| Everolimus is a derivative of rapamycin,belongs to the mTOR inhibitor,a serine threonine kinase downstream of the PI3K/AKT pathway.The drug was first researched by Swiss company Novartis and was first approved in Sweden in 2003 to prevent rejection after kidney transplants and heart transplants.In March 2009,everolimus was approved in the United States for patients with advanced renal cell carcinoma after the treatment of sunitinib or sorafenib.Everolimus can slow the growth of renal cell carcinoma and reduce the death rate by 67%,by inhibiting the growth and proliferation of tumor cells,it directly acts on tumor cells.It can be used to reduce tumor blood vessels and play an indirect role in anti-tumor.Through looking at the FDA and EMEA relevant information,the original company has approved with the dimension of therapy existing 2.5 mg,5 mg,and 10 mg,but there are residual solvents and stability problems,the paper to overcome defects of existing technology as a starting point,studied 2.5 mg and 10 mg prescription craft,The solid dispersion was prepared by using hydroxypropyl cellulose instead of hypromellose,and then mixed with other excipients,suppress tablet.through the screening of the prescription of everolimus tablets,the study of the solution curve of everolimus tablets,the determination of the prescription of everolimus tablets,stability investigation of everolimus tablets,preliminary verification of processof everolimus tablets,shows that dissolution reproducibility of this product and the copy are well using the f2 factor method for evaluating the similarity of the dissolution curve of this product and the copy.In order to achieve the goal of controlling its quality and improving the quality standard,this paper carried out the research on the quality research and stability of the prepared everolimus tablets.The everolimus tablets content of quality research is to study on the characteristics,identification and inspection(water,content uniformity,solubility,related substances,isomers,content,etc.),as well as the dissolution,the relevant material and content of method validation,the suitable determination method for the quality of the product prescription and process of application.The results showed that the special attribute method is strong,accurate,high precision,linear range conform to the requirements of the content determination,through the method of determination indicators of the everolimus in accordance with the dimension of the Chinese Pharmacopoeia 2010,the sample peak is well separated from the related material peak,the peaks of everolimus and its isomers and the degradation products after the forcible destruction can be effectively separated,and the relevant materials are far below the standard of pharmacopoeia,this method can be used as an inspection method of everolimus tablets.The stability study highly inspects influence factor test,accelerated test,long term stability test.The results showed that the high temperature(60 ℃),light(4500 lx),high humidity(75%15%,92.5%±5%)conditions,the matter is obviously increased under the conditions of high temperature and high humidity;however,it is stable under of lighting and accelerated experiments conditions,which is in accordance with Chinese pharmacopoeia.It shows that everolimus is sensitive to heat and humidity,and should be protected from moisture proof,should be preserved at normal temperature.The results of this article provides the basis for filling the domestic blank and realize industrialization in the future. |
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