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Esomeprazole sodium hemihydrate

A technology of esomeprazole sodium and water compound, applied in the field of medicine, can solve the problems of high total amount of impurities, large number of esomeprazole sodium impurities, low optical purity and the like

Active Publication Date: 2012-01-18
TIANJIN HANRUI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] In the research process, repeating the method of the above-mentioned patent documents, the obtained esomeprazole sodium has a large number of impurities, a high total amount of impurities, and low optical purity.

Method used

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  • Esomeprazole sodium hemihydrate
  • Esomeprazole sodium hemihydrate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Add 60 grams of esomeprazole sodium and 300 milliliters of water into a 500ml reaction bottle equipped with stirring, a thermometer and a condenser, add 0.5 grams of dimethylformamide (DMF) to the above aqueous solution, stir for 30 minutes, and filter , the filtrate was cooled to 12°C and set aside.

[0059] Cool 1150ml of acetonitrile-methyl ethyl ketone = 5:5 mixture to 13°C, add the above standby solution while stirring, keep warm for 18 hours, crystals precipitate, filter, and dry to obtain 53.3 grams of white crystals. Measured 3 times by Karl Fischer method, get the average value, contain 2.40% (weight percent) moisture. Purity 99.9% (HPLC normalization method), optical purity 99.96% ee (chiral HPLC).

[0060] Elemental Analysis Results:

[0061] Measured value (calculated value), C:54.28(54.25),H:5.16(5.09),N:11.21(11.16),

[0062] S: 8.59 (8.52), Na: 6.19 (6.11).

[0063] The X-ray diffraction pattern of the crystal is shown in figure 1 . Instrument model...

Embodiment 2

[0066] Injection containing esomeprazole sodium hemihydrate

[0067] Prescription: Esomeprazole Sodium Hemihydrate (20g as anhydrous substance), 100g mannitol, 140g lactose, 500ml water for injection, made into 1000 sticks.

[0068] Process: Take esomeprazole sodium hemihydrate, mannitol, lactose, and water for injection and stir to dissolve, then add 4g of activated carbon, stir at room temperature for 10 minutes, filter out the activated carbon, and use a microporous membrane to filter bacteria. Pack 1000 tubes, pre-freeze for 3 hours, freeze-dry under reduced pressure for 20 hours, then warm to room temperature, and seal.

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Abstract

The invention belongs to the technical field of medicine, and particularly relates to an esomeprazole sodium hemihydrate and a preparation method thereof; the esomeprazole sodium of the invention comprises a hemihydrate, and has the following advantages that: the chemical purity is 99.9%; the maximal impurity content is less than one thousandth; the optical purity is up to 99.96%ee; and the stability is good. The invention also relates to an application of a composition of the hydrate in the preparation of medicaments for treating stomach burning sensation caused by non-erosive gastroesophageal reflux, and erosive esophagitis.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to esomeprazole sodium hemihydrate and a preparation method thereof. The invention also relates to the use of the hydrate composition to manufacture non-erosive gastroesophageal reflux for treating gastroesophageal reflux disease The application of drugs for the burning sensation in the stomach caused by erosive esophagitis. Background technique [0002] For the drug treatment of acid-related diseases, the first H2 receptor antagonist cimetidine was first introduced in the 1970s, and proton pump inhibitors were discovered in the 1980s, which significantly changed the acid-related diseases. The clinical efficacy of diseases such as peptic ulcer (including stress ulcer), gastroesophageal reflux disease (including reflux esophagitis), gastrinoma, and some functional dyspepsia has made the control rate of such diseases reach had an effect that had never been seen before. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12A61K31/4439A61P1/04
Inventor 严洁黄欣
Owner TIANJIN HANRUI PHARMA
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