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首页> 外文期刊>European journal of pharmaceutical sciences >Pharmacodynamic behaviour of the selective cyclooxygenase-2 inhibitor lumiracoxib in the lipopolysaccharide-stimulated rat air pouch model.
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Pharmacodynamic behaviour of the selective cyclooxygenase-2 inhibitor lumiracoxib in the lipopolysaccharide-stimulated rat air pouch model.

机译：选择性环氧合酶2抑制剂lumiracoxib在脂多糖刺激的大鼠气袋模型中的药效动力学行为。

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摘要

PURPOSE: To investigate the pharmacodynamic behaviour of the selective cyclooxygenase-2 inhibitor, lumiracoxib, in the rat air pouch. METHODS: Air pouches were injected with lipopolysaccharide to stimulate prostaglandin E2 (PGE2) production 1h after lumiracoxib treatment. Pouch fluid samples were collected 6 or 24 h after lumiracoxib administration to measure PGE2 levels. Lumiracoxib concentrations in pouch fluid and plasma were measured by mass spectrometry. RESULTS: Oral administration of lumiracoxib resulted in dose-dependent inhibition of PGE2 production 6 and 24 h post-dose. The estimated ED50 values for inhibition of PGE2 production were 0.1 and 2.0 mg/kg at 6 and 24 h, respectively. Lumiracoxib concentrations in plasma and pouch fluid increased in proportion to dose. There was a strong positive correlation between lumiracoxib concentrations in plasma and pouch fluid compartments. Lumiracoxib concentrations were higher in plasma than in pouch fluid 6 h post-dose, but at 24 h post-dose, pouch fluid concentrations were > or =4-fold greater than plasma concentrations. CONCLUSIONS: Lumiracoxib readily enters the air pouch and persists in this extravascular compartment for a longer period of time than in plasma. This distribution profile may contribute to the ability of lumiracoxib to inhibit PGE2 production up to 24 h after dosing.
机译：目的：研究选择性环氧合酶-2抑制剂路美昔布在大鼠气囊中的药效学行为。方法：在空气囊中注射脂多糖以刺激lumiracoxib治疗1h后产生前列腺素E2（PGE2）。施用卢美昔布后6或24 h收集囊液样品以测量PGE2水平。通过质谱法测量囊液和血浆中Lumiracoxib的浓度。结果：口服卢美昔布导致剂量后6和24小时PGE 2产生的剂量依赖性抑制。抑制PGE2产生的ED50估计值在6小时和24小时分别为0.1和2.0 mg / kg。血浆和囊液中Lumiracoxib的浓度与剂量成正比。血浆和袋装液室中的lumiracoxib浓度之间存在很强的正相关。给药后6小时血浆中Lumiracoxib的浓度高于囊液中的浓度，但是在给药后24小时，囊液中的浓度比血浆浓度高>或= 4倍。结论：Lumiracoxib容易进入气囊并在血管外腔室中停留的时间比血浆中更长。该分布曲线可有助于鲁米昔布在给药后24小时内抑制PGE 2产生的能力。

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