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2-(对甲基烯丙基氨基苯基)丙酸(阿明洛芬)在人体单次及多次口服给药后的药代动力学

Pharmacokinetics of 2-(p-methylallylaminophenyl) propionic acid, alminoprofene, in man after single and multiple oral doses.

作者信息

Premel-Cabic A, Allain P, Pidhorz L, Streichenberger G

出版信息

Eur J Clin Pharmacol. 1980 Nov;18(5):419-22. doi: 10.1007/BF00636796.

DOI:10.1007/BF00636796
PMID:7439265
Abstract

2-(p-methylallylaminophenyl) propionic acid, alminoprofene (INN), a new antalgic drug, was administered orally to men as a single (300 mg) and multiple doses (300 mg three times daily). Plasma and urine concentrations of alminoprofene were determined by gas-liquid chromatography. After the single oral dose, the peak plasma level (36.2 to 41.5 mg/l) was reached within 0.5 -1.5 h. the biological half-life ranged from 2.5 to 3.2 h. During chronic administration of alminoprofene, steady-state equilibrium was established within 24 h. The urinary excretion of alminoprofene as unchanged product and as glucuronide was very important.

摘要

2-(对甲基烯丙基氨基苯基)丙酸,阿明洛芬(国际非专利药品名称),一种新型镇痛药,以单次剂量(300毫克)和多次剂量(每日三次,每次300毫克)口服给予男性受试者。采用气液色谱法测定血浆和尿液中阿明洛芬的浓度。单次口服给药后,在0.5至1.5小时内达到血浆峰值水平(36.2至41.5毫克/升)。生物半衰期为2.5至3.2小时。在阿明洛芬的长期给药过程中,24小时内建立了稳态平衡。阿明洛芬以未变化产物和葡糖醛酸苷形式的尿排泄非常重要。

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本文引用的文献

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GLC determination of ibuprofen ((plus or minus)-2-(p-isobutylphenyl)propionic acid) in plasma.血浆中布洛芬((±)-2-(对异丁基苯基)丙酸)的葡萄糖氧化酶法测定
J Pharm Sci. 1974 Feb;63(2):219-21. doi: 10.1002/jps.2600630208.
2
[Biological behavior: serum levels, excretion and biotransformation of (3-benzoylphenyl)-2-propionic acid, or ketoprofen, in animals and men].[生物学行为:(3-苯甲酰基苯基)-2-丙酸或酮洛芬在动物和人体中的血清水平、排泄及生物转化]
Ann Pharm Fr. 1973 Dec;31(12):735-49.