Preparation And Lipid-lowering Effect Of Fenofibrate Sustained Release Microspheres

Objective The fenofibrate-loaded polymeric microspheres have been prepared to ensure the quality of microspheres,with high encapsulation efficiency and high drug loading,and meet the requirements and to exert sustained-release effect in vivo.Methods L9(3)4orthogonal test was used to prepare microspheres.The encapsula tion efficiency was evaluated.The effects of emulsifier,ultrasonic time and ultrasonic powe on the stability of fenofibrate sustained-release Microspheres,and to optimize the formulation and preparation of fenofibrate sustained-release microspheres.The content of fenofibrate in fenofibrate sustained-release microspheres was determined by high perfor mance liquid chromatography(HPLC).The in vitro release test,stability test and pharma cokinetic study of the fenofibrate microspheres were carried out to determine the content of fenofibrate.Whether norbet sustained-release microspheres have sustained-release and lipid-lowering effects in vivo.Results The optimal preparation method of fenofibrate sustained release microspheres was ultrasonic time 3 min,oil / water ratio 5:1,PVA concentration 2% and FN / PLGA dosage ratio of 1:2.Fenofibrate standard curve in the range of 5 ~ 90 ?g· mL-1,the linear regression equation was Y= 24.905 X + 44.269(r = 0.9998).The results showed that the prepared fenofibrate microspheres were white powder with a high particle size and a high encapsulation efficiency and drug loading.The in vitro release and stability of the fenofibrate microspheres were in agreement with each other.To meet the requirements,rats in vivo hypolipidemic test has also been a promising expected effect.Conclusions The optimal drug loading was(10.14±0.34)% and the entrapment efficiency was(77.55±1.28)% for Fenofibrate microspheres.trehalose 5% was added in freeze dried protective agent,and the white powder surface is smooth,the appearance does not collapse,do not shrink,re-dissolve faster.The HPLC method was simple,rapid and accurate for the determination of fenofibrate.It has a extraordinary effect on the treatment of hyperlipidemia,can reduce the number of times of administration and prolong the metabolic time of the drug in vivo,and provides a good theoretical basis for the development of new formulations of fenofibrate.