Formulation And Process Development Of Rivaroxaban Tablets

Thrombosis is increasingly threatening human health.Rivaroxaban tablets(trade name:Xarelto)have obvious advantages in the clinical treatment of thrombosis.But the current price is relatively high,and the single-dose price is about 15 rmb.There is no generic drug that can be replaced,and the cost of treatment is high.Therefore,imitation of rivaroxaban has obvious significance.In order to achieve the successful imitation of rivaroxaban tablets,the main purpose of this thesis is to carry out the development of prescription and process in the laboratory of the development section of the generic drug with Xarelto as a reference preparation.Studying the dissolution curve detection method and the nature of the APIs,which provides a basis for the evaluation of the development of rivaroxaban prescriptions and processes.Mainly we determine the rationality of the dissolution curve detection method from the investigation of specific properties,linear range,precision,recovery rate,solution stability,reproducibility and other items.It provides basic data for prescription and process development from the investigation of the solubility of raw materials under different pH conditions and the compatibility of raw materials with high temperature,high humidity,and light.Studying the formulation process of rivaroxaban tablets,in order to avoid infringement and reduce the risk that the dissolution curve will not fit,based on the components of the original research drug prescription,we systematically study the dosage of each component to obtain dissolution with the original research drug Products with consistent behavior.Research on rivaroxaban tablet technology.This thesis studies the process development using wet granulation,examines the processes from wet granulation to coating,and determines the suitability of the process.At the same time,as a BCS class ? drug,it studies the particle size and improves the dissolution behavior of the product.The results show that through research,we have determined a suitable dissolution test method.In the research stage,pH4.5 acetate buffer was used as the dissolution medium for the dissolution curve test to guide the development.We determined that there was no compatibility between the drug substance and the excipients.Excipients are suitable for prescription development.Using dissolution curve comparison and f2 value as the main evaluation index,the final prescription and process are determined,and it is confirmed that the co-crushing process can effectively improve the dissolution of rivaroxaban tablets.