Preparation Of Esomeprazole Magnesium Delayed-release Capsules

Esomeprazole,a new proton pump inhibitor,is the S-isomer of omeprazole.It is widely used for the treatment of gastric acid related diseases.The enteric-coated capsules of esomeprazole magnesium is a kind of pellets capsules.A systematic study of related formulation and preparation was carried out in this thesis.This study aims to prepare esomeprazole magnesium enteric-coated pellets capsules,and determined its quality and the stability.Firstly,the in vitro analysis methods of esomeprazole magnesium enteric-coated pellets capsules were introduced in this thesis.The preformulation study and brand drug analysis were also conducted.Sceondly,both fluidized bed and centrifugation pelletizing coating technology were used to prepare esomeprazole magnesium enteric-coated pellets.All enteric-coated pellets were prepared from blank pill core,and related process parameters were determined according to coating efficiency and the controllability of coating process.The isolation layer was added to ensure the stability of the esomeprazole magnesium.The optimal formulation and weight gain of isolation layer and enteric layer were determined following formulation screening through single factor analysis on the stability,acid resistance and dissolution.Finally,the quality research and stability investigation were carried out via corresponding in vitro analysis methods.Enteric-coated pellets with good roundness,uniform size and small differences among batches were preparaed by two methods.The formulation had a good reproducibility;The quality of esomeprazole magnesium enteric-coated pellets capsules was evaluated.The content,related substances and enantiomer of the optimized formulations were all complied with the requirements.In the stability test,the variation tendencies of properties,content,related substances and dissolution between brand and self-made samples were basically consistent which indicates a good stability of self-made capsules.Above results demonstrate that self-made enteric-coated pellets capsules are good in quality and stability and coincide with the brand preparation.These results also provide references for the industrialization of esomeprazole magnesium enteric-coated capsules.