2-(α-羟基戊基)苯甲酸钾冻干粉注射液的血管及肌肉刺激、溶血、过敏试验研究  

Experiment Study on Potassium 2-(alpha-Hydroxypentyl) Benzoate Lyophilized Powder for Injection on Vascular and Muscular Stimulation,Hemolysis and Sensitization

作　　者：李江[1] 丁晓霜[1,2] 王晓良[1] 徐少锋[1] 王爱平[1,2] 靳洪涛[1,2] 

机构地区：[1]中国医学科学院药物研究所,北京100050 [2]中国医学科学院.北京协和医学院新药安全评价研究中心,北京100050

出　　处：《中国药业》2012年第18期22-23,共2页China Pharmaceuticals

基　　金：国家"十一五"重大新药创制专项;项目编号:2009ZX0912-038;2008ZX09305-001;基本科研业务费专项;项目编号:2006QN37

摘　　要：目的观察Ⅰ类抗脑缺血候选药物2-(α-羟基戊基)苯甲酸钾(dl-PHPB)冻干粉注射液的血管、肌肉刺激性和是否具有溶血、凝聚及过敏作用。方法Beagle犬静脉滴注dl-PHPB 1.2,3.6,10.8 g/L及氯化钠注射液对照组,给药30 d,每天1次,停药后观察3周;家兔耳缘静脉及股四头肌注射dl-PHPB 1 mg/kg和2 mg/kg,给药7 d,每天1次,停药后观察2周;进行病理检查。不同浓度的dl-PHPB在5 mL兔红细胞氯化钠注射液中放置4 h,观察溶血及凝聚作用。豚鼠静脉注射dl-PHPB 3,30 mg/k g,隔日1次,共5次,末次致敏后14 d激发1次,激发剂量为致敏剂量的3倍,观察其过敏反应。结果dl-PHPB冻干粉注射液在兔及beagle犬的血管内皮及兔肌肉组织未见明显的损伤和刺激作用;对兔红细胞没有致溶血和凝聚作用,豚鼠未出现过敏反应。结论dl-PHPB冻干粉注射液对用药血管、肌肉无刺激性反应,无红细胞溶血、凝聚现象及过敏反应。上述研究结果为dl-PHPB的临床安全合理应用提供了参考。Objective To observe the vascular and muscular stimulation, hemolyzation, agglutination and sensitization of class I anti- cerebral ischemic candidate drug Potassium 2- （alpha Hydroxypentyl） Benzoate （dl-PHPB） Lyophilized Powder for Injection. Methods Beagle dogs were intravenously dripped with dl-PHPB at the dose of 1.2, 3.6 and 10. 8 g/L, once daily for 30 d, with Sodium Chloride Injection as the control, and observed for 3 weeks after drug withdrawal. Rabbits were injected with dl- PHPB at a dose of 1 mg/kg or 2 mg/kg, once daily for 7 d, and observed for 2 weeks after drug withdrawal. The pathological examination was performed. The different concentrations of dl- PHPB were placed in 5 mL of rabbit red blood cells Sodium Chloride Injection for 4 h, then the hemolyzation and agglutination were observed. Guinea pigs were intravenously injected with dl- PHPB at a dose of 3 or 30 mg/kg, once every other day, for 5 times. Stimulation was performed on 14 d after last sensitization and the booster dose was 3 times of sensitization dose. The allergic reactions were observed. Results dl- PHPB Lyophilized Powder for Injection had no obvious vascular or muscular ir- ritation and injury effects on rabbits and beagle dogs. No evidences of hemolyzation and aggregation on rabbit erythrocyte in vitro, and no allergic reactions on guinea pigs in vivo were observed. Conclusion dl- PHPB Lyophilized Powder for Injection has no vascular or muscular stimulation, no sensitization in vivo, and no hemolyzation or agglutination. These research results provide reference for the clini- cal rational and safe application of dl- PHPB in clinic.

关 键 词：3-正丁基苯酞 前药2-(α-羟基戊基)苯甲酸钾 血管及肌肉刺激性 溶血 过敏 

分 类 号：R965.3[医药卫生—药理学] R972[医药卫生—药学]