【摘要】 <正>萘普生(Naproxen)是芳基乙酸类消炎镇痛药。Harrison等曾指出它具有抗炎作用,Roszkowski在动物实验中证明萘普生具有高效的消炎止痛退热作用。Dorfman在该药国际专题讨论会上作了该药动物实验的综述。在临床试用结果亦证明该药对类风湿关节炎、骨关节炎和非关节性风湿病、痛风和一些疼痛具有良好的作用。由于该药疗效好,副作用小,英国已收载于1978年药典。国内广州第八制药厂已合成成功试产。本文主要是就该厂提供的萘普生[d-2-(6’-甲氧基-2’-萘基)丙酸)进行镇痛、消炎、退热等药理研究。更多还原

【Abstract】 Naproxen, d-2- (6’ me thoxy-2’ -naphthy1) propionic acid, is a nonste-roidal anti-inflammatory drug that has been shown in the literature to possess good anti-inflammatory, analgesic and antipyretic effects, after oral administration. This paper reports on the results of the study of the pharmacological activity of naproxen produced by the Eighth Guangzhou Pharmaceutical Factory.In the mouse. tartar emetic provoked writhing model, naproxen was shown to be more effective as an analgesic than aspirin, the relative potency of naproxen being 7,24 times higher then aspirin.In the rabbit vaccine-induced pyretic model, a single oral dose of 5 mg/kg of naproxen decreased the body temperature of the rabbit 1 hour later, and the antipyretic action was approximately the same as that of 100u mg/kg of aspirin.In the rat granuloma model, 20mg/kg of naproxen every day for seven days significantly inhibited the proliferation of granulomatous tissues induced by the implanted cotton pellet indicating the marked anti-inflammatory activity oi the drug.The actute 50% lethal dose ( LI ) of naproxen after a single oral administration was 1.66 ( 1.37-1.87 ) g/kg. Before death of the animals some signs of central nervous system irritability and convu1sions were encountered.The aforementioned data indicated that naproxen is a drug with a wide margin of safety. The therapeutic index, the ratio of LD50 ( 1660mg/kg ) to the analgesic ED50(9.72mg/kg), was calculated to be 165.更多还原