Studies On The Preparation And Quality Of Entecavir Tablets

It is reported that more than 2 billion people worldwide are infected with the hepatitis B virus(HBV)and about 350 million are chronically infected.Hepatitis B virus infection causes cirrhosis,liver failure,and primary hepatocellular carcinoma,which kills about one million people a year.Interferon and nucleoside(acid)drugs are two kinds of drugs that are internationally recognized for antiviral therapy,among which nucleoside(acid)drugs are oral drugs,convenient and quick,and are widely favored.Currently,the major drugs listed in China are adefovir dipivoxil,entecavir,lamivudine and tebivudine.Among them,entecavir tablet(ETV),a new generation of anti-HBV nucleoside analogs,was approved by FDA in the United States in March2005,followed by SFDA approval for domestic marketing in November that year.It is the first HBV-specific antiviral drug that has no cross-reaction with HIV and scarbavirus.Due to its advantages of high efficiency and very low drug resistance rate,it has become the preferred drug for this kind of treatment.The purpose of this study was to prepare stable entecavir tablets to meet the medication needs of the majority of HBV infected patients in China,as well as to reduce the drug price and meet the needs of clinical treatment of HBV infected patients.The main research contents include the pre-prescription study of entecavir tablets,the stability of raw materials,the compatibility test of raw materials and excipients,and the research on the preparation process,dissolution,quality and stability.Then the pilot scale test was carried out to screen out the final prescription process.The process was required to be simple,stable and suitable for the demand of industrial production,and the quality control standard was developed.Final prescription screening process,this paper has carried on the pilot enlarge get three batch samples,three batch samples according to the general principles of the "Chinese pharmacopoeia" 2015 edition 9001 "raw material medicine and preparation stability test guiding principles for factors affecting test,accelerated test and long-term test,the product of the content and related substances,according to the results conform to the standard.The formula adopted in this experiment is simple and stable.The pilot scale test proves that the final prescription technology can be applied to mass production.