Preparation And Quality Evaluation Of EDM Nanoemulsion

Evodiamine(Evodiamine,EDM) is the ingredients extracted from thetraditional Chinese medicine Evodia.It has anti-inflammatory, analgesic,weight loss, anti-tumor and other pharmacological effects.Recent researchon the anti-tumor activity showed that EDM has broad developmentprospects.However the bioavailability of the EDM in vivo is toolow.Therefore,this paper prepared EDNE to improve the bioavailability ofthe EDM and evaluated EDNE from the in vitro nature,in the intestinalabsorption and pharmacokinetics.The first part of this paper prepared EDNE and determined theaverage particle size and average Zeta potential of EDNE.They were28.68nm and-12.0mV respectively.First established a HPLC method for thedetermination of in vitro samples, the regression equationis:A=212.9160C-1.5549,r=0.9995(n=5),the concentration range of0.2~15μg·mL-1.This paper examined the EDM and EDNE in vitro release.Theresults showed EDNE improved the vitro release of EDM,and both releasebehavior in0.1mol·L-1HCl and pH6.8PBS were in line with the Weibull model.The second part of this paper studied rats absorbed in theintestines.The experimental resulted that the average percentage of thetotal absorption of EDM and EDNE in the duodenum, jejunum, ileum andcolon four bowel were (12.34±2.09)%and (49.21±10.89)%respectively.The absorption rate constant (Ka) and the effectivepermeability (Peff) of EDNE in four intestine were higher than EDM.Thisillustrated that EDNE increased absorption of EDM in the intestine.The third part of this paper studied the bioavailability of EDNE.Firstestablished a method for determination of EDM in plasma,the regressionequation:Y=3.6488C-0.0380,r=0.9989(n=5),linear range was0.03~0.5μg·mL-1.Then determinated EDM concentrations in plasma samples atdifferent points of time,and fitted non-compartmental model (statisticalmoments) by DAS software.The main pharmacokinetic parameters:TmaxofEDM and EDNE were (2.17±2.45) h and (0.75±0.02) h,Cmaxwere(82.2219.07) μg·L-1and (409.73±64.60) μg·L-1,AUC(0-48h)were(781.25±139.38) μg·h·L-1and (1723.88±467.91) μg·h·L-1.Thebioavailability of EDNE was220%that of EDM.