Nakamura H, Motoyoshi S, Imazu C, Ishii K, Yokoyama Y, Seto Y, Kadokawa T, Shimizu M
Nihon Yakurigaku Zasshi. 1982 Aug;80(2):125-35.
Anti-inflammatory, analgesic, and anti-pyretic activities of orally administered etofenamate, the diethylene glycol ester of flufenamic acid, were investigated in experimental animals. Against acetic acid-induced vascular permeability in mice and ultra-violet light-induced erythema in guinea pigs, etofenamate produced a dose related inhibition at doses of 40--320 mg/kg and 5--20 mg/kg, respectively. In rats, felt-pellet-induced granuloma formation and adjuvant-induced arthritis were significantly inhibited by repeated administration of etofenamate at doses of 20 mg/kg/day for 5 days and 40 mg/kg/day for 21 days, respectively. Etofenamate showed an inhibitory activity on the squeak response caused by flexing and extending the silver nitrate-induced arthritic joint in rats; and it produced a dose related anti-writhing activity at doses of 50--300 mg/kg and 10--80 mg/kg in mice and rats, respectively, in the acetic acid-induced writhing test. Etofenamate showed a significant anti-pyretic activity at doses of 0.2 mg/kg or more. These potencies of etofenamate were 0.5 to 1.6 times those of flufenamic acid. In particular, the anti-erythema, anti-arthritis, and anti-pyretic activities of etofenamate were approximately equivalent to or superior to those of flufenamic acid. From these results, it was suggested that etofenamate given orally, like other non-steroidal anti-inflammatory drugs, showed anti-inflammatory, analgesic, and anti-pyretic activities in experimental animals.
研究了口服依托芬那酯(氟芬那酸二甘醇酯)在实验动物中的抗炎、镇痛和解热活性。在小鼠醋酸诱导的血管通透性实验以及豚鼠紫外线诱导的红斑实验中,依托芬那酯在40 - 320mg/kg和5 - 20mg/kg剂量下分别产生了剂量相关的抑制作用。在大鼠中,分别以20mg/kg/天的剂量连续给药5天和40mg/kg/天的剂量连续给药21天,依托芬那酯对棉球诱导的肉芽肿形成和佐剂诱导的关节炎有显著抑制作用。依托芬那酯对大鼠硝酸银诱导的关节炎关节屈伸引起的吱吱声反应有抑制活性;在醋酸诱导的扭体实验中,依托芬那酯在小鼠和大鼠中的剂量分别为50 - 300mg/kg和10 - 80mg/kg时产生剂量相关的抗扭体活性。依托芬那酯在0.2mg/kg及以上剂量时表现出显著的解热活性。依托芬那酯的这些效力是氟芬那酸的0.5至1.6倍。特别是,依托芬那酯的抗红斑、抗关节炎和解热活性与氟芬那酸大致相当或优于氟芬那酸。从这些结果表明,口服依托芬那酯与其他非甾体抗炎药一样,在实验动物中表现出抗炎、镇痛和解热活性。