复方硫酸铝注射液兔体内药动学研究和安全性评价  

Study on the pharmacokinetics and safety of compound aluminum sulfate injection in rabbits

作　　者：徐风华[1] 蒋雪芹[2] 谷峰[3] 方翼[1] 高秀云[1] 

机构地区：[1]解放军总医院临床药理药学研究室,北京100853 [2]天津医科大学,2002级本科实习生天津300070 [3]解放军总医院生化科,北京100853

出　　处：《药学服务与研究》2006年第3期200-202,共3页Pharmaceutical Care and Research

摘　　要：目的:研究复方硫酸铝注射液静脉注射后的药动学和肌肉注射后的全身吸收,以及注射后血清生化指标的变化。方法:兔耳静脉注射复方硫酸铝注射液1 mg/kg(以无水硫酸铝计)和股四头肌注射80 mg/kg(以无水硫酸铝计),耳静脉采血,采用等离子体质谱法测定血铝浓度,并常规测定血生化指标。结果:静脉注射复方硫酸铝注射液后,硫酸铝体内药动学过程符合二房室模型,t1/2β为(1.08±0.46)h,AUC0→24 h为(1.52±0.92)mg.h.L-1(n=5)。股四头肌注射复方硫酸铝注射液后,血铝浓度略有升高,但不明显,不能进行药动学参数分析。采用梯形法计算AUC,平均AUC0→24 h为(2.93±1.82)mg.h.L-1(n=5),复方硫酸铝注射液肌肉注射后铝的生物利用度约为2.41%。血清生化指标除偶见丙氨酸氨基转移酶升高和肌肉注射组肌酐水平缓慢下降,其余未见明显改变。结论:复方硫酸铝注射液静脉注射后血液中清除速率快,局部注射后全身吸收量很低,是一种安全的新制剂。Objective： To study the pharmacokinetics of compound aluminum sulfate injection after iv injection in rabbits and its absorption after im injection. Methods： Compound aluminum sulfate injection 1 mg/kg was injected iv to the left-ear or 80 mg/kg im in femoral quadriceps. Blood samples were collected at different time points after injection from the right-ear vein. ICP-MS assay was used to determine the aluminum concentration. Pharmacokinetic parameters were calculated with DAS program. The clinical biochemical analyses were conducted with an automatic analyzer. Results： The blood aluminum concentration-time profiles after iv injection of 1 mg/kg aluminum sulfate fitted to a two-compartment model, with t1-2β（1.08±0.46） h and AUC0→21h（1.52±0.92） mg · h · L^-1 （n=5）. A little elevation of blood aluminum concentration was seen after im injection of 80 mg/kg aluminum sulfate. The average AUC0→24h was （2. 93±1. 82） mg · h· L^-1（n=5） and bioavailability was only 2.41%. Except for an occasional elevation of alanine aminotransferase in both groups and a slow decrease in creatinine level in im group, no obvious changes in the serum levels of clinical biochemical parameters were seen after drug administration. Conclusion： Compound aluminum sulfate injection is a safe preparation which is poorly absorbed after im injection.

关 键 词：复方硫酸铝注射液 药物动力学 安全性 

分 类 号：R917.1[医药卫生—药物分析学] R979.19[医药卫生—药学]