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一项关于新型非甾体抗炎药(屈昔康)与吡罗昔康在健康志愿者单次及多次给药后生物利用度的交叉研究。

Cross-over study of the bioavailability of a new NSAID (droxicam) versus piroxicam in healthy volunteers following single and multiple dose administration.

作者信息

Bartlett A, Costa A, Martinez L, Roser R, Sagarra R, Sanchez J

机构信息

Research Centre, Laboratorios Dr Esteve SA, Barcelona, Spain.

出版信息

Eur J Drug Metab Pharmacokinet. 1992 Jul-Sep;17(3):195-9. doi: 10.1007/BF03190145.

DOI:10.1007/BF03190145
PMID:1490488
Abstract

Droxicam is a new anti-inflammatory drug which is a pro-drug of piroxicam and possesses delayed absorption kinetics. In this study, the comparative bioavailability of the two compounds was investigated. The study was performed following a cross-over design with single (20 mg) and multiple (20 mg/day for 30 consecutive days) administration in 25 healthy volunteers. The peak plasma concentrations of piroxicam, obtained following administration of droxicam, were lower than those calculated for administration of piroxicam, and the time taken to reach these peak concentrations was increased by approximately 5-7 h. There was no significant difference in either the elimination kinetics of piroxicam or the AUC values found following administration of the two products. Bioavailability of droxicam is equal to that of piroxicam, with a slower rate of absorption.

摘要

屈昔康是一种新型抗炎药物,它是吡罗昔康的前体药物,具有延迟吸收动力学。在本研究中,对这两种化合物的相对生物利用度进行了研究。该研究采用交叉设计,在25名健康志愿者中进行单次(20毫克)和多次(连续30天每天20毫克)给药。服用屈昔康后测得的吡罗昔康血浆峰浓度低于服用吡罗昔康时计算得出的浓度,达到这些峰浓度所需的时间增加了约5 - 7小时。两种产品给药后吡罗昔康的消除动力学或AUC值均无显著差异。屈昔康的生物利用度与吡罗昔康相等,但吸收速率较慢。

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1
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本文引用的文献

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Analysis of piroxicam in plasma by high-performance liquid chromatography.采用高效液相色谱法分析血浆中的吡罗昔康。
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Pharmacokinetics of droxicam in rat and dog.屈昔康在大鼠和犬体内的药代动力学。
Methods Find Exp Clin Pharmacol. 1986 Jul;8(7):423-9.
5
Comparative light and electron microscopic observations of the lesive effects of two non-steroid anti-inflammatory drugs plus stress on rat gastric mucosa.两种非甾体抗炎药加应激对大鼠胃黏膜损伤作用的光镜和电镜比较观察
Methods Find Exp Clin Pharmacol. 1987 Jun;9(6):353-70.
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Pharmacological properties of droxicam, a new non-steroidal anti-inflammatory agent.新型非甾体抗炎药屈昔康的药理特性
Methods Find Exp Clin Pharmacol. 1986 Jul;8(7):407-22.
7
Pharmacological profile of droxicam.屈昔康的药理特性
Gen Pharmacol. 1988;19(1):49-54. doi: 10.1016/0306-3623(88)90004-3.
8
Comparative study of the multiple dose pharmacokinetics and the tolerance of a new NSAID (droxicam) versus piroxicam in healthy volunteers.新型非甾体抗炎药(屈昔康)与吡罗昔康在健康志愿者中多次给药的药代动力学及耐受性的对比研究。
Methods Find Exp Clin Pharmacol. 1988 Nov;10(11):729-37.
9
Effects of droxicam on in vivo prostaglandin synthesis and ex vivo platelet aggregation.屈昔康对体内前列腺素合成及体外血小板聚集的影响。
Methods Find Exp Clin Pharmacol. 1987 Apr;9(4):209-13.
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The influence of gastric emptying on droxicam pharmacokinetics.
J Clin Pharmacol. 1989 Aug;29(8):739-45. doi: 10.1002/j.1552-4604.1989.tb03409.x.