Formulation Process Research And Quality Evaluation Of Ezetimibe Tablets

Objective:In order to ensure the safety and effectiveness of the Ezetimibe,the formulation and preparation technology of Ezetimibe were studied based on the reference of the original preparation agent.At the same time,quality research was carried out and the corresponding quality standard was formulated,which provided the basis for the industrial production of this product.Methods:(1)The dosage of auxiliary materials including fillers,disintegrating agent,adhesives and lubricants were used to determine the formulation of Ezetimibe tablets.Meanwhile,based on mobility,hardness,friability,content and dissolution curves as the main indicators,to conduct the process screening experiment.Verify the process step by step through the small test,amplification and pilot study,and determine the key process steps and process parameters.(2)The content and dissolution rate of Ezetimibe were determined by HPLC,and the dissolution method was verified.(3)The dissolution curves of the three small samples and three pilot samples were compared with those of the original preparation agents and foreign generic drugs.Results:(1)The best prescription of the homemade Ezetimibe tablets was determined,and the process was determined to be the wet granulation tabletting process.In the process of prescription technology research,there was no significant difference in the appearance,content,dissolution and other indexes between the self-made preparation and the reference preparation,and the quality control was basically the same.(2)The results of HPLC methodological show that the method has high detection sensitivity,good separation degree,and blank excipients do not interfere with the determination of samples.Ezeimibe concentration in 6.08～101.25μg/ml(R≥0.9999)had good linearity and the method had high accuracy and good precision,which meet the requirements of the Pharmacopoeia.(3)The similarity factor f2 of the dissolution curves of the three small samples and three pilot samples and the reference preparations in four media were more than 50;the similarity factor f2 of the dissolution curves of the three small samples and three pilot samples and the foreign generic drugs in four media were also more than 50.The results showed that the dissolution of homemade Ezetimibe tablets was similar to that of reference preparation and foreign generic drugs.Conclusion:The results of this study showed that the formulation of Ezetimibe tablets was scientific and reasonable,and the preparation process was feasible and stable,which could meet the needs of industrial production.The content of the main components and the dissolution curve of the tablets was eteminated,The results provided a basis for the quality control of Ezeimibe in the later stage.