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模拟失重效应下龙血素B在大鼠体内的药物动力学及排泄

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模拟失重效应下龙血素B在大鼠体内的药物动力学及排泄
Study on Pharmacokinetics and Excretion of Loureirin B in Rats Under Simulated Weightlessness Condition
投稿时间:2016-03-03
DOI:10.15918/j.tbit1001-0645.2017.08.019
中文关键词:模拟失重龙血素B药物动力学药物排泄
English Keywords:simulated weightlessnessloureirin Bpharmacokineticsexcretion
基金项目:国家自然科学基金资助项目(81573693);国家重大仪器专项基金资助项目(2012YQ040140);1226重大基金资助项目(AWS16J018)
作者单位E-mail
陈博北京理工大学 生命学院, 北京 100081
张宇实中国中医科学院中药研究所, 北京 100029
苏靖河北省邢台市第三医院, 河北, 邢台 054000
王睿北京理工大学 生命学院, 北京 100081
邓玉林北京理工大学 生命学院, 北京 100081
李玉娟北京理工大学 生命学院, 北京 100081lylyjlzh2006@163.com
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中文摘要:
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21 d模拟失重效应,单次灌胃给予25 mg/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.
English Summary:
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 25 mg/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 (AUC0-t), maximum concentration (Cmax), time to peak concentration (tmax), volume of distribution (Vd), elimination rate constant (Ke), and biological half-life (T1/2) 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.
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