阿立哌唑注射液肌肉刺激、溶血及过敏试验研究

Experimental study of Aripiprazole Injection on muscular irritation, hemolysis and sensitization

目的评价阿立哌唑注射液的肌肉刺激性,观察其否具有溶血、凝聚及过敏反应。方法采用兔股四头肌sc给药,观察阿立哌唑注射液对注射局部肌肉的刺激性;采用2%兔血红细胞混悬液检查阿立哌唑注射液有无溶血和红细胞凝聚反应;采用豚鼠全身主动过敏试验(ASA)评价阿立哌唑注射液有无过敏反应。结果阿立哌唑注射液对兔红细胞无溶血及凝聚作用;新西兰兔单次及连续7 d sc给予阿立哌唑注射液,均发现其对股四头肌有刺激作用,以肌纤维的变性坏死为主,肌纤维崩解消失,病灶内可见散在的炎细胞浸润,停药14 d后刺激反应消失;每只3.75、7.50 mg剂量下给予阿立哌唑注射液,豚鼠未见过敏反应。结论阿立哌唑注射液未见溶血和过敏反应,较高浓度下可能会引起肌肉刺激性反应。

Objective To evaluate the muscular irritation, hemolysis and sensitization of Aripiprazole Injection. Methods Thelocal muscle irritation of Aripiprazole Injection was observed through sc injection on quadriceps femoris in rabbits. The 2% redblood cell suspension in the blood of rabbit was used to check whether Aripiprazole Injection could cause the reaction of emolysisand erythrocyte agglutination. The method of systemic active allergic test （ASA） was used to evaluate the effect of AripiprazoleInjection on allergic reaction in Guinea pigs. Results No evidence of hemolyzation and aggregation on rabbit erythrocyte in vitrowas observed after Aripiprazole Injection treatment. Test substance was sc injected by single or multiple doses for 7 d, both of themhad 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 wasrecovered. 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.