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使用吡罗昔康新戊酸酯进行长期治疗期间血浆和滑液中吡罗昔康的浓度。

Plasma and synovial fluid concentrations of piroxicam during prolonged treatment with piroxicam pivalic ester.

作者信息

Chérié Lignière G, Montagnani G, Alberici M, Acerbi D

出版信息

Arzneimittelforschung. 1987 May;37(5):560-3.

PMID:3619977
Abstract

Piroxicam pivalic ester (CHF 10/21) is a prodrug of piroxicam and is characterized by a reduced gastric irritant activity. Plasma and synovial fluid samples were simultaneously taken from 7 patients with mono- or poly-articular arthritis causing knee effusion, during 4 weeks of treatment with CHF 10/21 at the dose of 30 mg/day. The time courses of plasma levels of both the prodrug and the active principle were studied and a correlation of the latter with synovial fluid levels was made. After 14 days of treatment the steady-state was reached in the systemic (plasma) and peripheral (synovial fluid) compartments with therapeutically active drug levels. Clinical results were good and a complete disappearance of local pain occurred in 2 cases. Good gastric tolerance was also achieved.

摘要

吡罗昔康特戊酸酯(CHF 10/21)是吡罗昔康的前体药物,其特点是胃刺激性活性降低。在7例因单关节或多关节关节炎导致膝关节积液的患者中,以30毫克/天的剂量用CHF 10/21治疗4周期间,同时采集血浆和滑液样本。研究了前体药物和活性成分的血浆水平随时间的变化过程,并将后者与滑液水平进行了相关性分析。治疗14天后,全身(血浆)和外周(滑液)腔室达到稳态,药物水平具有治疗活性。临床结果良好,2例局部疼痛完全消失。还实现了良好的胃耐受性。

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