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大鼠体内的左旋布诺洛尔代谢:尿中代谢物的鉴定

l-Bunolol metabolism in rats: identification of urinary metabolites.

作者信息

Leinweber F J, Szpiech J M, Di Carlo F J

出版信息

J Pharm Sci. 1978 Jan;67(1):129-31. doi: 10.1002/jps.2600670138.

Abstract

Urine collected for 24 hr from rats given a single oral dose of 3H-l-bunolol (10 mg/kg) was found to contain only 25.8% of the dose and more than 30 labeled compounds. Nine compounds were identified and quantified as follows: bunolol (0.35% of urinary tritium), bunolol glucuronide (5.12%), bunolol sulfate (0.08%), dihydrobunolol (0.08%), dihydrobunolol glucuronide (0.74%), dihydrobunolol sulfate (0.12%), hydroxydihydrobunolol (0.58%), beta-(5-oxytetralonyl)lactic acid (0.74%), and (5-oxytetralonyl) acetic acid glucuronide (1.12%). The total quantity of identified labeled compounds was only 2.3% of the dose and 8.9% of the urinary radioactivity.

摘要

给大鼠单次口服剂量为3H-1-布诺洛尔(10毫克/千克)后,收集其24小时尿液,发现尿液中仅含有25.8%的剂量以及30多种标记化合物。鉴定并定量了9种化合物,具体如下:布诺洛尔(占尿中氚的0.35%)、布诺洛尔葡糖醛酸苷(5.12%)、布诺洛尔硫酸盐(0.08%)、二氢布诺洛尔(0.08%)、二氢布诺洛尔葡糖醛酸苷(0.74%)、二氢布诺洛尔硫酸盐(0.12%)、羟基二氢布诺洛尔(0.58%)、β-(5-氧代四氢萘甲酰基)乳酸(0.74%)以及(5-氧代四氢萘甲酰基)乙酸葡糖醛酸苷(1.12%)。已鉴定的标记化合物总量仅为剂量的2.3%,占尿中放射性的8.9%。

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