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Novel esomeprazole strontium compound, and pharmaceutical composition and application thereof

A technology of esomeprazole strontium and meprazole strontium is applied in the field of medicine and achieves the effects of being convenient for storage and transportation, reducing manufacturing costs and costs, and being easy to prepare

Pending Publication Date: 2019-12-03
刘力
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The literature has reported crystalline S-omeprazole strontium tetrahydrate and S-omeprazole strontium anhydrate (document 15: Chinese patent, CN101296921A), and the U.S. FDA has approved the listing of esomeprazole strontium 4 hydrate; however , Judging from the current actual situation, there are some problems in the stability or preparation of esomeprazole strontium 4 hydrate, and continuous innovation is still needed from the pharmaceutical point of view
[0007] Up to now, there is no published bibliographical report at home and abroad with better stability or easier to prepare novel esomeprazole strontium compounds of the present invention, such as esomeprazole strontium α-type, β-type, κ-type new Molecular formula crystalline compounds, esomeprazole strontium ν-type crystalline compounds, esomeprazole strontium ω-type crystalline compounds, namely new esomeprazole strontium crystalline hydrates with different molecular formulas or different crystal forms and their Preparation method and use

Method used

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  • Novel esomeprazole strontium compound, and pharmaceutical composition and application thereof
  • Novel esomeprazole strontium compound, and pharmaceutical composition and application thereof
  • Novel esomeprazole strontium compound, and pharmaceutical composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0116] The preparation of embodiment 1 esomeprazole strontium 3 hydrate (ν type)

[0117] At room temperature, add 6.824g of esomeprazole sodium and 40ml of methanol to a 250ml flask, stir to dissolve, heat to about 40°C, then dropwise add about 16ml of methanol solution of 2.37g of strontium chloride hexahydrate, stir, about 10 A large amount of precipitates precipitated in about 12 minutes, continued to stir for about 12 minutes, took out the suction filter, washed a small amount of water and ethanol to remove the residual sodium chloride in the solid, and filtered the solid. Air-drying about 4h, obtain off-white solid 6.3g; HPLC: measure with two kinds of methods of content and related substance respectively, the main peak retention time of the HPLC of the product of this embodiment and esomeprazole or esomeprazole sodium reference substance main peak The HPLC retention time is consistent; Karl Fischer's method measures moisture to be 6.65%, thermal analysis: platform weigh...

Embodiment 2

[0118] The preparation of embodiment 2 esomeprazole strontium 3 hydrates (ν type)

[0119] At room temperature, add 6.91g of esomeprazole sodium and 40ml of methanol to a 250ml flask, stir to dissolve, add about 20ml of methanol solution of 2.38g of strontium chloride hexahydrate at about 40°C, stir to dissolve, stir, about After a large amount of white precipitate precipitated in about 10 minutes, continue to stir for 20 minutes, add about 2ml of water, continue to stir for 8 minutes, filter the object in the reaction bottle with suction, wash with a small amount of water and ethanol five times, and filter with suction, the obtained solid is diluted at about 46°C. Air-drying 5h, obtain off-white solid 6.2g; HPLC: measure with two kinds of methods of content and related substance respectively, the main peak retention time of its HPLC is consistent with the HPLC retention time of main peak of esomeprazole sodium reference substance; Moisture is 6.77%, thermal analysis: platform...

Embodiment 3

[0120] The preparation of embodiment 3 esomeprazole strontium 3.5 hydrate (ω type)

[0121] In a 500ml flask, add 13.8g of esomeprazole sodium (purity 99.9%), add 85ml of methanol, stir at about 40°C to dissolve, add 4.75g of strontium chloride hexahydrate, about 40ml of methanol solution, stir to dissolve, stir , A large amount of white precipitate precipitated in about 10 minutes, continue to stir for about 20 minutes, add about 10ml of water, continue to stir for about 10 minutes, suction filter the object in the reaction bottle, wash the solid with a small amount of water and ethanol to remove the residual sodium chloride in the solid, Suction filtration, the resulting solid was diluted and dried in a blast drying oven at about 30°C for 1h, and then dried at 45°C for about 2h to obtain 12.4g of off-white solid; HPLC: determined by two methods of content and related substances, the main peak of HPLC remained Time is consistent with the main peak retention time of esomeprazo...

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Abstract

The invention discloses alpha-type, beta-type, kappa-type, niu-type and omega-type compounds with a new molecular structure of esomeprazole strontium. The compounds have the characteristics of being more easily and quickly prepared with low energy consumption, and having less hygroscopicity, good storage stability, good accessibility and the like. The compounds are suitable for preparing medicinesor medicine compositions for treating diseases such as gastroesophageal reflux diseases, erosive reflux esophagitis, upper gastrointestinal hemorrhage, stress ulcer and duodenal ulcer of human beingsor animals, eradicating helicobacter pylori and Zollinger-Ellison syndrome, preventing recurrence of peptic ulcer related to helicobacter pylori, and preventing recurrence of cured esophagitis patients by long-time maintaining treatment, and adverse reactions in treatment are reduced.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular, it provides a new proton pump inhibitor esomeprazole strontium compound and a pharmaceutical composition thereof. Background technique [0002] Esomeprazole is an optical isomer proton pump inhibitor of omeprazole, mainly in the form of sodium and magnesium salts. It can inhibit the H+ / K+-ATPase near the acid oxyntic ducts of gastric parietal cells, and has a good acid-suppressing effect. Due to its metabolic advantages, esomeprazole has higher bioavailability and more consistent pharmacokinetics, Increase the drug reaching the proton pump, and has been widely used in the clinical treatment of gastroesophageal reflux disease, erosive reflux esophagitis, upper gastrointestinal bleeding, stress ulcer, duodenal ulcer, eradication of pyloric screw rod Helicobacter pylori-related peptic ulcer recurrence, long-term maintenance treatment to prevent recurrence of cured esophagitis patien...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12A61K31/4439A61P1/04A61P1/00A61P7/04A61P31/04
CPCC07D401/12A61P1/04A61P1/00A61P7/04A61P31/04A61K31/4439
Inventor 刘力
Owner 刘力
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