西来昔布作为选择性COX-2抑制剂的药效学考察  

Pharmacodynamic Investigation of Xelecoxib as a Selective COX-2 Inhibitor

作　　者：安泳潼[1] 沈龙海[1] 

机构地区：[1]中国医药工业研究总院上海医药工业研究院,创新药物与制药工艺国家重点实验室,上海200437

出　　处：《中国医药工业杂志》2015年第11期1207-1212,共6页Chinese Journal of Pharmaceuticals

摘　　要：通过建立角叉菜胶诱发大鼠足肿胀模型、大鼠佐剂性关节炎模型和棉球致大鼠肉芽肿模型,以塞来昔布、吲哚美辛或布洛芬为阳性对照,考察选择性环氧合酶2抑制剂西来昔布的抗炎作用。同时,考察其抑制热刺激及化学刺激引起小鼠疼痛的作用及对小鼠产生白介素1（IL 1）的影响。结果表明,在1.25~10 mg/kg剂量范围内,西来昔布对上述模型大鼠均有明显的抗炎作用,对受试小鼠则均有明显的镇痛作用,同时抑制小鼠产生IL 1。并且在受试范围内,西来昔布的药效与剂量有一定的相关性。The anti-inflammatory effects of xelecoxib, a selective cyclooxygenase-2 （COX-2） inhibitor, were investigated through the rat models of paw edema induced by carrageenan, arthritis by adjuvant and granuloma by cotton- ball with celecoxib, indomethacin or ibuprofen as the positive controls. Meanwhile, its analgesic effects in mice were investigated by hot plate and acetic acid induced writhing tests and its impact on the production of interleukin 1 （IL-1） in mice was also measured. The results showed that xelecoxib exhibited a significant anti-inflammatory effect in all above rat models as well as a significant analgesic effect in both pain models in mice at dose range of 1.25 - 10 mg/kg. The production of IL- 1 in mice was also significantly inhibited by xelecoxib. Within the tested dose range, xelecoxib showed a certain dose-effect relationship.

关 键 词：西来昔布 药效 抗炎 镇痛 白介素1 

分 类 号：R96[医药卫生—药理学]