比较正常重力与模拟失重效应下大鼠口服龙血素B的血浆药物动力学及排泄差异.大鼠吊尾21d模拟失重效应,单次灌胃给予25mg/kg龙血素B.于系列时间点收集静脉血,并分时间段收集尿液、粪便和胆汁,采用HPLC-MS方法测定各样本中龙血素B含量,并求算药物动力学参数和排泄量.模拟失重效应下龙血素B的血药浓度-时间曲线下面积(AUC0-t)、血药峰浓度(Cmax)、达峰时间(tmax)、表观分布容积(Vd)、消除速率常数(Ke)以及生物半衰期(T1/2)与正常重力组相比均出现显著变化,说明模拟失重效应明显改变龙血素B在大鼠体内的药物动力学过程.尿液、粪便和胆汁中龙血素B的排泄量也在增加,但与正常重力相比不明显.
To study pharmacokinetics and excretion difference of loureirin B(LB)in rats after single oral administration between simulated weightlessness and gravitation condition,a series of test was executed.Rats were tail-suspended for 21 days to simulate weightlessness effect.After a single oral administration of 25mg/kg LB,venous blood and excretion samples were collected at different time points.Concentration of LB in samples was determined by HPLC-MS method.Pharmacokinetic parameters and excretion amount were calculated.Results show that,compared with normal gravity rats,the area under cuve(AUC_(0-t)),maximum concentration(C_(max)),time to peak concentration(t_(max)),volume of distribution(V_d),elimination rate constant(K_e),and biological half-life(T_(1/2))of simulated weightless rats ware significantly changed.Meanwhile,the excretion of LB in urine,feces,and bile are also up-regulated in simulated weightlessness group,while no obvious differences are observed.