Metabolism, Distribution and Excretion of 2, 2, 3, 3, 3-Pentafluoropropanol in Rats

K. Minegishi, A. Takahashi
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引用次数: 4

Abstract

The elimination and metabolism of 2, 2, 2, 3, 3-pentafluoropropanol (5-FP) were investigated in male and female rats for 7 d after a single oral administration at doses of 4, 40, and 400 mg/kg. 5-FP glucuronide and 2, 2, 3, 3, 3-pentafluoropropionic acid (5-FPA) as major metabolites were determined by head-space analysis using GC-MS in the selected ion monitoring-mode. 5-FP glucuronide and 5-FPA were found in urine and feces of both male and female rats. The cumulative excretion of 5-FP in the urine was 28.6-59.3% of the dose and only 0.46-1.28% in the feces in both sexes. A sex-related difference in urinary excretion of 5-FPA was observed in the two dose levels (4 and 40 mg/kg). The recoveries of 5-FPA in the urine of rats administered 5-FP were 10.7-11.9% in male and 33.0-38.2% in female by 7 d post treatment. The sex-related difference of biological half-lives (t1/2) were also observed in some tissues such as liver, kidney and blood.
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2,2,3,3,3 -五氟丙醇在大鼠体内的代谢、分布和排泄
在雄性和雌性大鼠单次口服4、40和400 mg/kg剂量后7 d,研究了2,2,2,3,3 -五氟丙醇(5-FP)的消除和代谢。选择离子监测模式,采用气相色谱-质谱法顶空分析测定5-FP葡萄糖醛酸和2,2,3,3,3 -五氟丙酸(5-FPA)为主要代谢物。在雄性和雌性大鼠的尿液和粪便中均检测到5-FP葡糖苷和5-FPA。两性尿中5-FP的累积排泄量为剂量的28.6-59.3%,粪便中5-FP的累积排泄量仅为剂量的0.46-1.28%。在两种剂量水平(4和40 mg/kg)下,尿中5-FPA的排泄量存在性别差异。给药后7 d,雄大鼠尿液中5-FPA的回收率为10.7 ~ 11.9%,雌大鼠尿液中5-FPA的回收率为33.0 ~ 38.2%。在肝脏、肾脏和血液等组织中,生物半衰期(t1/2)也存在性别差异。
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