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新型血管扩张药非洛地平在人、狗、大鼠及小鼠体内的尿液代谢产物

Urinary metabolites of felodipine, a new vasodilator drug, in man, dog, rat and mouse.

作者信息

Weidolf L, Borg K O, Hoffmann K J

出版信息

Xenobiotica. 1984 Aug;14(8):657-66. doi: 10.3109/00498258409151463.

DOI:10.3109/00498258409151463
PMID:6495759
Abstract

The urinary excretion of total 14C after oral administration of 25 mg (approximately 1 mumol/kg) 14C-felodipine to man, and intragastric administration (5 mumol/kg) to dog, rat and mouse, was 70, 39, 44 and 53% dose, respectively, in 72 h. Metabolites of felodipine were separated and quantified by h.p.l.c. Unchanged felodipine and its oxidized analogue were not excreted by any of the species studies. Three metabolites, present in all species studied, were isolated from urine and identified as products of the oxidation of felodipine to its pyridine analogue followed by hydrolysis of one or both of the pyridine carboxylic acid esters.

摘要

给人体口服25毫克(约1微摩尔/千克)的14C-非洛地平,给狗、大鼠和小鼠胃内注射(5微摩尔/千克)后,72小时内14C的总尿排泄量分别为给药剂量的70%、39%、44%和53%。非洛地平的代谢产物通过高效液相色谱法进行分离和定量。所有研究的物种均未排泄出未变化的非洛地平及其氧化类似物。从所有研究物种的尿液中分离出三种代谢产物,鉴定为非洛地平氧化为其吡啶类似物后,一种或两种吡啶羧酸酯水解的产物。

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Urinary metabolites of felodipine, a new vasodilator drug, in man, dog, rat and mouse.新型血管扩张药非洛地平在人、狗、大鼠及小鼠体内的尿液代谢产物
Xenobiotica. 1984 Aug;14(8):657-66. doi: 10.3109/00498258409151463.
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引用本文的文献

1
Absorption, distribution and elimination of felodipine in man.非洛地平在人体内的吸收、分布及消除。
Drugs. 1985;29 Suppl 2:9-15. doi: 10.2165/00003495-198500292-00004.
2
Metabolism of [14C] felodipine, a new vasodilating drug, in healthy volunteers.新型血管舒张药物[14C]非洛地平在健康志愿者体内的代谢情况。
Drugs. 1987;34 Suppl 3:43-52. doi: 10.2165/00003495-198700343-00010.
3
Clinical pharmacokinetics of felodipine. A summary.非洛地平的临床药代动力学。综述。
Drugs. 1987;34 Suppl 3:16-27. doi: 10.2165/00003495-198700343-00005.
4
Felodipine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in hypertension.非洛地平。对其药效学和药代动力学特性以及在高血压治疗中的应用的综述。
Drugs. 1988 Oct;36(4):387-428. doi: 10.2165/00003495-198836040-00002.
5
Biliary secretion of felodipine metabolites in man after intravenous [14C]felodipine.静脉注射[14C]非洛地平后人体中其代谢产物的胆汁分泌情况。
Eur J Clin Pharmacol. 1990;38(5):421-4. doi: 10.1007/BF02336677.