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利用单点干血斑评估口服氟比洛芬的代谢比。

Oral flurbiprofen metabolic ratio assessment using a single-point dried blood spot.

机构信息

Clinical Pharmacology and Toxicology, Geneva University Hospitals, Geneva, Switzerland.

出版信息

Clin Pharmacol Ther. 2012 Mar;91(3):489-96. doi: 10.1038/clpt.2011.247. Epub 2012 Jan 11.

Abstract

We investigated whether a single blood measurement using the minimally invasive technique of a finger prick to draw a blood sample of 5 µl (to yield a dried blood spot (DBS)) is suitable for the assessment of flurbiprofen (FLB) metabolic ratio (MR). Ten healthy volunteers who had been genotyped for CYP2C9 were recruited as subjects. They received FLB alone in session 1 and FLB with fluconazole in session 2. In session 3, the subjects were pretreated for 4 days with rifampicin and received FLB with the last dose of rifampicin on day 5. Plasma and DBS samples were obtained between 0 and 8 h after FLB administration, and urine was collected during the 8 h after administration. The pharmacokinetic profiles of the drugs were comparable in DBS and plasma. FLB's apparent clearance values decreased by 35% in plasma and DBS during session 2 and increased by 75% in plasma and by 30% in DBS during session 3. Good correlations were observed between MRs calculated from urine, plasma, and DBS samples.

摘要

我们研究了使用微创技术从手指刺取 5µl 的血样(产生干血斑(DBS))是否适合评估氟比洛芬(FLB)代谢比(MR)。我们招募了 10 名已对 CYP2C9 进行基因分型的健康志愿者作为研究对象。他们在第 1 次试验中单独接受 FLB,在第 2 次试验中接受 FLB 和氟康唑。在第 3 次试验中,志愿者连续 4 天用利福平预处理,并在第 5 天接受最后一剂利福平时接受 FLB。在 FLB 给药后 0 至 8 小时之间采集血浆和 DBS 样本,在给药后 8 小时内采集尿液。DBS 和血浆中的药物药代动力学特征相似。在第 2 次试验中,FLB 在血浆和 DBS 中的表观清除率分别下降了 35%,在第 3 次试验中,FLB 在血浆和 DBS 中的清除率分别增加了 75%和 30%。从尿液、血浆和 DBS 样本计算得出的 MR 之间存在良好的相关性。

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