dehydroestradiol) have been identified as the major metabolites in plasma and urine. These metabolites, along with the unchanged drug, were isolated and purified by ether extraction and thin‐layer chromatography of the urine samples after enzyme hydrolysis. The trimethylsilyl ether derivatives of the isolated metabolites were characterized by comparison of their mass spectra and chromatographic properties with those of synthetic reference standards.