阿替洛尔注射液对血管刺激、溶血和过敏的实验研究

目的 :观察阿替洛尔注射液血管刺激性和是否具有溶血、凝聚和过敏作用。方法 :兔耳缘静脉注射阿替洛尔 ,0 .2 5mg·kg- 1,qd× 3d ,停药 2 4h后做病理组织学检查 ,并与氯化钠注射液对照组比较 ;体外不同浓度的阿替洛尔注射液 0 .1～ 0 .5mL在 5mL兔红细胞氯化钠注射液中放置 0 .5～ 2 4h ,观察对兔红细胞悬液的溶血作用及有无红细胞凝聚作用 ;给豚鼠腹腔注射阿替洛尔 ,每只 0 .5mL ,qod× 3次 ,2wk和 3wk后分别再腹腔注射该药 ,每只2 .5mL- 1,然后观察 30min内是否出现过敏反应。结果 :阿替洛尔注射液对兔血管内皮没有损伤和刺激作用 ,与氯化钠注射液对照血管比较 ,两者无明显差异 ,对兔红细胞没有致溶血作用和凝聚作用 ,豚鼠未出现过敏反应。结论 :阿替洛尔注射液对用药血管没有刺激性反应 ,也无溶血及红细胞凝聚现象 ,对豚鼠无过敏反应。制剂有关安全性检测结果符合新药申报要求。

Experiment studies of atenolol injection on vascular stimulation, hemolysis, and sensitization

AIM: To observe whether atenolol injection has vascular stimulation, hemolyzation, agglutination, and sensitization. METHODS:The studies had been done according to the experimental methods of injection agents in pharmacodynamics guide principle on toxic test methods of application. The vascular stimulative assay of atenolol injection on rabbit at the dose of 0.25 mg·kg -1, qd for 3 d, the hemolyzation or agglutination of it in vitro, at the concentration of 0.1-0.5 mL for 0.5-24 h. The allergic reaction on guinea pig in vivo were performed. RESULTS:It was showed that the atenolol injection had no vascular irritation and injury effect on rabbit vascular endothelial cell. Compared with that of the sterile sodium chloride injection control group there was no difference. No evidences of hemolyzation and aggregation on rabbit erythrocyte in vitro, and no allergic reaction on guinea pig in vivo were observed. CONCLUSION:The test results of atenolol injection show there are no vascular stimulation on rabbit vascular endothelial cell and sensitization on guinea pig in vivo, and no hemolyzation or agglutination on rabbit red blood cells in vitro. These results of preparation safety will just fit the new drugs application reguirements.