论文部分内容阅读
目的:研究一类创新药苯胺洛芬的安全性药理,为新药研发提供依据。方法:通过小鼠自发活动试验、协调力实验和戊巴比妥钠催眠实验来考察苯胺洛芬对中枢神经系统的影响;通过麻醉Bealge犬实验考察苯胺洛芬对呼吸系统和循环系统的影响;通过正常大鼠和胃溃疡大鼠来考察苯胺洛芬对胃黏膜的影响。结果:苯胺洛芬剂量为临床拟用剂量的18倍时(小鼠216 mg.kg-1、大鼠162 mg.kg-1、犬45 mg.kg-1)单次给药后会导致麻醉Beagle犬血压一过性升高、小鼠自主活动降低、协调能力降低、与戊巴比妥钠具有协同作用;其余各剂量组和各观察指标均未见异常。结论:苯胺洛芬在剂量为临床拟用剂量的18倍时对中枢神经系统和心血管系统具有明显的影响;苯胺洛芬在剂量为临床拟用剂量的6倍时对中枢神经系统、呼吸系统和心血管系统未见明显影响;各剂量组对大鼠胃黏膜均未见明显影响。
Objective: To study the safety pharmacology of an innovative drug, aniline, to provide the basis for the development of new drugs. Methods: The spontaneous activity test in mice, coordination test and sodium pentobarbital hypnosis test were used to investigate the effect of aniline on central nervous system. The effects of aniline on respiratory and circulatory system were investigated by anesthesia in Bealge dogs. The effects of aniline on gastric mucosa were investigated by normal rats and gastric ulcer rats. RESULTS: The single dose of anamiloprofen at a dose of 18 times the clinical dose (216 mg.kg-1 for mice, 162 mg.kg-1 for rats and 45 mg.kg-1 for dogs) led to anesthesia Beagle dogs transiently elevated blood pressure, decreased autonomic activity in mice, reduced coordination, and pentobarbital sodium synergy; the rest of the dose group and the observed indicators were normal. Conclusion: Phenylalanine has a significant effect on the central nervous system and cardiovascular system at a dose 18 times as much as the clinical dose. Anamorphine exerts a significant effect on the central nervous system, respiratory system And cardiovascular system no significant effect; each dose group had no significant effect on gastric mucosa.