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血液透析对布洛芬及其主要代谢产物药代动力学的影响。

The influence of hemodialysis on the pharmacokinetics of ibuprofen and its major metabolites.

作者信息

Antal E J, Wright C E, Brown B L, Albert K S, Aman L C, Levin N W

出版信息

J Clin Pharmacol. 1986 Mar;26(3):184-90. doi: 10.1002/j.1552-4604.1986.tb02931.x.

DOI:10.1002/j.1552-4604.1986.tb02931.x
PMID:3958223
Abstract

The pharmacokinetics of ibuprofen and its two major metabolites, the hydroxy and carboxy derivatives, were studied in seven functionally anephric subjects undergoing hemodialysis therapy. Subjects received ibuprofen 800 mg tid for 14 days. Hemodialysis was performed three times weekly during this period. Arterial and venous blood samples were collected before dialysis and along with dialysate, and during the final dosing interval and dialysis session. No accumulation of ibuprofen plasma concentrations and an absence of intact ibuprofen in dialysate indicated clearance through metabolic pathways. The metabolites did accumulate significantly (mean plasma levels, carboxy 249 micrograms/mL and hydroxy 57 mu/mL); however, both were detected in dialysate. Mean extraction efficiencies were 0.16 (hydroxy) and 0.15 (carboxy). Dialysis clearance calculated by arterial-venous difference was found to agree with actual recovery in dialysate for both metabolites. Side effects were not observed in any subject.

摘要

对7名接受血液透析治疗的功能性无肾受试者,研究了布洛芬及其两种主要代谢物(羟基和羧基衍生物)的药代动力学。受试者每日3次服用800毫克布洛芬,共14天。在此期间,每周进行3次血液透析。在透析前、与透析液一起以及在最后给药间隔和透析期间采集动脉和静脉血样。布洛芬血浆浓度无蓄积且透析液中无完整的布洛芬,表明通过代谢途径清除。代谢物确实有显著蓄积(平均血浆水平,羧基为249微克/毫升,羟基为57微克/毫升);然而,两者均在透析液中被检测到。平均提取效率分别为0.16(羟基)和0.15(羧基)。通过动静脉差值计算的透析清除率与两种代谢物在透析液中的实际回收率一致。未在任何受试者中观察到副作用。

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