Studies For Esomeprazole Magnesium Enteric-coated Tablets

Esomeprazole is a proton pump inhibitor.It is widely used for the treatment of acid related diseases.The enteric-coated tablet of esomeprazole magnesium is a kind of pellets tablet.The formulation and preparation technology as well as the quality of this pellets tablet were studied in this thesis.The analysis on the brand preparation of esomeprazole magnesium enteric-coated tablet was firstly carried out.The physical property,prescription,stability,acid tolerance,release,content and content uniformity were included.Based on the analysis,the properties of the brand preparation were understood and these results provided the basis for the study of self-made products.For the small-scale test,the formulation and preparation technology of pellets were investigated.The formulation of all intermediate pellets was determined according to the state of mixed suspension of each layer,the phenomenon in the process of coating and the stability of pellets.According to the fluidized state of coating process,the preparation technology of all intermediate pellets was established via bottom spray fluid bed coating technology following adjusting related parameters.Finally,direct compression method was used for the preparation process.The tablet formulation included fillers,lubricants,adhesives and disintegrating agents.By using single factor experiment,the amount of compression adjuvant was determined according to the hardness and the disintegration time.For the scale up test,because all indexes of the samples prepared according to the formulation in the small-scale test were qualified,the preparation technology become the main research object.The preparation technology of all intermediate pellets was determined according to the fluidized state of pellets in the fluidized bed.On the basis of the mixing uniformity,the blending technology of enteric-coated pellets and excipients was ascertained.In the light of the content uniformity,disintegration time and hardness,the compression technology was established.Finally,a quality assessment for the samples of the scale up test were carried out in this thesis.The morphology of pellets was characterized by scanning electron microscopy and the results indicate that the surface of enteric-coated pellets is integrated and the internal structure of self-made pellets is similar to that of brand pellets.The content of all intermediate pellets,the content uniformity,acid tolerance and dissolution curve of self-made tablet and also the samples in the stability test were measured via High performance liquid chromatography.Results showed that the content detection value of all intermediate pellets is close to the formulation-based value,the content uniformity and acid tolerance are complied with the requirements,the dissolution curve of self-made tablet is consistent with that of brand preparation,the variation tendencies of related substances,isomers,appearance,content and dissolution of the samples in the stability test are similar to those of brand drug.