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芬氯酸代谢与排泄的种属差异。

Species differences in the metabolism and excretion of fenclofenac.

作者信息

Greenslade D, Havler M E, Humphrey M J, Jordan B J, Rance M J

出版信息

Xenobiotica. 1980 Oct;10(10):753-60. doi: 10.3109/00498258009033803.

Abstract
  1. The excretion and metabolism of radiolabelled fenclofenac (2-(2,4-dichlorophenoxy)phenylacetic acid, Flenac) has been studied in five species. 2. In the rat, absorption of oral doses of fenclofenac was virtually complete and elimination occurred mainly by the bile and faeces. The guinea-pig excreted equal amounts of radioactivity in urine and faeces, while in rabbit, baboon and man renal excretion was the more important route. 3. In all species the majority of excreted radioactivity was present as fenclofenac ester glucuronide. Amino acid conjunction with fenclofenac was minimal in all species studied. 4. Mono- and di-hydroxylated metabolites have been detected in urine from guinea-pig, baboon and man. The major hydroxylated metabolite in baboon urine has been identified as 2-(2,4-dichlorophenoxy)-5'-hydroxyphenylacetic acid.
摘要
  1. 已在五个物种中研究了放射性标记的芬氯酸(2-(2,4-二氯苯氧基)苯乙酸,Flenac)的排泄和代谢情况。2. 在大鼠中,口服芬氯酸的吸收几乎是完全的,消除主要通过胆汁和粪便进行。豚鼠尿和粪便中排出的放射性物质数量相等,而在兔、狒狒和人类中,肾脏排泄是更重要的途径。3. 在所有物种中,排出的放射性物质大部分以芬氯酸酯葡糖醛酸苷的形式存在。在所有研究的物种中,芬氯酸与氨基酸的结合极少。4. 在豚鼠、狒狒和人类的尿液中检测到了单羟基和二羟基代谢物。狒狒尿液中的主要羟基化代谢物已被鉴定为2-(2,4-二氯苯氧基)-5'-羟基苯乙酸。

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