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健康志愿者中二氢麦角碱的生物利用度。

Bioavailability of dihydroergosine in healthy volunteers.

作者信息

Cvelbar P, Culig J, Kopitar Z, Lenardic A, Smerkolj J U, Zorz M

出版信息

Eur J Drug Metab Pharmacokinet. 1987 Jan-Mar;12(1):1-4. doi: 10.1007/BF03189854.

DOI:10.1007/BF03189854
PMID:3609067
Abstract

Eight healthy volunteers received an oral dose of 10 mg and an intravenous dose of 0.75 mg of dihydroergosine. Plasma concentrations were measured by HPLC method, and some pharmacokinetic parameters were calculated. The biologic half-life in the elimination phase was 8.35 +/- 1.87 h after oral administration and 8.84 +/- 3.64 h after intravenous administration. In both cases of administration a secondary rise in plasma concentration of dihydroergosine was observed, which can be attributed to hepatic recycling. The calculated bioavailability of the drug was 9.80 +/- 2.8%.

摘要

八名健康志愿者口服了10毫克双氢麦角碱,并静脉注射了0.75毫克双氢麦角碱。采用高效液相色谱法测定血浆浓度,并计算了一些药代动力学参数。口服给药后消除相的生物半衰期为8.35±1.87小时,静脉给药后为8.84±3.64小时。在两种给药情况下均观察到双氢麦角碱血浆浓度的二次升高,这可归因于肝肠循环。该药物计算得出的生物利用度为9.80±2.8%。

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Bioavailability of dihydroergosine in healthy volunteers.健康志愿者中二氢麦角碱的生物利用度。
Eur J Drug Metab Pharmacokinet. 1987 Jan-Mar;12(1):1-4. doi: 10.1007/BF03189854.
2
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本文引用的文献

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Dihydroergotoxine kinetics in healthy men after intravenous and oral administration.
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Bioavailability of dihydroergotamine in man.双氢麦角胺在人体中的生物利用度。
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Pharmacokinetics of dihydroergosine in rats after intravenous and oral administration.大鼠静脉注射和口服二氢麦角碱后的药代动力学
Eur J Drug Metab Pharmacokinet. 1983;8(1):17-20. doi: 10.1007/BF03189576.
4
Low oral bioavailability of dihydroergotamine and first-pass extraction in patients with orthostatic hypotension.二氢麦角胺口服生物利用度低及体位性低血压患者的首过效应
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Plasma kinetics of dihydroergotoxin in rat by using a radioreceptor assay.采用放射受体分析法研究大鼠体内二氢麦角毒素的血浆动力学。
Pharmacol Res Commun. 1984 May;16(5):437-46. doi: 10.1016/s0031-6989(84)80011-9.
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Hemodynamic effects of two ergot derivatives in the conscious spontaneously hypertensive rat.
Pharmacology. 1984;29(4):215-23. doi: 10.1159/000138016.
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First-pass elimination. Basic concepts and clinical consequences.首过消除。基本概念及临床后果。
Clin Pharmacokinet. 1984 Jan-Feb;9(1):1-25. doi: 10.2165/00003088-198409010-00001.
8
Clinical pharmacokinetics of ergotamine, dihydroergotamine, ergotoxine, bromocriptine, methysergide, and lergotrile.麦角胺、双氢麦角胺、麦角毒碱、溴隐亭、甲基麦角新碱和麦角腈的临床药代动力学。
Int J Clin Pharmacol Ther Toxicol. 1983 Mar;21(3):135-42.