Study On The Prescription Technology And Quality Of Azilsartan Tablets

Objective:Azilsartan Tablets,which is mainly used to treat mild and moderate hypertension,is a kind of angiotensin II receptor antagonist,and it is more effective,even more,it has the same safety and tolerability,so it would be the first choice against hypertension.But the product isn't available in China,and with more and more hypertension patients now,there is a huge potential market in China.In order to provide the foundation for preclinical and clinical research of Azilsartan Tablets,the author has studied on the synthesis of raw materials,the formulation process and the draft of quality standard.Under the draft's guidance,we can get the same or even better quality new product.Methods:(1)Studies on the formulation processThis subject based on the patent of Takeda Pharmaceutical Co Ltd Pharmaceutical composition(No.200780037942.5)and instructions of AZILVA Tablets,the author observes the main index of the tablet,eg,appearance,hardness,disintegration time and stripping phenomenon,and then determines a better formulation and preparation procedure on the basis of test results.(2)Quality researchReferring to the pharmacopoeias,review principle,the relevant requirements of the international CTD and references,the author studied the quality of Azilsartan Tablets,including characteristics,the design of identification methods of UV and HPLC and the establishing of methods of inspection item about dissolution rate,content uniformity,and the building of measuring methods,and then validated a methodology to the dissolution rate,related substances and content determination,including specificity,linear,instrument precision,stability and recovery rate.On the basis of that,the quality standard draft was established.The system was used to test two bath of products from small scale experiment,three baths of products from pilot scale experiment and some commercially available products.(3)StabilityOn the foundation of the quality standard in this study,according to the domestic and foreign review principle,the author have studied the stability of Azilsartan Tablets,including stress test,accelerated test and long-run test.Results1 Studies on the formulation process(1)Taking appearance properties,weight differential,hardness,disintegration time and angle of repose,friability,dissolution rate and content determination into consideration,studying on the formulation process,the results show that recipe 12 is the best,that is starch(15mg),lactose(55mg),microcrystalline cellulose(20mg),adhesive(High substitution hydroxypropyl cellulose:1.5mg),disintegrating agent(Low substitution hydroxypropyl cellulose:10mg),polyethylene glycol 6000(4mg),lubricant(0.2mg magnesium stearate and lmg talcum powder).(2)According to the appearance properties,dissolution rate and content determination,the formulation process was established,that is granularity of raw materials<150 mesh,the whole grain sieve of 26 mesh,moisture content of pellet<3%,premixed time of 8 minutes,total mixed time of 20 minutes,tablet hardness in the range of 2.5 to 7 kg.2 Establish the quality standardEstablished a detection method for some key projects,for example,the dissolution rate,related substances and content determinationCompleted a whole quality standard draft of Azilsartan Tablets according to the comparison and validation of all the test parametersThe quality standard draft has through the investigation of methodology,which has the advantages of good repeatability,specificity,high sensitivity,good system applicability.3 Stabilitythe good results of stress test,accelerated test and long-run test to the two bath of products from small scale experiment,three bath of products from pilot scale experiment show that the product has stable quality.ConclusionThis study has developed Azilsartan Tablets successfully,which is similar to the original quality,more stable and effective.At the time,a whole quality standard draft of Azilsartan Tablets completed,which has the advantages of good repeatability,specificity,high sensitivity,good system applicability.The products from small scale experiment and pilot scale experiment have checked by the draft,the result proves it has the similar safety and effectiveness to the original products.