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Pharmaceutical composition containing esomeprazole sodium, and preparation method thereof

A technology of esomeprazole sodium and its composition, which is applied in the field of esomeprazole sodium pharmaceutical composition and its preparation, and achieves the effects of high yield, simple operation and low cost

Active Publication Date: 2012-12-12
CHENGDU GUOHONG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The applicant of the present invention finds in actual test, this method will consume a large amount of industrial raw materials acetonitrile, and the esomeprazole sodium final product yield that this method refines is lower than 20%, in the product of refining gained repeatedly , the content of sulfone is still greater than 03%

Method used

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  • Pharmaceutical composition containing esomeprazole sodium, and preparation method thereof
  • Pharmaceutical composition containing esomeprazole sodium, and preparation method thereof
  • Pharmaceutical composition containing esomeprazole sodium, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0101] Put 7.0g (0.212mol) of omemersulfide and 46ml of ethyl acetate into the reaction flask, start stirring, and add in sequence 0.145g of purified water, 4.48g of D-(-)diethyl tartrate, 3.12g of VI isopropyl titanate g. Raise the temperature to 55°C, react for 1 hour, cool down to 20°C, add 1.9ml of triethylamine, then dropwise add 4.38mL of 70% cumene hydroperoxide, and react for 2 hours. After the reaction, separate the organic phase, combine the water layer, add 6mL methyl isobutyl ketone to the water layer, cool in an ice-water bath, add glacial acetic acid under vigorous stirring to adjust the pH to 6.5-7.5, separate the organic layer, and reuse the water layer Extract once with 6 mL of methyl isobutyl ketone, combine the organic layers, and wash once with 6 mL of saturated brine to obtain 25 ml of a methyl isobutyl ketone solution of esomeprazole.

[0102] Add the methyl isobutyl ketone solution of esomeprazole into the reaction flask, start stirring, add methanol so...

Embodiment 2

[0105] 7.0 g (0.212 mol) of omemersulfide was put into the reaction flask, and 2.6 g of crude esomeprazole sodium was prepared according to the method of Example 1.

[0106] Put the crude product of esomeprazole sodium into the reaction kettle, add the mixed solution of methanol and acetonitrile (methanol 1.8mL, acetonitrile 3.6mL), stir at room temperature until completely dissolved. After filtration, 18ml of acetonitrile was added to the filtrate. While stirring, the temperature was maintained at 30°C, and crystallization was carried out for 30 hours. Put the material into the filter for suction filtration, wash the filter cake with acetonitrile after pumping dry, and pump dry again. Obtained 1.76g of esomeprazole sodium refined product (refining yield: 67.6%), which contains 5-(-)-methoxy-2-[[(4-methoxy-3,5-di Methyl-2-pyridyl)methyl]sulfonyl]-1H-benzimidazole sodium 0.07%, except 5-(-)-methoxy-2-[[(4-methoxy-3,5- The maximum amount of single impurity other than dimethyl...

Embodiment 3

[0108]Put 7.0 g (0.212 mol) of omeprazole into the reaction flask, and prepare 2.7 g of crude esomeprazole sodium according to the method of Example 1.

[0109] Put the crude product of esomeprazole sodium into the reaction kettle, add a mixed solution of methanol and acetonitrile (2.2 mL of methanol, 2.2 mL of acetonitrile), and stir at room temperature until completely dissolved. After filtration, 13.2 ml of acetonitrile was added to the filtrate. The temperature was maintained at 0°C under stirring, and crystallization was carried out for 18 hours. Put the material into the filter for suction filtration, wash the filter cake with acetonitrile after pumping dry, and pump dry again. Obtain 1.5g of esomeprazole sodium refined product (refining yield: 55.5%), this refined product contains 5-(-)-methoxy-2-[[(4-methoxy-3,5-di Methyl-2-pyridyl)methyl]sulfonyl]-1H-benzimidazole sodium 0.12%, except 5-(-)-methoxy-2-[[(4-methoxy-3,5- The maximum amount of single impurity other tha...

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Abstract

The invention relates to a pharmaceutical composition containing esomeprazole sodium, and a preparation method thereof. Among the active components of the pharmaceutical composition provided by the invention, the amount of 5-(-)-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]sulfonyl]-1H-benzimidazole sodium is lower than 0.3%. The invention also provides a method for producing a target product through a salt forming reaction and recrystallization of esomeprazole. With the controlling over reaction conditions and reaction solvents, advantages such as simple process, low cost, high yield, and suitability for industrialized productions are realized, and the esomeprazole sodium provided by the invention can be obtained. The invention also provides prescriptions and a preparation method of the pharmaceutical composition.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a pharmaceutical composition of esomeprazole sodium and a preparation method thereof. Background technique [0002] The chemical name of Esomeprazole sodium is (S)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl] Sulfinyl-1H-benzimidazole) sodium. Esomeprazole sodium for injection is used as an alternative therapy for gastroesophageal reflux disease when oral therapy is not applicable. On March 31, 2005, FDA approved AstraZeneca's application for esomeprazole sodium for injection. In 2007, China Food and Drug Administration approved AstraZeneca's esomeprazole sodium freeze-dried powder The import of needles, whose trade name is Nexium, which is packaged in a 5ml vial, is used by adding 5ml of 0.9% sodium chloride solution to the vial for intravenous injection. Nexium’s prescription contains the main drug Exome In addition to prazole sodium, it also contains auxiliary ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4439A61K9/19A61K47/10A61K47/18A61P1/04C07D401/12
Inventor 刘玺王兵郭礼新
Owner CHENGDU GUOHONG PHARMA
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