Fenner H
Fortschr Med. 1982 Sep 23;100(36):1642-6.
For NSAID's the clinical evidence of their efficacy is evaluated empirically employing tedious procedures. For diclofenac, indometacin and piroxicam proposals for a more rational procedure of their dose-response relationship determination are discussed. Preclinical data regarding the prostaglandin inhibition are correlated with pharmacokinetic parameters of target-tissue concentrations. In the range of inhibitory drug concentrations in the synovial fluid an antiinflammatory and analgesic effect can be established clinically. Studies on transsynovial kinetics of NSAID's therefore should supply appropriate evidence for an approach to their therapeutic regimen in clinical dose finding studies.
对于非甾体抗炎药(NSAID),其疗效的临床证据是通过采用繁琐的程序进行经验性评估的。对于双氯芬酸、吲哚美辛和吡罗昔康,讨论了一种更合理的确定其剂量反应关系的程序建议。关于前列腺素抑制的临床前数据与靶组织浓度的药代动力学参数相关。在滑液中抑制性药物浓度范围内,临床上可确立抗炎和镇痛作用。因此,关于NSAID经滑膜动力学的研究应为临床剂量探索研究中确定其治疗方案提供适当的证据。