The Formulation Process Of Esmeprazole Magnesium Enteric-coated Tablets

Esmeprazole magnesium enteric-coated tablets,a kind of multi-unit pellet tablets,induce powerful long-lasting inhibition of gastric acid secretion.The pellet tablet technology which is susceptible to the external environment requires the pellets and excipients with special characteristics.Based on the preparation of esmeprazole magnesium enteric-coated pellets and reference preparation,we explored the formulation and process.Furthermore,the quality of tablets was evaluated to verify the prescription and process.Firstly,according to the prescription information of reference listed drug,the proportion of microcrystalline cellulose（MCC）,magnesium stearate（MS）,crosslinked polyvinylpyrrolidone（PVPP）and coating weight were investigated using the appearance,content uniformity,acid resistance,dissolution and hygroscopicity as indicators.The prescription was confirmed as:MCC 67.4%,MS 0.6%,PVPP 2%and enteric-coated pellets 30%.The coating weight was between 4%and 5%and the polishing weight was1.0%.Secondly,the mixing uniformity of materials,hardness of the tablets,content uniformity and hygroscopicity were used as indicators to determine the type of the mixer,speed,mixing time,fill level,tablet speed,the feed rate and the temperature during the coating process.Blending was carried out by a multi-dimensional mixer.Its speed was 30Hz and the range of mixing time was between 5 minutes and 10 minutes.The fill level was75%of machine capacity and the tablet speed was 20 000 tablets per hour.The feeding speed was 10 Hz and the coating temperature was from 45℃to 50℃.Finally,a comparative study on the quality of self-made esmeprazole magnesium enteric-coated tablets and reference preparation was carried out.The content uniformity and dissolution of the self-made product were in accordance with the reference preparations.The similarity factor f₂,of the dissolution curves in various media was more than 50.The changes in the stability test of the content,related substances,enantiomers,and dissolution,were consistent with the reference preparation.It illustrated that the formulation and process could ensure that the product quality met the requirements.