抱合型薬物の代謝研究(第2報)3-デオキシエストラジオール17-サルフェートその2その可能な代謝物の高速液体クロマトグラフィーによる定量法の確立

概要

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To investigate the metabolic pattern of such a drug having two counter functional groups in the molecule : a hydrophylic sulfate group and a hydrophobic aromatic ring, as 17-sulfate of 17β-hydroxyestra-1,3,5 (10)-triene (3-deoxyestradiol) was incubated with rat hepatic microsomes under a reduced nicotinamide adenine dinucleotide phosphate-generating system. The metabolites assigned were mono-and dihydroxylated products hydroxylated only at the aromatic ring. The phenolic products having hydroxyl group at the position 2,3,or 4 were detected in the male and female rats. The two catechol products having hydroxyl groups at 2,3 and 3,4 were detected only in the male rats. No other metabolites were formed except a phenol product hydroxylated at the position 1 in the case of the male rats. These metabolisms were confirmed to proceed without removal of the sulfate group. A simple method for the determination of these metabolites was established by using reversed-phase high-performance liquid chromatography. The devised technique involves an elution with a mixture of 0.5% NH_4H_2PO_4 (pH 3.0) and methanol on a TSK-Gel ODS-120A column with electrochemical and/or ultraviolet detectors.
社団法人日本薬学会の論文
1989-05-25