不同环境条件下大鼠体内莫沙必利药代动力学比较研究  

Comparative Study on Pharmacokinetics of Mosapride in Different Environmental Conditions in Rats

作　　者：张娟红[1,2] 向大伟[3] 王荣[1,2] 谢华[1] 尹强[1] 贾正平[1,2] 李文斌[1] 王延玲[1,2] 武晓玉[1] 

机构地区：[1]兰州军区兰州总医院全军高原损伤防治重点实验室,兰州730050 [2]兰州大学药学院,兰州730000 [3]兰州军区兰州总医院医务部,兰州730050

出　　处：《解放军医药杂志》2013年第6期24-27,共4页Medical & Pharmaceutical Journal of Chinese People’s Liberation Army

基　　金：国家科技部重大资助项目(2008ZXJ09014-010);全军医药科研"十二五"重点项目(BWS12J012);全军医药科研"十二五"面上项目(CWS11C231)

摘　　要：目的探讨平原组与急进高原组大鼠体内莫沙必利的药物代谢动力学特征。方法 7只Wistar大鼠相隔一周清洗期分别于平原(平原组)及高原地区(急进高原组)禁食12 h后将0.0027 g(约含莫沙必利0.10 mg)枸橼酸莫沙必利片剂灌胃。于给药前(0 h)及给药后0.083、0.25、0.5、0.75、1、1.5、2、4、6、8、12、24 h由眼眶后静脉丛取血,采用高效液相色谱-串联质谱法测定血药浓度。结果莫沙必利平原组与急进高原组比较药代动力学参数发生显著变化,药时曲线下面积从(2.909±0.385)μg/L.h增大到(9.549±2.019)μg/L.h,峰浓度增大,半衰期、达峰时间、体内平均驻留时间延长,总清除率降低。结论急进高原后,莫沙必利在大鼠体内代谢过程发生明显改变,研究结果为平原和急进高原后临床合理应用莫沙必利提供参考依据。Objective To explore pharmacokinetics of mosapride in rats lived in plains （group A） and highland （ group B） after acute movement. Methods One week wash-out period later, 7 Wistar rats in groups A and B underwent intragastric administration with 0. 0027g （0.10 mg of mosapride） of M osapride citrate tablets after fasting for 12 h. Blood drug levels in veins of eye socket were detected with high-performance liquid chromatography and tandem mass spectrome- try （HPLC-TMS） before medication （0 h） , at 0.083,0.25,0.5, 0.75, 1, 1.5, 2, 4, 6, 8, 12 and 24 hours after medication. Results Mosapride pharmacokinetic parameters in group A were significantly different from those in group B, area under curve during medication from （ 2. 909 ± 0. 385 ） μg/L · h to （9. 549 ± 2. 019） μg/L · h, the Cmax in group B was significantly higher; half life period, Tmax and intracorporal average residence time in group B were signifi- cantly prolonged, while total body clearance in group B was reduced. Conclusion Rats＇internal metabolic processes of Mosapride may significant changes after acute movement in highland, which may provide references for clinical rational application of Mosapride in plains and after acute movement in highland.

关 键 词：莫沙必利 药代动力学 大鼠 高效液相色谱-串联质谱法 高原病 

分 类 号：R-332[医药卫生] R969.1