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速尿缓释制剂在人体中的药效学和药代动力学研究。

Pharmacodynamic and pharmacokinetic study of a slow-release formulation of furosemide in man.

作者信息

Ebihara A, Tawara K, Oka T

出版信息

Arzneimittelforschung. 1983;33(1):163-6.

PMID:6681970
Abstract

A slow-release formulation of 40 mg furosemide as capsules (Eutensin) was investigated for its pharmacokinetic and pharmacodynamic properties in comparison with conventional tablets containing 40 mg furosemide (Lasix) in a single-blind clinical pharmacological trial in 6 healthy subjects. The following results were obtained: 1. The AUC0-24 after the administration of slow-release (SR) furosemide was about 42% of that after furosemide tablets. 2. Urine volume and urinary excretion of Na and Cl were significantly greater after furosemide tablets than after SR furosemide during the first 10 h after administration. No significant difference was observed between the two formulations in the urinary excretion of K, creatinine and uric acid. No significant difference was noted in every tested pharmacodynamic parameter during the cumulative 24 h after administration. It was concluded that SR furosemide may be used in the treatment of hypertension due to its characteristics of a slow-release diuretic feature, delayed peak blood concentration, delayed maximum diuretic effect and prolonged duration of action.

摘要

在一项针对6名健康受试者的单盲临床药理学试验中,研究了40毫克速尿的缓释胶囊制剂(优特喜)与含40毫克速尿的常规片剂(速尿)相比的药代动力学和药效学特性。获得了以下结果:1. 服用缓释速尿后的AUC0-24约为服用速尿片剂后的42%。2. 服用后前10小时内,速尿片剂后的尿量以及钠和氯的尿排泄量显著高于缓释速尿后的。两种制剂在钾、肌酐和尿酸的尿排泄方面未观察到显著差异。给药后累计24小时内,各项测试的药效学参数均未发现显著差异。得出的结论是,缓释速尿因其具有缓释利尿特性、血药浓度峰值延迟、最大利尿作用延迟和作用持续时间延长等特点,可用于治疗高血压。

相似文献

1
Pharmacodynamic and pharmacokinetic study of a slow-release formulation of furosemide in man.速尿缓释制剂在人体中的药效学和药代动力学研究。
Arzneimittelforschung. 1983;33(1):163-6.
2
Clinical investigations on the pharmacology of azosemide (SK-110) in comparison with furosemide in healthy volunteers.与速尿相比,阿佐塞米(SK-110)在健康志愿者中的药理学临床研究。
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A comparative study of the diuretic, natriuretic, and kaluretic effects of furosemide when administered at 07:00 h and at 19:00 h.呋塞米分别于7:00和19:00给药时利尿、利钠和排钾作用的比较研究。
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[Clinical and pharmacokinetic comparison of 2 oral preparations of nifedipine: 10 mg capsules and 20 mg delayed-release tablets].硝苯地平两种口服制剂的临床及药代动力学比较:10毫克胶囊与20毫克缓释片
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Diuretic effect and duration of action of a single intravenous dose of furosemide in uremia and myocardial infarction.单次静脉注射速尿在尿毒症和心肌梗死中的利尿作用及作用持续时间。
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引用本文的文献

1
Influence of drug formulation on drug concentration-effect relationships.药物制剂对药物浓度-效应关系的影响。
Clin Pharmacokinet. 1994 Feb;26(2):135-43. doi: 10.2165/00003088-199426020-00006.
2
Pharmacokinetic and pharmacodynamic study of the combination of furosemide retard and triamterene.
Eur J Clin Pharmacol. 1984;26(2):191-5. doi: 10.1007/BF00630285.
3
Bioavailability and elimination kinetics of the combination furosemide-retard/triamterene.
Eur J Drug Metab Pharmacokinet. 1985 Apr-Jun;10(2):127-32. doi: 10.1007/BF03189706.
4
Bioavailability and diuretic effect of furosemide during long-term treatment of chronic respiratory failure.
Eur J Clin Pharmacol. 1985;28(1):53-9. doi: 10.1007/BF00635708.
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Effects of the rate and composition of fluid replacement on the pharmacokinetics and pharmacodynamics of intravenous furosemide.补液速率和成分对静脉注射呋塞米的药代动力学和药效学的影响。
J Pharmacokinet Biopharm. 1986 Oct;14(5):495-509. doi: 10.1007/BF01059657.
6
Furosemide pharmacokinetics and pharmacodynamics in health and disease--an update.呋塞米在健康与疾病状态下的药代动力学和药效学——最新进展
J Pharmacokinet Biopharm. 1989 Feb;17(1):1-46. doi: 10.1007/BF01059086.
7
Furosemide (frusemide). A pharmacokinetic/pharmacodynamic review (Part II).呋塞米。药代动力学/药效学综述(第二部分)。
Clin Pharmacokinet. 1990 Jun;18(6):460-71. doi: 10.2165/00003088-199018060-00003.