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老年关节炎患者中缓释噻洛芬酸的药代动力学

The pharmacokinetics of sustained release tiaprofenic acid in elderly arthritic patients.

作者信息

Hosie G A, Hosie J

出版信息

Br J Clin Pharmacol. 1987 Jul;24(1):93-5. doi: 10.1111/j.1365-2125.1987.tb03141.x.

Abstract

Tiaprofenic acid is a non-steroidal anti-inflammatory drug which is highly protein bound and excreted mainly by the kidneys. Previous pharmacokinetic studies with tiaprofenic acid in conventional formulations in elderly arthritic patients have shown no evidence of accumulation of this drug over periods of up to 12 weeks. A sustained release formulation of the drug was given to 14 elderly arthritic patients over 4 weeks and plasma profiles obtained at the beginning and end of treatment over a 24 h period. Area under the curve (AUC), maximum plasma concentration (Cmax) and plasma concentration at 24 h (C24) were calculated and elimination half life (t1/2) was estimated. AUCs to infinity at week 0 were compared with AUCs to infinity at week 4 as a measure of drug accumulation. No significant differences were found for any of these parameters between the beginning and end of treatment. The mean t1/2 for both weeks was approximately 4.4 h. There was no evidence of any accumulation.

摘要

噻洛芬酸是一种非甾体抗炎药,它与蛋白质高度结合,主要通过肾脏排泄。先前针对老年关节炎患者使用传统剂型的噻洛芬酸进行的药代动力学研究表明,在长达12周的时间内,没有证据表明该药物会蓄积。给14名老年关节炎患者服用该药物的缓释制剂,持续4周,并在治疗开始和结束时的24小时内获取血浆曲线。计算曲线下面积(AUC)、最大血浆浓度(Cmax)和24小时时的血浆浓度(C24),并估算消除半衰期(t1/2)。将第0周时的AUC直至无穷大与第4周时的AUC直至无穷大进行比较,以此作为药物蓄积的指标。治疗开始和结束时,这些参数均未发现显著差异。两周的平均t1/2约为4.4小时。没有任何蓄积的证据。

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Clinical pharmacokinetics of tiaprofenic acid and its enantiomers.噻洛芬酸及其对映体的临床药代动力学
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