Esomeprazole sodium composition used for injection and its preparation method

Abstract

The invention provides an Esomeprazole sodium composition used for injection and its preparation method, the Esomeprazole sodium composition is prepared by the following steps: 1) liquid preparation: selecting esomeprazole sodium and ethylenediamine tetraacetic acid or ethylenediamine tetraacetic acid salt as raw materials, wherein the weight ratio of esomeprazole sodium to ethylenediamine tetraacetic acid or ethylenediamine tetraacetic acid salt is 1:0.01-0.1, weighting a proper amount of raw materials into a preparation tank, and adding water for injection to the weight of 23.47-234.7 timesof esomeprazole sodium, stirring and uniformly mixing the solution, adjusting the pH value of 10.0-12.5; 2) activated carbon finishing; 3) adsorbing; 4) sterile filtrating and split charging; 5) vacuum freeze-drying to obtain the esomeprazole sodium composition used for injection. The esomeprazole sodium composition used for injection and the preparation method are capable of ensuring the heat source, visible foreign matter and insoluble particulate to accord with the requirements of the injection for the injection preparations such as esomeprazole sodium preparation liquid with high pH value.

Description

technical field [0001] The invention relates to an esomeprazole sodium composition for injection and a preparation method thereof, belonging to the technical field of medicine preparation. Background technique [0002] The chemical name of esomeprazole sodium is 5-methoxy-2-((S)-((4-methoxy-3,5-dimethyl-2-pyridyl)methyl)sulfinyl- 1H-benzimidazole sodium, the structural formula is [0003] [0004] Esomeprazole sodium is clinically used for the treatment of gastroesophageal reflux disease (GERD)-erosive reflux esophagitis. Long-term maintenance treatment for cured patients with esophagitis to prevent recurrence. Symptom control in gastroesophageal reflux disease (GERD). Used in combination with appropriate antibacterial therapy to eradicate H. pylori and - heal duodenal ulcers associated with H. pylori infection - prevent recurrence of H. pylori-associated peptic ulcers. [0005] Esomeprazole sodium is unstable in an acidic environment. On the one hand, esomeprazole so...

AI Technical Summary

Problems solved by technology

However, the use of activated carbon to adsorb heat sources in esomeprazole sodium injection also has its defects. Activated carbon is obtained by simple treatment after burning wood, and there are inevitably a large amount of impurities. In the production process of esomeprazole sodium injection, Activated carbon also introduces new impurities while adsorbing heat sources and colored substances, resulting in a significant reduction in the control level of visible foreign matter and insoluble particles. This situation becomes more obvious as the pH value of the prepared solution of esomeprazole sodium increases. The higher the pH value of the prepared solution of Someprazole Sodium, the more impurities released by the activated carbon during the decarbonization process. These impurities cannot be removed in the 0.22 μm filter filtration process, so they remain in the final preparation, making the finished preparation visible. Insoluble particles failed to pass the inspection, resulting in the scrapping of the entire batch of products

In addition, the quality difference between batches of activated carbon will also significantly affect the quality of the product after decarbonization. Different batches of activated carbon have different levels of impurities released during decarbonization, and these effects are unpredictable. The final quality of the product brings great hidden dangers

[0007] However, none of the existing technologies has any suggestions for improving the above defects: Chinese patent CN200380101430.2 discloses a kind of preparation of omeprazole or esomeprazole by using pyridine methanol as raw material via picolyl chloride and pimeprazole The method does not solve the above technical defects

Chinese patent CN200810004014.5 discloses a method for preparing omeprazole or esomeprazole by using pyridinemethanol as raw material via picolyl chloride and pimeprazole, which is characterized in that the whole reaction process is carried out without separation or purification In the case of intermediates, it does not solve the above technical defects

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