Bradley J D, Rudy A C, Katz B P, Ryan S I, Kalasinski L A, Brater D C, Hall S D, Brandt K D
Department of Medicine, Indiana University School of Medicine, Indianapolis 46202-5103.
J Rheumatol. 1992 Jan;19(1):130-4.
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.
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。