Preparation Of Silybin Nanoparticles By High Gravity Reaction Precipitation Method And Silybin Capsules

Silybin is an antioxidant and it can help stabilize the liver cell membrane and increase the anti toxic ability of liver cells.It is commonly used in the treatment of acute and chronic hepatitis,and early cirrhosis and fatty liver.However,the water solubility of silybin is very poor,which causes it is difficult to be absorbed as an oral preparation and poor bioavailability.and nanotechnology can reduce the particle size of drugs,thereby increase the solubility of drugs,thus raising the bioavailability of drugs.In this paper,the nano composite powder of silybin was prepared by the reaction precipitation method and the super gravity reaction precipitation method,and the silybin capsule was also made by composite particles.The main contents of the full text are as follows:1.Silybin nanocomposite particles were prepared by reaction precipitation and optimized high gravity reaction precipitation method.The effects of acid type,acid base ratios,concentration of acid and drug,reaction temperature,dosage and type of surfactants,rotational speed of rotating packed bed,feed rate,and drying methods on the morphology and average particle size of silybin composite particles were investigated,and the properties of the products were characterized.The results show that the optimum technological conditions are:making silybin in 0.1 mol/L sodium hydroxide to form a concentration of silybin with a concentration of 25 mg/ml,acid solution of 0.1 mol/L hydrochloric acid,acid base ratio was 1.1,reaction temperature was 15 ℃,PVP was used as stabilizer and the ratio of stabilizer/drug substance was 1.0,the rorating speed of rotating packed bed was 2150 rpm,feeding speed was 160 ml/min.The average particle size of silybin could be obtained in the slurry with an average diameter of about 65 nm,and it can be 178 nm in water dispersing after further spary drying process.The results of characterization analysis showed the crystalline form of the silybin composite powder was reduced,the particle size decreased obviously,and the dissolution rate was obviously improved,and the dissolution rate was about 4.8 times that of the raw material in 120 minutes.2.The process of preparing silybin capsules by silybin composite powder was also carried out.The optimization of granulating mode,filling agent,fluxing agent,surfactant and disintegration agent was carried out mainly on the fluidity and dissolution rate.The optimum technological parameters in the experimental range were 2 granulations by dry granulator,the filling agent as the direct pressure lactose with the ratio of filling agent/composite powder was 1:1 and the micropowder silica gel with the mass fraction of 1%,The surface active agent was SDS with mass fraction of 1%,and the disintegration agent was CCMC-Na with a mass fraction of 1%,and the addition method was selected by internal and external.And the dissolution rater can reach 88.2%in 120 minutes.