Study On The Preparation Technology And Quality Control Of The Vonoprazan Fumarate Tablets

Vonoprazan fumarate(TAK-438,Takecab)is a potassium ion competitive acid blocker developed by Takeda Pharmaceuticals, the first time approved the listing in Japan is December 2014 for the treatment of Helicobacter pylori infection,gastroesophageal reflux, peptic ulcer, duodenal ulcer, esophagitis, ulcers and other acid-related diseases(ARDs).In vitro experiments showed that the capacity of the active compound is a proton pump inhibiting Lansoprazole 400 times, with respect to Na+, K+-ATPase in more than 500-fold selectivity.In the rabbit gastric tissue cultured, TAK-438 showed a higher Bilansuola azole enrichment rates and slower clearance rate, which it has a stronger and longer lasting efficacy acid-suppressing effect in vivo.The paper fully examines the basic drugs and the materials properties,with microcrystallinec elluose, croscarm ellose sodium, hydroxypropyl cellulose, mannitol,magnesium stearate as auxiliary materials,the formulation was optimized by screening of single factor investigation and factors.The experimental results show that the pescription of the optimized design is reasonable,the technology is stable,inter assay reproducibility was good.For the control of vonoprazan fumarate accdording to the quality,characteristics and physicochemical properties of vonoprazan fumarate tablets, established the detection method of vonoprazan fumarate tablets release,content,related substance.The results show the method has high specificity,good precision,high accuracy,and can effectively control the quality of products,provides the bacis for formulation the quality standard of the preparation.The reference drug stability test guide liner equirements,with appearance,dissolution,content,related substances and other projects as the indexes,the vonoprazan fumarate tables were influence factors test,accelerated test and long-term test.The results from the visible,each index vonoprazan fumaratetables in the during the experiment were not changed,to prove the stability of the formulation is good.Its preparation process and quality standard of reseach,the method is feasible and resonable.