复方硫酸铝注射液局部注射的安全性研究(英文)  

Experimental studies and evaluation on safety of compound aluminum sulfate injection

作　　者：徐风华[1] 符伟军[2] 张志萍[1] 王晓雄[2] 

机构地区：[1]解放军总医院临床药理药学研究室,北京100853 [2]解放军总医院泌尿外科,北京100853

出　　处：《中国临床药理学与治疗学》2006年第5期510-514,共5页Chinese Journal of Clinical Pharmacology and Therapeutics

摘　　要：目的:研究复方硫酸铝注射液肌肉注射后的局部刺激性和药物的全身吸收,并考察犬膀胱壁肌层注射后局部坏死和愈合情况,以评价该药的安全性。方法:新西兰兔股四头肌注射复方硫酸铝注射液,观察局部刺激反应;耳静脉采血,等离子体质谱法测定血铝浓度,DAS药代动力学程序处理血药浓度数据。手术暴露犬膀胱内壁,注射给药后观察药物浸润范围及愈合情况,并行病理学检查。结果:复方硫酸铝注射液兔股四头肌注射后,局部呈极严重刺激反应,血铝浓度略有升高,平均AUC0 -24为2 .93±1 .82 mg·h·L-1(n=5) ,相对生物利用度约为2 .77 %。膀胱壁肌层注射造成局部坏死,但坏死部位能够在4周内愈合,不会产生大出血、膀胱壁穿孔等严重不良反应。结论:复方硫酸铝注射液膀胱局部注射使组织坏死,药物全身吸收量很低,膀胱壁对由本品所致坏死的愈合能力强。本品是一种安全的新制剂。AIM： To study the in situ stimulation effect of compound aluminum sulfate injection after i. m. in rabbit quadriceps and dog bladder. The absorption of aluminum and the healing of the bladder wall were also studied to give an evaluation on the safety of the compound injection. METHODS： Compound aluminum sulfate injection was i.m. injected into quadriceps of the rabbits. The in situ stimulation effect was observed macrographically. Blood samples were collected at different time after i.m. injection. Aluminum concentrations were determined by ICP-MS assay and simulated with DAS software. Tissue necrosis as well as the healing of the bladder wall were observed macrographically or pathologically after the injection was given into dog bladder. RESULTS：Severe stimulation was observed after intra quadriceps injection, however, there was no obvious elevation of blood aluminum concentration. The average AUC0-24 was 2.93 ± 1.82 mg2 h· L^-1 （ n = 5）, corresponding to a relative bioavailability of about 2.77%. Injecting in bladder muscle necrotized the bladder wall in situ, but fibroblast generated and took place of the necrotized membrane and muscle four weeks after injection. There was no bleeding or perforation on the bladder wall. CONCLUSION： Caused compound aluminum sulfate injection in situ necrosis which healed up in 4 weeks. Aluminum absorption is very low after injection, giving a further explanation to the safety of the compound injection.

关 键 词：复方硫酸铝注射液 膀胱 刺激性 吸收 

分 类 号：R965.3[医药卫生—药理学]