质量平衡和代谢[H](3)在健康男性Formoterol结合静脉输液和口服administration-mimicking吸入。
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Rosenborg J,拉尔森P Tegner K·海尔萨姆G
质量平衡和代谢[H](3)在健康男性Formoterol结合静脉输液和口服administration-mimicking吸入。
药物金属底座Dispos。1999年10月27日(10):1104 - 16。
- PubMed ID
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10497135 (在PubMed]
- 文摘
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质量平衡和代谢formoterol了六个健康男性在一个开放的研究。平均年龄为49.7岁(范围:40 - 63)。同时口服(平均剂量88.6 nmol 49.3兆贝可)和增长值(平均剂量38.2 nmol, 21.4兆贝可)剂量的出现formoterol接种。这两届政府旨在模拟的结合吸入formoterol的命运。总放射性监测24小时在血浆和尿液和粪便中至少4天。Formoterol和代谢物测定使用液相色谱+ radiodetection,离心后直接在尿液和血浆样本检查后和粪便。尿液中代谢物被确定,抽样从两个主题,使用液态chromatography-electrospray电离质谱分析。意味着管理formoterol剂量的总回收率为86%,62%,尿液和粪便的24%。氚化水生成,因为其体内流动缓慢,终端总放射性剂量缓慢复苏的下降在采样周期是不完整的。Formoterol共轭是不活跃的硫酸葡糖苷酸和未知。 The phenol glucuronide of formoterol was the main metabolite in urine. Formoterol was also O-demethylated and deformylated. Plasma exposure to these pharmacologically active metabolites was low. O-demethylated formoterol was seen mainly as inactive glucuronide conjugates and deformylated formoterol only as an inactive sulfate conjugate. Intact formoterol and O-demethylated formoterol dominated recovery in feces. Mean recovery of unidentified metabolites was 7. 0% in urine and 2.0% in feces.
