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布洛芬立体异构体血清浓度与髋膝关节骨关节炎治疗中临床反应的相关性。

Correlation of serum concentrations of ibuprofen stereoisomers with clinical response in the treatment of hip and knee osteoarthritis.

作者信息

Bradley J D, Rudy A C, Katz B P, Ryan S I, Kalasinski L A, Brater D C, Hall S D, Brandt K D

机构信息

Department of Medicine, Indiana University School of Medicine, Indianapolis 46202-5103.

出版信息

J Rheumatol. 1992 Jan;19(1):130-4.

PMID:1556674
Abstract

Stereoselective pharmacokinetic measurements of the active enantiomer, S-ibuprofen, were correlated with clinical response in 45 participants in a randomized double blinded 4 week comparison of ibuprofen, 1200 or 2400 mg/day, for treatment of hip or knee osteoarthritis. Ibuprofen dose correlated with S-ibuprofen area under the serum concentration curve (AUC), trough and average concentration, but not with clinical outcome. AUC of S-ibuprofen correlated with improvement in disability, rest pain and in the physician's global assessment (p = 0.02, 0.08, and 0.10, respectively), and negatively with the subject's weight and creatinine clearance (p = 0.09 and 0.07, respectively). Some individual variation in responsiveness to ibuprofen (and other nonsteroidal antiinflammatory drugs) may be attributed to pharmacokinetic differences.

摘要

在一项为期4周的随机双盲试验中,对45名髋部或膝部骨关节炎患者进行了布洛芬(1200或2400毫克/天)治疗,同时对活性对映体S-布洛芬进行了立体选择性药代动力学测量,并将其与临床反应进行了关联分析。布洛芬剂量与S-布洛芬的血清浓度曲线下面积(AUC)、谷浓度和平均浓度相关,但与临床结果无关。S-布洛芬的AUC与残疾改善、静息痛改善以及医生的整体评估相关(分别为p = 0.02、0.08和0.10),与受试者体重和肌酐清除率呈负相关(分别为p = 0.09和0.07)。对布洛芬(和其他非甾体抗炎药)反应的个体差异可能归因于药代动力学差异。

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