小鼠经口给予纳米雄黄后砷的药动学特点

The features of pharmacokinetic of Arsenic in the rats after the nano-realgar was taked orally

目的:研究纳米雄黄与传统水飞雄黄中砷在小鼠体内的药动学行为差异,为新药的研发及临床用药提供一定的实验基础。方法:以140只小鼠为研究对象,随机分为两组,每组70只,分别单次灌胃2.062mg·mL-1的纳米雄黄和水飞雄黄混悬液0.5mL,于服药后不同时间点摘眼球采血,用电感耦合等离子体质谱仪(ICP-MS)测得血中砷元素浓度,计算主要药动学参数。结果:纳米雄黄组与传统水飞雄黄组中砷的药代动力学参数经统计学分析均有显著差异(P<0.05)。纳米雄黄中砷达峰时间早、峰浓度高、药时曲线下面积(AUC)大,前者砷的消除半衰期较长,吸收速率常数较大。结论:纳米雄黄组在达峰时间、峰浓度、AUC等方面优于传统雄黄组。纳米雄黄组与传统水飞雄黄组相比,砷吸收快,消除慢,药物在体内维持时间长,说明雄黄经过纳米化后,其药动学特性发生明显变化,吸收速率增大而消除速率减小。

Objective：To study the pharmacokinetics of arsenic of nano-realgar in rats and compare the differences of pharmacokinetics between nano-realgar and traditional realgar. Provide basis of experiments for the research and development of new drugs, and clinical medications. Methods： 140 rats were divided into two groups by random, and then a single ig dose of 2. 062 mg·mL^-1 of nano-realgar and traditional realgar were given to the two groups, 0.5 mL respectively. To collect serum samples after ig of drugs in rats at certain time. The concentration of arsenic in samples were determined by ICP-MS. Results： There was a significant difference in pharmacokinetics parameters between nano-realgar group and traditional realgar group. Tpeak, C and AUC in nano-realgar group were better than traditional realgar, t1/2 Ke of arsenic in nano-realgar group was longer. Conclusion： Compared with traditional realgar, arsenic of nano-realgar distributed more quickily but eliminated slowly. Nano-reaglar had better pharmacokinetics parameters in-vivo. The studies we had done could accelerate the development of nanorealgar.