Quality Evaluation Of Esomeprazole Magnesium Enteric-coated Tablets

Esomeprazole magnesium,a proton pump inhibitor,is used for the treatment of acid-related diseases.As the first single optical isomer,in 2003,esomeprazole magnesium enteric-coated tablets were approved in China(Trade name: Nexium).The quality of esomeprazole magnesium enteric-coated tablets was verified in this thesis.The main conclusions are as follows:The chromatographic conditions for the measurement of related substances: column: Microspher C18(4.6 mm×100 mm,3?m);mobile phase A: water-phosphate buffer at pH7.6(per 1000 mL contained 0.0052 mol sodium dihydrogen phosphate and 0.0135 mol disodium phosphate)-acetonitrile(80:10:10);mobile phase B: acetonitrile-phosphate buffer at pH 7.6-water(80:1:19);injection volume: 20 ?L;column temperature: 35?;detection wavelength: 302 nm;flow rate: 1 mL/min.Results showed that the separation degrees of esomerprazole peak and related impuritie D peak were all greater than 2.5.Blank pharmaceutic adjuvants did not interfere with the assay of the related substances.The calibration curves for esomeprazole magnesium and its related substances were good in linearity.This method is simple,sensitive and reproducible.Thus,it is applicable for the quality control of esomeprazole magnesium enteric-coated tablets and its related substances.The chromatographic conditions for the measurement of content and dissolution curve: column: Microspher C18(4.6 mm×100 mm,3?m);mobile phase: acetonitrile-phosphate buffer at pH7.3(per 1000 mL contained 0.0105 mol sodium dihydrogen phosphate and 0.0300 mol disodium phosphate)–water(35:50:15);detection wavelength: 302 nm;injection volume: 20 ?L;flow rate: 1 m L/min;column temperature: 40?.The main peak retention time is greater than 3.5 minutes.The content and dissolution of esomeprazole magnesium enteric-coated tablets can be accurately measured through this method.The chromatographic conditions for isomer: mobile phase: acetonitrile-phosphate buffer at pH6.0(per 1000 mL contained 0.0137 mol sodium phosphate and 0.0551 mol disodium phosphate)–water(35:50:15);column: CHIRALAPK? AGP(100×4 mm,5?m);detection wavelength: 302 nm;injection volume: 20 ?L;flow rate: 0.6 mL/min;column temperature: 25?.This method is simple,accurate,with well specificity.The content of R-omeprazole can be accurately determined by this method.Finally,the stability of esomeprazole magnesium enteric-coated tablets was investigated.According to appearances,dissolution,content related substance,the influencing factors and accelerated test of six months were carried out to investigate the stability of esomeprazole magnesium enteric-coated tablets.The results showed that esomeprazole magnesium enteric-coated tablets was unstable at a high temperature,high humidity,which suggested that the tablets should be stored at a dry place and avoided contact with high temperature environments.The results of accelerated test showed that the reference listed drug and self-made tablets had the same changing trends in content,related substances and dissolution.The quality of self-made tablets with good stability meets the requirements of Chinese Pharmacopoeia.