1重水素標識化合物を用いたSelected Ion Monitoring(SIM)によるBefunolol代謝物の2種Glucuronideの定量に関する基礎的検討

概要

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Selected ion monitoring has heen developed for the determination of two glucuronides detected in human urine after oral administration of befunolol(BF). It was confirmed that not only multi-deuterium labelled compound(I-d6)but also mono-deuterium labelled one(I-d1)were useful internal standard at determination of the common aglycone, 2-(1-hydroxyethyl)-7-(2-hydroxy-3-isopropylaminopropoxy)benzofuran of these glucuronides. The glucuronides had been identified as O-glucuronide of side-chain of I(II)and O-glucuronide of 2-side-chain of I(III). Each glucuronide was determined by the combination of enzymatic hydrolysis, thin layer chromatography and selected ion monitoring using II-d1 as internal standard. The overall recoveries(%)of II and III were 101.3±1.9(SE)and 101.1±1.4(SE)respectively. Over 70% of dose determined as I, II and III in the urine of man received BF 15-20 mg orally. It can therefore be presumed that major metabolic pathway of BF in man is the reduction followed by the glucuronidation.
日本質量分析学会の論文