5-Aminosalicylic Acid Microemulsion Delivery System And Solid Preparation Research

Objective:A method for the determination of 5-aminosalicylic acid in vitro was established.The optimal formulation and preparation process of 5-aminosalicylic acid microemulsion and its suppository were optimized,and its quality standard was established.The initial stability was investigated.Methods: Establish a high performance liquid chromatography determination of 5-aminosalicylic acid in vitro analysis method,5-aminosalicylic acid prepared by phase inversion emulsification method microemulsion,using the single factor investigation and response surface method,with microemulsion,pseudo ternary phase during a appearance grade index,optimize the best prescription of microemulsion coating rate as index,the best preparation technology of optimized microemulsion and through differential scanning for characterization and quality evaluation;The optimum freeze-drying process of 5-aminosalicylic acid microemulsion was optimized by taking the characteristics and encapsulation rate of freeze-dried powder as the index.The optimal formulation and preparation process of 5-aminosalicylic acid microemulsion suppositories were optimized by taking the weight difference and melting time of suppositories as investigation indexes.The quality standard of 5-aminosalicylic acid microemulsion suppository was established according to the "suppository guiding principle" of general principles 0107 of Chinese pharmacopoeia(2015).Result:A scientific and feasible method for the determination of 5-aminosalicylic acid in vitro was established by HPLC.5-aminosalicylic acid microemulsion preparation process for the best emulsifier for the polyoxyethylene hydrogenated castor oil,auxiliary emulsifier for propylene glycol,oil phase for oleic acid ethyl ester,water phase for phosphate buffer,solvent amount to 20 ml,mixing temperature of 35 ℃,the ratio of emulsifier and auxiliary emulsifier for 4:1,oil mixed with emulsifier ratio of 4:6,stirring time 30 minutes,stirring speed of 450 rotations per minute(RPM),the first to join the emulsifier and auxiliary emulsifier,add oil and stir well,join the prescriptions of5-aminosalicylic acid,stir in water phase.The best technology of 5-aminosalicylic acid microemulsion powder is freeze-drying.Differential scanning proved 5-aminosalicylic acid in the amorphous and amorphous state exists in microemulsion,through melting method with 5-aminosalicylic acid microemulsion producing and semi synthesis fatty acid glyceride(36),the preparation of suppository,mode of mixing,pouring temperature and cooling temperature investigation,determine the mixing method for magnetic stirring,pouring temperature of 40 ℃,4 ℃ cooling 10 min,established quality standards.Conclusion: The preparation process of 5-aminosalicylic acid microemulsion is simple,feasible and feasible,and the quality standard is perfect,which is suitable for large industrial production.