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Esomeprazole sodium and lyophilized preparation comprising same

A technology of esomeprazole sodium and sodium hydroxide, which is applied in the field of medicine, can solve problems such as the decline in the quality of life of patients, and achieve the effects of drug safety, easy preparation process, and high preparation precision

Inactive Publication Date: 2019-03-12
SHANXI PUDE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] At present, with the social development of our country, environmental changes, changes in population structure and people's lifestyles, the incidence of peptic ulcer mainly caused by factors such as smoking, drinking, emotional stress, and drug stimulation has gradually increased, becoming a common disease and a frequent disease. morbidity, causing great pain to the patient, leading to a decline in the quality of life of the patient

Method used

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  • Esomeprazole sodium and lyophilized preparation comprising same
  • Esomeprazole sodium and lyophilized preparation comprising same
  • Esomeprazole sodium and lyophilized preparation comprising same

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Embodiment Construction

[0032] The principles and features of the present invention will be described below with reference to the embodiments. The examples cited are only used to explain the present invention, and are not used to limit the scope of the present invention.

[0033] The esomeprazole of the present invention can be prepared by the chemical reaction equation shown below, and includes the following steps:

[0034] Step 1: Synthesis of intermediate: Add 3.76 kg of 2-chloromethyl-3,5-dimethyl-4-methoxypyridine hydrochloride and 2-mercapto-5-methoxybenzimidazole to the reactor 3.0kg, 37L methanol, stirred to dissolve, add 0.7kg sodium hydroxide and 2.7L water solution within 15 minutes, the clear solution became turbid. After heating to reflux, a solution of 0.7 kg of sodium hydroxide and 2.7 L of water was added dropwise within about 15 minutes. After the addition is completed, reflux is maintained at 55-65°C for 2 hours, and TLC is finally controlled (developing solvent: dichloromethane / methano...

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Abstract

The invention provides esomeprazole sodium and a lyophilized preparation comprising the same. A preparation method of esomeprazole sodium includes following steps: 1), synthesizing an intermediate; 2), synthesizing esomeprazole sodium; 3), roughly preparing esomeprazole sodium; 4), finely preparing esomeprazole sodium. Esomeprazole sodium prepared by the method is higher in preparation accuracy and safer to use; the preparation process is easier to control, and step decomposition brings convenience to quality control of middle steps, so that ensuring of preparation accuracy of esomeprazole sodium is facilitated, and drug prepared from esomeprazole sodium is safer.

Description

Technical field [0001] The invention relates to the field of medicine, in particular to an esomeprazole sodium and a freeze-dried preparation containing the same. Background technique [0002] Esomeprazole is the s-optical isomer of omeprazole. It is the world's first isomer proton pump inhibitor, which reduces gastric acid secretion by specifically inhibiting the proton pump of gastric parietal cells. It has been confirmed by a large number of clinical experiments and drug studies that it maintains intragastric pH> 4 has a longer time, higher acid suppression efficiency, better efficacy than the previous two generations of proton pump inhibitors, and small individual differences. As a new generation of proton pump inhibitors, it is now widely used in clinical treatment of many acid-related diseases. Proton pump inhibitors are the first choice for the treatment of acid-related diseases such as digestive ulcers and gastroesophageal reflux disease. At present, there are five k...

Claims

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Application Information

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IPC IPC(8): C07D401/12A61K31/4439A61K9/19A61P1/04
CPCA61K9/19C07D401/12
Inventor 李立忠王勇吴志苏志强昝建强李海娇何海忠王佳佳
Owner SHANXI PUDE PHARMA CO LTD
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