复方硫酸铝注射液局部注射的安全性研究

中国临床药理学与治疗学 ›› 2006, Vol. 11 ›› Issue (5): 510-514.

复方硫酸铝注射液局部注射的安全性研究

徐风华, 符伟军¹, 张志萍, 王晓雄¹

解放军总医院临床药理药学研究室, ¹泌尿外科, 北京 100853

收稿日期:2006-02-28 接受日期:2006-05-11 出版日期:2006-05-26 发布日期:2020-12-09

Experimental studies and evaluation on safety of compound aluminum sulfate injection

XU Feng-hua, FU Wei-jun¹, ZHANG Zhi-ping, WANG Xiao-xiong¹

Division of Clinical Pharmacology &Pharmaceutics, ¹Department of Urology, PLA General Hospital, Beijing 100853, China

Received:2006-02-28 Accepted:2006-05-11 Online:2006-05-26 Published:2020-12-09
Contact: XU Feng-hua, female, master, associate researcher, tutor of master, main research fields are novel drug delivery system. Tel:010-85455768 　 E-mail:xufh@yahoo.com

摘要/Abstract

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 AUC_0-24 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。

关键词: 复方硫酸铝注射液, 膀胱, 刺激性, 吸收

Abstract: AIM: To study the in situ stimulation ef-fect 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 com-pound injection.METHODS: Compound aluminum sul-fate injection was i.m.injected into quadriceps of the rabbits.The in situ stimulation effect was observed mac-rographically.Blood samples were collected at different time after i.m.injection.Aluminum concentrationswere 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 pathologi-cally after the injection was given into dog bladder.RESULTS: Severe stimulation was observed after intra quad-riceps injection, however, there was no obvious elevation of blood aluminum concentration.The average AUC_0-24 was 2.93±1.82 mg·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 fi-broblast generated and took place of the necrotized mem-brane and muscle four weeks after injection.There was no bleeding or perforation on the bladder wall.CONCLU-SION: Caused compound aluminum sulfate injection in situ necrosis which healed up in 4 weeks.Aluminum ab-sorption is very low after injection, giving a further expla-nation to the safety of the compound injection.

Key words: compound aluminum sulfate injection, bladder, stimulation effect, absorption

中图分类号:

R965.3

徐风华, 符伟军, 张志萍, 王晓雄. 复方硫酸铝注射液局部注射的安全性研究[J]. 中国临床药理学与治疗学, 2006, 11(5): 510-514.

XU Feng-hua, FU Wei-jun, ZHANG Zhi-ping, WANG Xiao-xiong. Experimental studies and evaluation on safety of compound aluminum sulfate injection[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2006, 11(5): 510-514.

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