中枢神经兴奋剂莫达非尼在大鼠体内的药动学

Study on pharmacoknetics of modafinil in rat

目的 :研究SD大鼠单剂量口服莫达非尼后 ,莫达非尼在大鼠体内的药动学特征。方法 :SD大鼠单剂量 4 .0mg·kg-1 灌胃莫达非尼混悬液 ,于各时间点 ,心脏取血 ,分离血清 ,用高效液相色谱法测定莫达非尼的浓度 ,所得血药浓度 时间数据用 3P87药动学软件处理 ,求得药动学参数。结果 :莫达非尼药 时曲线符合二室模型 ,T1 /2α为 (0 .4 8± 0 .0 9)h ,T1 /2 β为(3.5 5± 0 .2 7)h ,Tmax为 (0 .79± 0 .0 6 )h ,Cmax为 (3.5 3± 0 .0 5 )mg·L-1 ,AUC0～∞ 为 (1 4 .32± 0 .30 )mg·h·L-1 。结论 :莫达非尼在大鼠体内分布较快 ,消除较慢 ,具有良好的药代动力学特征。

OBJECTIVE To study the pharmacokinetics behavior of modafinil in rat.METHODS The concentration of modafinil in serum was determined by HPLC following a single oral dose. The pharmacokinetics parameters were fitted by 3P87 program. The steady state concentrations of modafinil in blood were also determined by HPLC.RESULTS The RSD of intra day and inter day were less than 3%.The serum concentration curves fitted the two compartment model. The main parameters were as follows: T 1/2α was ( 0.48 ± 0.09) h , T 1/2β was ( 3.55 ± 0.27) h , T max was ( 0.79 ± 0.06) h , C max was ( 3.53 ± 0.05) mg ·L -1 ,AUC 0～∞ was ( 14.32 ± 0.30) mg .The actual value and expectant result was anastomotic elementally. CONCLUSIONS The distribution of modafinil in rats is fast, the elimination is slow.