Solvent evaporation method for preparation of nanomatrix has the disadvantages,such as residual organic solvent,environmental pollution,explosion-proofing and so on.To overcome these shortcomings,a series of fenofibra...Solvent evaporation method for preparation of nanomatrix has the disadvantages,such as residual organic solvent,environmental pollution,explosion-proofing and so on.To overcome these shortcomings,a series of fenofibrate nanomatrix drug delivery system(NDDS)consisting of nano-porous silica Sylysia■350(S350)and pH sensitive material Eudragit■L100-55(EL100-55)were prepared using hot-melt extrusion(HME),and their in vitro dissolution and in vivo bioavailability were compared.Finally,the formulation with the highest in vivo bioavailability was selected as the optimized formulation for DSC and PXRD characterization.The results showed that the optimized NDDS showed a higher bioavailability than the reference formulation,although there was crystalline form drug remaining in NDDS.The relative bioavailability of the optimized formulation was 157.1%compared with the commercial product Lipanthyl■.In addition,the relative bioavailability of the optimized formulation was 124.8%in comparison with the formulation prepared by solvent evaporation method,showing that the NDDS prepared by the HME method was effective in improving the bioavailability of fenofibrate.In conclusion,HME was a promising method to prepare NDDS.展开更多
基金National Basic Research Program of China(Grant No.2015CB932100)
文摘Solvent evaporation method for preparation of nanomatrix has the disadvantages,such as residual organic solvent,environmental pollution,explosion-proofing and so on.To overcome these shortcomings,a series of fenofibrate nanomatrix drug delivery system(NDDS)consisting of nano-porous silica Sylysia■350(S350)and pH sensitive material Eudragit■L100-55(EL100-55)were prepared using hot-melt extrusion(HME),and their in vitro dissolution and in vivo bioavailability were compared.Finally,the formulation with the highest in vivo bioavailability was selected as the optimized formulation for DSC and PXRD characterization.The results showed that the optimized NDDS showed a higher bioavailability than the reference formulation,although there was crystalline form drug remaining in NDDS.The relative bioavailability of the optimized formulation was 157.1%compared with the commercial product Lipanthyl■.In addition,the relative bioavailability of the optimized formulation was 124.8%in comparison with the formulation prepared by solvent evaporation method,showing that the NDDS prepared by the HME method was effective in improving the bioavailability of fenofibrate.In conclusion,HME was a promising method to prepare NDDS.
