The Quality Standard Study On Ⅲ Type New-Drug Rivaroxaban

Rivaroxaban is a kind of new anticoagulant drug and an direct factor Xa inhibitor. The drug is mainly used for prevention of the formation of deep vein thrombosis(DVT) and pulmonary embolism(PE) in patients with hip and knee replacement. It can also be used to take precautions against stroke in patients with nonvalvular atrial fibrillation and non central nervous system embolism and toreduce the risk of recurrence of coronary artery disease.Based on the fact that the domestic patent of Rivaroxaban will be expired soon and it’s new crystal patent will be authorized after the previous patent period, the quality standard for Rivaroxaban was studied in this dissertation. The study on Rivaroxaban is still in the initial stage in China and there is no relevant the quality standard for Rivaroxaban. The significance of this study lies in providing fundamental research for the listing of Rivaroxaban. Rivaroxaban has extensive market prospect as a kind of new anticoagulant drug.Firstly, the development process, function characteristics and market development of Rivaroxaban was summarized in this dissertation. Studies on pharmaceutical performance and advantages, synthetic methods, and quality control of Rivaroxaban were reported.Secondly, this dissertation studied the synthetic process of Rivaroxaban raw material. It accounted the selection principle and reasonable basis on the synthetic route of Rivaroxaban material. The basic principle and technological process of chemical synthesis process were expounded, and the main products and by-products of the synthesis procedure of the Rivaroxaban material in each step were studied. Experimental results showed that, in the synthetic process of Rivaroxaban, the choice of synthetic route was premise. The selection of raw materials and the control of synthetic conditions had important influences on the synthetic of Rivaroxaban, which directly affect the purity of main products and the formation of impurity by-products.The physicochemical properties and the quality standard of the raw materials of Rivaroxaban were studied. On one hand, the general physical and chemical properties of Rivaroxaban were investigated such as chemical structure characteristics, specific rotation, UV absorption characteristics, distribution coefficient, hygroscopic, and crystalline property, etc. On the other hand, the quality control scheme and detection method of impurity was designed. By a comparative study of the characteristics and quality control system based on 3 batches of Rivaroxaban material, the experimental results showed that, the route choice of Rivaroxaban was feasible, the physical and chemical properties of the obtained raw material Rivaroxaban was stable, the quality control method was reliable.