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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。

相似文献

1
[Metabolism of etofenamate / Identification and analytic of metabolites, their pharmacological properties and species dependence of metabolism (author's transl)].[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)]
Arzneimittelforschung. 1981;31(1):9-16.
2
[Studies on metabolism and elimination of etofenamate by dogs (author's transl)].犬对依托芬那酯的代谢与排泄研究(作者译)
Arzneimittelforschung. 1981;31(1):21-6.
3
[Gas-liquid chromatographic determination of etofenamate/ Determination, method and use in biological material (author's transl)].[依托芬那酯的气-液色谱测定法/测定、方法及在生物材料中的应用(作者译)]
Arzneimittelforschung. 1981;31(1):17-21.
4
[Animal experimental evidence of the long-lasting efficacy of etofenamate by prolongation of the half-life after intramuscular application].[肌内注射后通过延长半衰期实现依托芬那酯长效疗效的动物实验证据]
Arzneimittelforschung. 1990 Mar;40(3):300-5.
5
[Renal elimination and metabolism of etofenamate in volunteers after administration of various doses].[不同剂量依托芬那酯给药后志愿者体内的肾脏排泄及代谢情况]
Arzneimittelforschung. 1990 Mar;40(3):311-6.
6
[Synthesis and properties of nuclear hydroxylated derivatives of flufenamic acid and etofenamate (author's transl)].氟芬那酸和依托芬那酯的核羟基化衍生物的合成与性质(作者译)
Arzneimittelforschung. 1982;32(3):183-6.
7
Etofenamate fatty acid asters. An example of a new route of drug metabolism.依托芬那酯脂肪酸星状物。药物代谢新途径的一个实例。
Drug Metab Dispos. 1982 Jan-Feb;10(1):55-60.
8
[Analysis of etofenamate. Particular determination in biological material (author's transl)].[依托芬那酯分析。生物材料中的特殊测定(作者译)]
Arzneimittelforschung. 1977;27(6B):1312-6.
9
[The mode of anti-inflammatory action of a topical non-steroidal anti-inflammatory drug, etofenamate].[一种外用非甾体抗炎药依托芬那酯的抗炎作用模式]
Nihon Yakurigaku Zasshi. 1987 Jan;89(1):15-24. doi: 10.1254/fpj.89.15.
10
[Pharmacology and toxicology of etofenamate. 2].[依托芬那酯的药理学与毒理学。2]
Arzneimittelforschung. 1977;27(6B):1333-40.