复方硫酸铝注射液局部注射的药效学和全身吸收实验研究

Experimental study on the effect and the uptake of compound aluminum sulfate injection after local administration

目的 考察复方硫酸铝注射液体内对小鼠移植肿瘤生长的抑制作用 ,以及局部注射后的全身吸收情况 ,并评价用药的安全性。方法 采用瘤内一次注射给药法考察药物体内抑制肿瘤生长的作用 ;采用兔背部皮下注射后测定血铝浓度的方法考察药物的全身吸收 ;血铝浓度的测定采用等离子体质谱法。结果 复方硫酸铝注射液对小鼠移植肿瘤的生长有显著的抑制作用 ,硫酸铝是抑制肿瘤的有效成分 ,其抑制作用与剂量呈明显的正相关 ,浓度为 0 .117,0 .175 ,0 .2 34 ,0 .2 92mol·L-1时平均抑制率分别为 2 3.0 % ,32 .7% ,45 .4%和 5 3.3% ,处方中其它成分不影响肿瘤的生长。复方硫酸铝注射液兔背部皮下注射0 .46 8mmol·kg-1(以无水硫酸铝计 ) ,血铝浓度没有明显的峰值 ,最高浓度为 30 0ng·mL-1(n =5 )。结论 复方硫酸铝注射液局部注射后显著抑制肿瘤生长 ,并且硫酸铝的全身吸收量很小 ,是一种有效。

OBJECTIVES: To study the effect on graft tumor growth and absorption after local injection of compound aluminum sulfate injection. The safety of the compound injection was also evaluated. METHODS: The inhibition on the tumor growth was evaluated by weighing the tumor 4 days after administration. The compound injection was injected into the graft tumors in mice. An ICP-MS assay was used to determine the aluminum concentrations in blood. The blood samples were collected at 0,5,15,25,35,45min,1,2,4,8,24 h after sc of 0.468 mmol &middot kg-1 aluminum sulfate in New Zealand rabbits. RESULTS: Compound aluminum sulfate injection remarkably inhibited the growth of graft tumors, with aluminum sulfate being the active ingredient and the other ingredients inactive. The inhibition was in positive proportion to the concentration of aluminum sulfate, from 23.0% to 32.7%,45.4% and 53.3% as the concentration of aluminum sulfate increased from 0.117 to 0.175, 0.234 and 0.292 mol&middotL-1, respectively. There was no obvious peak of aluminum concentration after sc of 0.468 mmol&middotkg-1 aluminum sulfate. The maximum concentration was less than 300 ng&middotmL-1(n = 5). CONCLUSION: Compound aluminum sulfate injection was an effective and safe preparation that significantly inhibited the growth of tumor after intra-tumor injection and absorbed little after sc.