Study On The Taste-masking Granules

For the drug taste-masking,primarily by altering the forms of the preparation and the process conditions to achieve the purpose of masking the bitter taste of drugs.Great progress of the drug taste masking techniques have been made in recent years,and there are a variety of taste-masking technologies,which are mainly according to the following mechanisms:(1)adding flavoring agents,the bitterness of many drugs are unacceptable,by adding specific flavors to achieve taste-masking purposes.(2)delay or prevent the release of the drug in the mouth,to prevent the bitter taste of the drug agent combining with the receptor in the oral mucosa,leave the drug apart from the taste buds,this can effectively cut off the signal conduction of the object and reach the purposes of masking bitterness,the main methods including coating method,ion exchange resin adsorption,clathrate method,microcapsules or microspheres method etc..Various taste masking technologies,and today’s taste masking methods commonly used in drugs were reviewed,and with clarithromycin as a model drug,methods of drug taste masking were studied in this thesis.Clarithromycin is a derivative of erythromycin,its current preparation in the form of capsules,granules,dispersible tablets,sustained-release tablets,injections and dry suspension,it’s very bitter in the oral cavity and with long duration,which greatly reduces patient compliance,and limits its application in the clinical practice.Therefore,the taste-masking of clarithromycin becomes very important.Taste masking methods used in this study were mainly by preparing resin skeleton clarithromycin granules to obtain taste masking agents,the contents of the study include :(1)Technology study on the clarithromycin taste masking agents.A preliminary assessment of the four options were made through primaries taste masking scheme,including taste,dissolution,water and other evaluations,and finally the resin skeleton method was chosen to prepare clarithromycin taste masking granules,and then PEG4000 was selected as the porogen by single factor test,the amount of PEG4000,resin and sodium bicarbonate,and the optimal prescription were determined by orthogonal experiment.According to the technology and formulation,taste masking effect of the final products is obvious,and the dissolution rate can reach 79.28%,and the method is simple in operation and has good repeatability.(2)Quality study on the clarithromycin granules.A HPLC method for determination of related substances and content of clarithromycin granules methods,UV-spectrophotometric determination of dissolution rate of clarithromycin granules were estabilished.The destructive tests showed that the method can effectively separate impurities,and accurately determine the related substances of clarithromycin granules;At the same time,this method can effectively determine the content of clarithromycin granules which was verified by repetitive testing,durability testing,precision testing etc.,the average recovery rate was up 99.72%;UV-spectrophotometric determination of dissolution rate of clarithromycin granules were verified by repetitive tests and precision test and other tests,results proved that the method can determine the dissolution of clarithromycin granules accurately.(3)Effect factors testing of clarithromycin granules.In the high-humidity test,related substances and moisture of clarithromycin significantly increased.So we recommend using a good moisture resistance of plastic packaging.Through these studies,we have a better understanding on the drug taste masking techniques,and has laid a good foundation for the further research on clarithromycin taste masking technology.