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S-布洛芬与布洛芬消旋体对比:一项针对类风湿性关节炎患者的随机双盲研究

S-ibuprofen versus ibuprofen-racemate. A randomized double-blind study in patients with rheumatoid arthritis.

作者信息

Stock K P, Geisslinger G, Loew D, Beck W S, Bach G L, Brune K

机构信息

Klinik Herzoghoehe, Bayreuth, Federal Republic of Germany.

出版信息

Rheumatol Int. 1991;11(4-5):199-202. doi: 10.1007/BF00332562.

DOI:10.1007/BF00332562
PMID:1784888
Abstract

Ibuprofen (ibu) is a racemic 2-arylpropionic acid non-steroidal anti-inflammatory drug whose activity is due mainly to the S-enantiomer. So far only the racemic compound is in clinical use. A double-blind randomized trial was carried out for a 2-week period in 50 patients with classical rheumatoid arthritis (RA) (Steinbrocker II-III) to compare the effectiveness and tolerance of S-ibu (400 mg T.I.D.) with that of the racemic compound (600 mg T.I.D.). Ritchie-index, limitation of movement, joint pain on pressure and pain at night decreased significantly in both groups. Due to lack of effectiveness, the dose had to be increased in 3 patients from the S-ibu group as well as in 6 patients from the racemic group resulting in mean daily doses of 1220 mg S-ibuprofen and 1870 mg racemic ibu. No statistically significant difference could be found between both groups concerning efficacy and unwanted effects. Therefore, S-ibu given alone may be advantageous because the metabolic load to the human body is reduced and patients are more likely to comply with drug doses of 1.2 g/day as compared to 1.8 g/day.

摘要

布洛芬(ibu)是一种消旋的2-芳基丙酸非甾体抗炎药,其活性主要归因于S-对映体。到目前为止,只有消旋化合物在临床中使用。对50例经典类风湿性关节炎(RA)(斯坦布鲁克II - III级)患者进行了为期2周的双盲随机试验,以比较S-ibu(每日三次,每次400毫克)和消旋化合物(每日三次,每次600毫克)的有效性和耐受性。两组患者的里奇指数、活动受限、压痛和夜间疼痛均显著降低。由于疗效不佳,S-ibu组有3名患者以及消旋组有6名患者不得不增加剂量,导致S-布洛芬的平均每日剂量为1220毫克,消旋布洛芬为1870毫克。两组在疗效和不良反应方面均未发现统计学上的显著差异。因此,单独使用S-ibu可能具有优势,因为它降低了对人体的代谢负担,而且与每天1.8克相比,患者更有可能遵守1.2克/天的药物剂量。

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本文引用的文献

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Stereoselective disposition of ibuprofen enantiomers in man.布洛芬对映体在人体内的立体选择性分布。
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Eur J Clin Pharmacol. 1990;38(5):493-7. doi: 10.1007/BF02336690.
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Pharmacological differences between the optical isomers of ibuprofen: evidence for metabolic inversion of the (-)-isomer.布洛芬光学异构体之间的药理学差异:(-)-异构体代谢转化的证据。
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