Compound for the treatment of gastrointestinal disease

A technology of sesquihydrate and pantoprazole sodium, which is applied in the field of compounds for the treatment of gastrointestinal diseases, can solve the problems of crystal form description, poor chemical stability and wet stability, instability, etc., and achieve good stability, containing The effect of stable water volume and low hygroscopicity

Active Publication Date: 2011-09-28
SHANDONG NEWTIME PHARMA
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  • Abstract
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  • Claims
  • Application Information

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Problems solved by technology

[0009] Chinese patent application 02109182 discloses a salt of chiral pantoprazole and a preparation method, and the preparation of its S-pantoprazole sodium is to dissolve S pantoprazole in an organic solvent and then add an aqueous solution of sodium hydroxide or sodium alkoxide After stirring, it was cooled and crystallized to obtain its monohydrate, but its crystal form was not described
[0011] S-pantoprazole sodium or its hydrate described in the prior art are all unstable solids, and its chemical stability and wet stability are all poor

Method used

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  • Compound for the treatment of gastrointestinal disease
  • Compound for the treatment of gastrointestinal disease
  • Compound for the treatment of gastrointestinal disease

Examples

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Embodiment 1

[0031] S-pantoprazole 17g, 340ml aqueous solution that is dissolved with 2.2gNaOH is put into the reaction flask, stir at room temperature until the material is completely dissolved, filter the feed liquid, and distill under reduced pressure at a temperature of 35°C. Stop the distillation when there is solid precipitation in the feed liquid, and place it in a refrigerator at 0° C. for crystallization for 48 hours. Filter the feed liquid, wash the filter cake with a small amount of cooled water, and dry at 50° C. under normal pressure for 6 hours to obtain 17 g of S-pantoprazole sodium di-sesquihydrate solid, with a yield of 85%. The moisture content determined by the Fischer method was 10.1%, and the related substances determined by HPLC were 99.8%.

Embodiment 2

[0033]17 g of S-pantoprazole, 34 ml of aqueous solution containing 5.2 g of NaOH, and 34 ml of methanol were put into a reaction flask, stirred at a temperature of 5° C. until the material was completely dissolved, filtered, and distilled under reduced pressure at a temperature of 40° C. Stop the distillation when there is solid precipitation in the feed liquid, and place it in a refrigerator at 10° C. for 24 hours for crystallization. Filter the feed liquid, wash the filter cake with a small amount of cooled water, and dry at 40° C. under normal pressure for 10 hours to obtain 18 g of S-pantoprazole sodium di-sesquihydrate solid, with a yield of 90%. The moisture content determined by the Fischer method was 10.2%, and the related substances determined by HPLC were 99.8%.

Embodiment 3

[0035] 17 g of S-pantoprazole, 85 ml of aqueous solution with 1.8 g of NaOH, and 25 ml of ethanol were put into a reaction flask, stirred at a temperature of 25° C. until the material was completely dissolved, filtered the feed liquid, and distilled under reduced pressure at a temperature of 30° C. of the feed liquid. Stop the distillation when there is solid precipitation in the feed liquid, and place it in a refrigerator at 5° C. for 8 hours for crystallization. Filter the feed liquid, wash the filter cake with a small amount of cooled water, and dry at 40° C. under normal pressure for 8 hours to obtain 18 g of S-pantoprazole sodium di-sesquihydrate solid, with a yield of 90%. The moisture content determined by Fischer's method was 10.5%, and the related substances determined by HPLC were 99.9%.

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Abstract

The invention provides a compound for the treatment of gastrointestinal diseases. The crystallization of the compound has the characteristics of a stable crystalline structure, small hygroscopicity and stable water content. Under normal preservation condition and in mechanical pulverization which might be included in the preparation process, the water content and the crystalline structure show good stability.

Description

technical field [0001] The present invention relates to the active compound (S)-5-difluoromethoxy-2-[(3,4-dimethoxy-2-pyridyl)methylsulfinyl]-1H-benzimidazole sodium, general A new bisesquihydrate named S-pantoprazole sodium, its crystals and its preparation method. technical background [0002] S-pantoprazole sodium has the function of inhibiting gastric acid secretion and is usually used as an antiulcer agent. The structural formula is: [0003] [0004] Pantoprazole is a racemic mixture of two single enantiomers, R and S, and its salts have the corresponding configurations. US Patent No. 588535 discloses that S-pantoprazole sodium has a stronger gastric acid secretion inhibitory effect than racemic pantoprazole sodium and R-pantoprazole sodium. [0005] The preparation method of the single enantiomer of pantoprazole mainly includes two approaches of precursor thioether chiral oxidation and racemate resolution. WO9617076 and WO9617077 etc. introduced the chiral oxid...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12A61K31/4439A61P1/00A61P1/04
Inventor 赵志全
Owner SHANDONG NEWTIME PHARMA
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