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[依托芬那酯的代谢/代谢产物的鉴定与分析、其药理学特性及代谢的物种依赖性(作者译)]

[Metabolism of etofenamate / Identification and analytic of metabolites, their pharmacological properties and species dependence of metabolism (author's transl)].

作者信息

Dell H D, Doersing M, Fischer W, Fiedler J, Jacobi H, Kamp R

出版信息

Arzneimittelforschung. 1981;31(1):9-16.

PMID:6971113
Abstract

After oral application of etofenamate to animals (rat, rabbit, dog, monkey) unchanged etofenamate and numerous metabolites are found in urine. Analytical properties (thin-layer chromatographic behavior, UV- and fluorescence data) of etofenamate, 5-hydroxy-, 4'-hydroxy, 5,4'-dihydroxy-etofenamate, flufenamic acid, 5-hydroxy-, 4'-hydroxy-, 5,4'-dihydroxy-flufenamic acid are described. Derivatives of etofenamate and flufenamic acid are excreted by rabbit, dog, monkey and man, whereas flufenamic acid derivatives are excreted preferentially by rats; profound degradation takes place in dogs. Metabolism in man is more similar to monkey than to dog and rodents. Metabolic pattern after oral and cutaneous application is quite similar. The six hydroxy derivatives have no pharmacological activity--they do not contribute to the pharmacological action of the substance.

摘要

给动物(大鼠、兔子、狗、猴子)口服依托芬那酯后,在尿液中可发现未变化的依托芬那酯及多种代谢物。描述了依托芬那酯、5-羟基-、4'-羟基、5,4'-二羟基-依托芬那酯、氟芬那酸、5-羟基-、4'-羟基-、5,4'-二羟基-氟芬那酸的分析特性(薄层色谱行为、紫外和荧光数据)。依托芬那酯和氟芬那酸的衍生物可由兔子、狗、猴子和人排出,而氟芬那酸衍生物在大鼠中优先排出;狗体内会发生深度降解。人体的代谢与猴子比与狗和啮齿动物更为相似。口服和皮肤给药后的代谢模式相当相似。这六种羟基衍生物无药理活性——它们对该物质的药理作用无贡献。

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