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使用高效液相色谱法来阐明速尿及其代谢产物的代谢和尿排泄情况。

The use of HPLC to elucidate the metabolism and urinary excretion of furosemide and its metabolic products.

作者信息

Andreasen F, Christensen C K, Jakobsen F K, Mogensen C E

出版信息

Acta Pharmacol Toxicol (Copenh). 1981 Sep;49(3):223-9. doi: 10.1111/j.1600-0773.1981.tb00897.x.

DOI:10.1111/j.1600-0773.1981.tb00897.x
PMID:7336980
Abstract

Three principles for the use of HPLC with spectrophotometric detection to determine the concentration of furosemide and of 4-chloro-5-sulfamoyl anthranilic acid (CSA) were studied. A reversed phase microbondapack C18 column was used for the separation of either unchanged furosemide (I), CSA (II) or the diazo product of CSA (III). The sensitivity of the methods for the determination of furosemide added to serum in vitro were for I 0.05, for II 0.020 and for III 0.01 microgram/ml. The methods I and II were used to study the excretion pattern in the urine of furosemide and CSA after intravenous injection of 80 mg to 10 normal subjects. An average of 48.1 +/- 9.8% (S.D.) of the furosemide was excreted during the first hour as unchanged furosemide. Simultaneously 1.9 +/- 0.8% of the dose was excreted as CSA. Only very low concentrations of CSA were found in serum and that metabolite apparently was excreted with a higher renal clearance than furosemide during the period 30-60 min. after the administration (30.3 +/- 145 ml/min. for CSA and 88 +/- 23 ml/min. for furosemide). During the 24 hour period following the administration 52.6 +/- 8.1 mg was excreted as unchanged furosemide and 11.4 +/- 5.2 mg as a glucuronidated product.

摘要

研究了使用高效液相色谱-分光光度检测法测定呋塞米和4-氯-5-氨磺酰基邻氨基苯甲酸(CSA)浓度的三项原则。使用反相微径键合硅胶C18柱分离未变化的呋塞米(I)、CSA(II)或CSA的重氮产物(III)。体外测定血清中添加的呋塞米的方法灵敏度,对于I为0.05,对于II为0.020,对于III为0.01微克/毫升。方法I和II用于研究10名正常受试者静脉注射80毫克后呋塞米和CSA在尿液中的排泄模式。平均48.1±9.8%(标准差)的呋塞米在第一小时以未变化的呋塞米形式排泄。同时,1.9±0.8%的剂量以CSA形式排泄。在血清中仅发现极低浓度的CSA,并且在给药后30 - 60分钟期间,该代谢物的肾清除率明显高于呋塞米(CSA为30.3±145毫升/分钟,呋塞米为88±23毫升/分钟)。在给药后的24小时内,52.6±8.1毫克以未变化的呋塞米形式排泄,11.4±5.2毫克以葡萄糖醛酸化产物形式排泄。

相似文献

1
The use of HPLC to elucidate the metabolism and urinary excretion of furosemide and its metabolic products.使用高效液相色谱法来阐明速尿及其代谢产物的代谢和尿排泄情况。
Acta Pharmacol Toxicol (Copenh). 1981 Sep;49(3):223-9. doi: 10.1111/j.1600-0773.1981.tb00897.x.
2
The urinary excretion of frusemide and its metabolites by kidney transplant patients.肾移植患者对速尿及其代谢产物的尿排泄情况。
Eur J Clin Pharmacol. 1987;32(3):313-5. doi: 10.1007/BF00607581.
3
Biotransformation of furosemide in kidney transplant patients.呋塞米在肾移植患者中的生物转化。
Eur J Clin Pharmacol. 1983;24(6):787-90. doi: 10.1007/BF00607088.
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Biotransformation of furosemide in patients with acute pulmonary edema.速尿在急性肺水肿患者中的生物转化
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Absorption and disposition of furosemide in healthy volunteers, measured with a metabolite-specific assay.
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6
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Microbial models of mammalian metabolism. N-dealkylation of furosemide to yield the mammalian metabolite CSA using Cunninghamella elegans.哺乳动物代谢的微生物模型。使用雅致小克银汉霉将速尿进行N-脱烷基化反应以生成哺乳动物代谢物CSA。
Drug Metab Dispos. 1992 Nov-Dec;20(6):882-8.
8
Thin-layer chromatographic determination of furosemide and 4-chloro-5-sulfamoyl anthranilic acid in plasma and urine.血浆和尿液中呋塞米及4-氯-5-氨磺酰基邻氨基苯甲酸的薄层色谱测定法
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Determination of furosemide in urine samples by direct injection in a micellar liquid chromatographic system.
Analyst. 2002 Jan;127(1):29-34. doi: 10.1039/b108358a.
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On the fate of furosemide in man.关于速尿在人体中的代谢情况。
Eur J Clin Pharmacol. 1975 Oct 10;9(1):51-61. doi: 10.1007/BF00613429.

引用本文的文献

1
In vitro studies on the hydrolysis of frusemide in gastrointestinal juices.速尿在胃肠液中水解的体外研究。
Br J Clin Pharmacol. 1982 Aug;14(2):306-9. doi: 10.1111/j.1365-2125.1982.tb01984.x.
2
Antihypertensive effect of diazoxide given intravenously in small repeated doses.小剂量重复静脉注射二氮嗪的降压作用。
Eur J Clin Pharmacol. 1983;24(2):151-6. doi: 10.1007/BF00613809.
3
The influence of age on renal and extrarenal effects of frusemide.年龄对速尿肾脏及肾外效应的影响。
Br J Clin Pharmacol. 1984 Jul;18(1):65-74. doi: 10.1111/j.1365-2125.1984.tb05023.x.
4
Pharmacokinetics of furosemide in man after intravenous and oral administration. Application of moment analysis.呋塞米静脉注射和口服给药后在人体内的药代动力学。矩量法的应用。
Eur J Clin Pharmacol. 1984;26(2):197-207. doi: 10.1007/BF00630286.
5
The pharmacokinetics of frusemide are influenced by age.速尿的药代动力学受年龄影响。
Br J Clin Pharmacol. 1983 Oct;16(4):391-7. doi: 10.1111/j.1365-2125.1983.tb02183.x.
6
Biotransformation of furosemide in kidney transplant patients.呋塞米在肾移植患者中的生物转化。
Eur J Clin Pharmacol. 1983;24(6):787-90. doi: 10.1007/BF00607088.
7
The urinary excretion of frusemide and its metabolites by kidney transplant patients.肾移植患者对速尿及其代谢产物的尿排泄情况。
Eur J Clin Pharmacol. 1987;32(3):313-5. doi: 10.1007/BF00607581.
8
Urinary excretion of frusemide and its metabolites in a diabetic nephropathy patient.速尿及其代谢产物在一名糖尿病肾病患者中的尿排泄情况。
Eur J Clin Pharmacol. 1988;35(1):113. doi: 10.1007/BF00555520.
9
Interaction between furosemide and the converting enzyme inhibitor benazepril in healthy volunteers.
Eur J Clin Pharmacol. 1988;34(5):465-8. doi: 10.1007/BF01046703.
10
Absence of a pharmacokinetic interaction between enalapril and frusemide.依那普利与速尿之间不存在药代动力学相互作用。
Br J Clin Pharmacol. 1987 Jan;23(1):84-7. doi: 10.1111/j.1365-2125.1987.tb03013.x.