Studies In Preparation And In Vitro Evaluation Methods Of Methylprednisolone Aceponate Cream

Methylprednisolone aceponate（MPA）is a new type of glucocorticoid.The Methylprednisolone aceponate cream（commercial name:Advantan^?）,which is marketed in Germany,has been proven to have a high therapeutic effect on dermatitis and eczema,and the side effects have the lowest side effects in similar drugs.At present,it has not been approved for marketing in China.In this paper,the prescription and preparation process were optimized from the micro-phase structure of the cream,and the MPA cream with the same quality as reference.First,The research study the physical and chemical properties of MPA.The results show that MPA has a suitable melting point and the solubility of MPA in the 20%ethanol-PBS can meet the condition of sinking,and the stability in 24 hours is suitable.The forced degradation test of MPA showed that MPA has poor stability under strong acid,alkali,H₂O₂ and high temperature conditions.It can be kept stable under high light conditions.Then,optimize the prescription of the MPA cream.The effects of glyceryl monostearate,hard fat and polyoxyl 40 stearate on the physical properties of the cream were investigated by single factor experiments.Furthermore,the effects of different excipients on the release of MPA were investigated.The optimum ratio of oil phase matrix was investigated by orthogonal test.The research is to investigate the effect of different emulsifier ratios on the physical properties and release properties of the cream.The prescription with similar release behavior of the reference was selected as the most optimal one.The effects of the preparation process on the physical properties of the cream were further investigated.After several researches about the emulsification time of MPA cream and the number of high pressure homogenization,the preparation process of MPA cream was finally determined.Finally,the experimental method of the cream release test was verified,and the particle size distribution measurement methodology is initially examined.The results show that the cream release methodology meets the methodological requirements and determines the particle size methodological parameters.The refractive index is 1.59,the absorption rate is0.001,and the pump speed is 2000 rpm.In summary,this study prepared a MPA cream that was consistent with Advantan^?in physical properties and drug release through formulation and process optimization,and provided a method that can be used to verify the in vitro release of creams,and method for determining the particle size distribution of a cream.