Study On Preparation Technology Of Simvastatin Chitosan Nanoparticles

Objective: To establish an in vitro method for simvastatin analysis.The optimal formulation and preparation method of simvastatin chitosan nanoparticles and their tablets were optimized,and their quality was evaluated.Methods: simvastatin in vitro analysis method was established by high performance liquid chromatography.Simvastatin chitosan nanoparticles were prepared by using simvastatin chitosan nanoparticles.The appearance grade score and encapsulation rate of nanoparticles were used as the evaluation indexes.The best preparation process of chitosan nanoparticles was optimized by using the encapsulation rate as the index.Phase identification was carried out by microscope(10×100 times)and differential scanning calorimetry.Particle size distribution was determined by laser particle size distribution instrument.Chitosan nanoparticles were characterized and their quality was evaluated.According to the tablet quality standard,the best formulation and preparation process of simvastatin chitosan nanoparticles were optimized by investigating the hardness,weight difference,content determination and release degree of the tablets.According to 0931,four general principles of the Chinese pharmacopoeia(2015),a quality evaluation standard for simvastatin chitosan nanoparticles was established.Results: Simvastatin chitosan nanoparticles were prepared by improved emulsion diffusion-ion exchange method.High performance liquid chromatography(HPLC)was used to establish the in vitro analysis of simvastatin.The best formulation of simvastatin chitosan nanoparticles is chitosan carrier,poloxam 188 as emulsifier,anhydrous ethanol as emulsifier,soybean phospholipid as surfactant,sodium tripolyphosphate as anionic polymer.The ratio of simvastatin to soybean phospholipid was 1:5.58,that of simvastatin to chitosan was 1:5.38,that of poloxam 188 to soybean phospholipid was 2:1,that of rotation speed was 800r/min,that of stirring time was 30.14 minutes,and that of sodium tripolyphosphate was 2mg/ml.Microscopy(10 x 100 times)results showed that chitosan drug-loading nanoparticles for circular droplets,the size of 262.4 nm,dispersion coefficient is 0.39,differential scanning heat method results show that the drug Mosaic or coated with chitosan,further nanoparticles prepared into tablet,optimum process for freeze drying time 30 hours,tablet pressure of 7 ~ 10 KGF,in vitro release was 92.61%,compared with simvastatin tablets have obvious sustained release effect,drug release model was fitted to prove its level of drug release;Verification test shows that the process is stable and feasible.The standard for quality evaluation of simvastatin chitosan nanoparticles was established.Conclusion: The stability of simvastatin chitosan nanoparticles tablets is good,the process is simple and the quality standard is perfect.