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目的:研究复方硫酸铝注射液静脉注射后的药代动力学以及肌肉和皮下注射后的全身吸收。方法:兔耳静脉、股四头肌和背部皮下注射,耳静脉采血,采用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。结果:静脉注射复方硫酸铝注射液1 mg.kg-1(剂量均以无水硫酸铝计),硫酸铝体内药代动力学过程符合二房室模型,t1/2β为1.08±0.46 h,AUC0-12h为1.52±0.92mg.h.L-1(n=5)。股四头肌注射复方硫酸铝注射液80 mg.kg-1,血铝浓度略有升高,但不明显,采用梯形法计算曲线下面积,平均AUC0-24h为2.93±1.82 mg.h.L-1(n=5),相对生物利用度约为2.41%。皮下注射160 mg.kg-1,血铝浓度没有明显的峰值,平均AUC0-24h为0.88±1.14 mg.h.L-1(n=5),相对生物利用度约为0.36%。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 intravenous injection and systemic absorption after intramuscular and subcutaneous injection. Methods: Rabbit ear vein, quadriceps femoris and back were injected subcutaneously and blood was collected from the ear veins. Plasma aluminum concentration was determined by plasma mass spectrometry. DAS pharmacokinetic program was used to process plasma concentration data. RESULTS: Intravenous injection of compound aluminum sulfate injection 1 mg.kg-1 (all based on anhydrous aluminum sulfate) showed that the pharmacokinetics of aluminum sulfate conformed to the two-compartment model with t1 / 2β of 1.08 ± 0.46 h and AUC0- 1.52 ± 0.92 mg.hL-1 (n = 5) at 12 h. Intracranial injection of compound aluminum sulfate 80 mg.kg-1, blood aluminum concentration increased slightly, but not obvious, using the trapezoidal method to calculate the area under the curve, the average AUC0-24h was 2.93 ± 1.82 mg.hL-1 (n = 5), relative bioavailability was about 2.41%. Subcutaneous injection of 160 mg.kg-1, blood aluminum concentration showed no significant peak, the average AUC0-24h was 0.88 ± 1.14 mg.h.L-1 (n = 5), the relative bioavailability of about 0.36%. Conclusion: The compound aluminum sulfate injection has a fast clearance rate in the blood and a very low systemic absorption after local injection. It is a safe new preparation.