Preparation And Characterization Of Ultrafine Prednisolone

In ninety percent of all medicines, the active ingredient is in the form of solid particles, and the particulate systems have a great impact on the quality of the final product, which are the important factors for the choice of the best formulation in the product development process. Prednisolone (PDL), is a very slightly water soluble synthetic adrenal corticosteroid, whose micronization is of great importance. Spray drying method and anti-solvent recrystallization method were employed in this study to obtain ultrafine prendnisolone of various morphologies and particle sizes.In spray drying method, different systems such as solutions and suspensions were spray dried and the influence of inlet temperature was discussed, and spherical particles with a mean particle size of1.07μm, clubbed particles with2～3μm in width and5～30μm in length and drug complex particles with an average particle size of3.56μm were successfully prepared.N and W were finally chosen as the solvent and anti-solvent, and surfactant Q was added to modify its crystal habits. Subsequently, hexagonal and tetragonal microcrystals were obtained by the anti-solvent recrystallization method. After F as the anti-solvent was introduced, hexagonal and tetragonal microcrystals with narrow particle size distribution (PSD) and mean particle size1.60and1.46μm were obtained under the optimum condition.The products prepared by the two methods were characterized by SEM> XRD、FT-IR and dissolution test, etc. The dissolution results showed that spherical particles obtained by spray drying the solution had much poorer dissolution rate due to the crystal form transition, while both microcrystals prepared by anti-solvent recrystallization were more stable in water than crude drug, and exhibited obviously higher dissolution rate and better anti-inflammation than that of raw materials in primary animal experiment.