非ステロイド性抗炎症薬Bermoprofen (AD-1590)の代謝物の抗炎症, 鎮痛, 解熱及び胃潰瘍形成作用

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Anti-inflammatory, analgesic, antipyretic and gastrointestinal ulcerogenic activities of metabolites of bermoprofen (AD-1590), a new non-steroidal anti-inflammatory drug, were investigated in order to ascertain whether they have pharmacological activities in experimental animals. Among 3 metabolites of AD-1590,main metabolite, 11-hydroxyl form (AD-2406) was the most active in the carrageenan-induced hind paw edema in rats, and the others weak or almost inactive at a dose of 80mg/kg, i.v. Anti-edema, analgesic (mouse phenylquinone and rat acetic acid writhing tests) and antipyretic (LPS febrile rabbits) activities of intravenously administered AD-2406 were approximately one-hundredth that of AD-1590 (0.04-1 mg/kg, i.v.), but equivalent or superior to that of oral aspirin. On the other hand, AD-2406 did not produce significant gastric ulcer in fasted rats in lethal toxic dosages, and its acute lethal toxicity (LD_<50>=373mg/kg, i.v.) was about one-second that of oral AD-1590 in fed rats. These results suggest that AD-2406 and 2 other metabolites do not contribute the pharmacological activities produced by AD-1590.
公益社団法人日本薬学会の論文
1988-08-25