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[摘要]
目的 評價阿立哌唑注射液的肌肉刺激性,觀察其否具有溶血、凝聚及過敏反應。方法 采用兔股四頭肌sc給藥,觀察阿立哌唑注射液對注射局部肌肉的刺激性;采用2%兔血紅細胞混懸液檢查阿立哌唑注射液有無溶血和紅細胞凝聚反應;采用豚鼠全身主動過敏試驗(ASA)評價阿立哌唑注射液有無過敏反應。結果 阿立哌唑注射液對兔紅細胞無溶血及凝聚作用;新西蘭兔單次及連續(xù)7 d sc給予阿立哌唑注射液,均發(fā)現(xiàn)其對股四頭肌有刺激作用,以肌纖維的變性壞死為主,肌纖維崩解消失,病灶內可見散在的炎細胞浸潤,停藥14 d后刺激反應消失;每只3.75、7.50 mg劑量下給予阿立哌唑注射液,豚鼠未見過敏反應。結論 阿立哌唑注射液未見溶血和過敏反應,較高濃度下可能會引起肌肉刺激性反應。
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[Abstract]
Objective To evaluate the muscular irritation, hemolysis and sensitization of Aripiprazole Injection. Methods The local muscle irritation of Aripiprazole Injection was observed through sc injection on quadriceps femoris in rabbits. The 2% red blood cell suspension in the blood of rabbit was used to check whether Aripiprazole Injection could cause the reaction of emolysis and erythrocyte agglutination. The method of systemic active allergic test (ASA) was used to evaluate the effect of Aripiprazole Injection on allergic reaction in Guinea pigs. Results No evidence of hemolyzation and aggregation on rabbit erythrocyte in vitro was observed after Aripiprazole Injection treatment. Test substance was sc injected by single or multiple doses for 7 d, both of them had muscular irritation on New Zealand rabbits, the major pathologic change was the degeneration and necrosis of myofibers, myofibers broke apart and disappeared, lots of inflammatory cells immersed. After drug withdrawal, muscular irritation was recovered. No allergic reactions on Guinea pigs in vivo were observed at the low dose of 3.75 mg and the high dose of 7.5 mg. Conclusion Aripiprazole Injection has no hemolyzation and sensitization, but may cause muscle irritation at higher concentration.
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