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《Academic Journal of Second Military Medical University》 2017-02
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Pharmacokinetics and in situintestinal absorption of evodiamine complex water-in-oil nanoemulation

YAN Sheng-lei;HU Jiang-bo;WANG Xue;SHI Ming-xin;ZHANG Jing-qing;Chongqing Research Center for Pharmaceutical Engineering,Chongqing Medical University;Department of Pharmacy,Chongqing Nan'an Maternal and Child Health Care Hospital;  
Objective To investigate the pharmacokinetic behavior and in situ intestinal absorption of evodiamine complex water-in-oil nanoemulation(WECNE).Methods WECNE was formulated with the titration stirring methods.Twelve male SD rats were intragastrically administered with evodiamine(EDA)and WECNE at the same EDA dose of100mg·kg-1.Blood samples were collected from eye socket at 0.083,0.25,0.5,0.75,1,2,5,8,12,24,48and72 hafter intragastrical administration,and the plasma concentrations of EDA were determined by RP-HPLC.DAS 2.1.1software was applied to evaluate the pharmacokinetic behavior.Single-pass intestinal perfusion was carried out to test the intestinal absorption in situ.Results The area under the curve(AUC0-72h),peak concentration(Cmax)and time to peak(Tmax)of WECNE were(4 924.59±1 105.28)μg·L·h-1,(305.47±51.23)μg·L-1 and(0.83±0.29)h,respectively.The absorption rate constant(Ka)of WECNE in the stomach,duodenum,jejunum,ileum and colon were(1.05±0.82)×10~(-5),(12.19±1.57)×10~(-5),(12.66±1.35)×10~(-5),(11.94±4.17)×10~(-5) and(11.21±1.25)×10~(-5) L·s~(-1),respectively.In addition,the effective permeability(Peff)of WECNE in the duodenum,jejunum,ileum and colon were(26.03±3.84)×10~(-5),(18.48±5.99)×10~(-5),(19.77±2.59)×10~(-5) and(36.02±1.48)×10~(-5) cm·s~(-1),respectively.Conclusion WECNE can improve the bioavailability and the absorption in situ of EDA in different parts of the gastrointestinal tract.
【Fund】: 重庆市科委项目(cstc2015jcyjBX0027)~~
【CateGory Index】: R285.5
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