Formulation,Process Development And Quality Evaluation Of Vildagliptin Tablets

Vildagliptin is Novartis's oral anti-diabetic new drug announced on September26,2007,approved by the European Commission.Its trade name is Galvus.It was listed in Japan in 2010 and approved for import on August 15,2011 in the country.Specifications It is 50mg.Vildagliptin is a potent and selective dipeptide-peptidase-4(DPP-4)inhibitor that rapidly and completely inhibits DPP-4 activity after administration,resulting in fasting and postprandial endogenous intestinal hypoglycaemia the levels of GLP-1(glucagon-like polypeptide-1)and GIP(glucose-dependent insulinotropic polypeptide)increase,and the amount of glucose produced in the liver decreases,which in turn reduces blood glucose.Wigligliptin tablets are suitable for the treatment of type 2 diabetes.When metformin is not effective as a monotherapy for the maximum tolerated dose,it can still effectively control blood glucose.Wigligetide tablets can be used in combination with metformin.Objective:Taking the original developer as a reference,the prescription and process of vildagliptin tablets were studied,and the quality control methods and indicators were established to simulate the bioequivalence of the original agent in vivo and in vitro.Methods:Pre-prescription studies,prescription process studies,in vitro analytical methods studies,process amplification studies,quality studies,and stability studies.Results:The raw materials are compatible with wet instability,so the relative humidity is controlled at 25 to 45%,and the vildagliptin tablets are prepared by a direct compression process.The final formulation was raw material(50 mg),microcrystalline cellulose MCC200(116 mg,dried at 80 ?),lactose monohydrate(20 mg),sodium carboxymethyl starch(12 mg),magnesium stearate(2 mg).The dissolution rate of the self-made tablets and the original preparation was determined by high performance liquid phase method.The dissolution behavior of the two tablets was similar,and the dissolution rate was more than 85%in 15 minutes.The process is amplified in three batches,the batch size is 10000 pieces/batch,the process parameters of each key process are controllable,and the test results of the finished products all meet the quality standards.The stability study shows that the influencing factors are 10 days,accelerated by 6 months and long-term 36 months.The dissolution rate is not less than 80%,the related substances are not significantly increased,the content is not significantly decreased,and the product quality is stableConclusion:Compared with the original preparation,the vildagliptin tablets produced by the designed prescription process are bioequivalent in vitro and the quality is controllable.