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Pharmaceutical compound for treating peptic ulcer and preparation method thereof

A technology for pharmaceutical compounds and peptic ulcers, applied in the field of medicine, can solve problems such as the lack of purification methods for vonoprazan fumarate, difficulty in balancing yield and purity, and difficulty in hydrate preparation. It is suitable for large-scale production, The preparation method is simple and easy to operate, and the effect of improving solubility

Inactive Publication Date: 2017-08-04
刘德鹏
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because there are many impurities in vonoprazan fumarate that are difficult to remove, and the prior art does not provide an efficient purification method for vonoprazan fumarate, it is difficult to balance yield and purity
The special physical and chemical properties of vonorazan fumarate bring great difficulties to the preparation of hydrate
The present invention has carried out a large number of tests on the existing literature technology and found that the vonoprazan fumarate prepared in the prior art is an anhydrous compound, which has problems such as poor solubility and low purity, which seriously affects the safety of people's medication. question

Method used

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  • Pharmaceutical compound for treating peptic ulcer and preparation method thereof
  • Pharmaceutical compound for treating peptic ulcer and preparation method thereof
  • Pharmaceutical compound for treating peptic ulcer and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Embodiment 1: Preparation of fumaric acid Vonola monohydrate

[0058] (1) Take 100g of vonoprazan fumaric acid crude product, add tetramethylethylenediamine / water (volume ratio: 25:1.0) mixed solution (700ml), stir (40 rpm) to dissolve for 1-2min, Activated carbon decolorization, suction filtration;

[0059] (2) Reduce the filtrate of step (1) to -2°C, add dropwise (1.0mL / min) 700ml of pre-cooled tetramethylethylenediamine, and continue to cool down (3°C per 10 minutes) to -10°C Crystallization;

[0060] (3) Insulate and stir until the crystallization is complete, grow the crystal for 2 hours, filter with suction, wash with water, and dry at 40°C to obtain a white crystalline powder.

[0061] The X-ray powder diffraction spectrogram that the prepared white crystalline powder uses Cu-Kα ray measurement to obtain is shown in figure 1 .

Embodiment 2

[0062] Embodiment 2: Preparation of fumaric acid Vonola monohydrate

[0063] (1) Take 100g of vonoprazan fumaric acid crude product, add tetramethylethylenediamine / water (volume ratio: 25:1.2) mixed solution (500ml), stir (50 rpm) to dissolve for 1-2min, Activated carbon decolorization, suction filtration;

[0064] (2) Reduce the filtrate of step (1) to -2°C, add dropwise (1.5mL / min) 250ml of pre-cooled tetramethylethylenediamine, and continue to cool down (the cooling rate is 2°C per 10 minutes) to -9°C Crystallization;

[0065] (3) Insulate and stir until the crystallization is complete, grow the crystal for 3 hours, filter with suction, wash with water, and dry at 50°C to obtain a white crystalline powder.

[0066] The X-ray powder diffraction spectrum obtained by measuring the prepared white crystalline powder using Cu-Kα rays is similar to that of Example 1.

Embodiment 3

[0067] Embodiment 3: Preparation of fumaric acid Vonola monohydrate

[0068] (1) Take 100g of vonoprazan fumaric acid crude product, add a mixed solution (600ml) of tetramethylethylenediamine / water (25:1.1 by volume), stir (30 rpm) and dissolve for 1-2min, Activated carbon decolorization, suction filtration;

[0069] (2) Reduce the filtrate of step (1) to -2°C, add dropwise (2.0mL / min) 480ml of pre-cooled tetramethylethylenediamine, and continue to cool down (3°C per 10 minutes) to -8°C Crystallization;

[0070] (3) Insulate and stir until the crystallization is complete, grow the crystal for 1 hour, filter with suction, wash with water, and dry at 45°C to obtain a white crystalline powder.

[0071] The X-ray powder diffraction spectrum obtained by measuring the prepared white crystalline powder using Cu-Kα rays is similar to that of Example 1.

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Abstract

The invention belongs to the technical field of medicines and discloses a pharmaceutical compound for treating peptic ulcer and a preparation method thereof. The invention in particular discloses a vonoprazan fumarate-hydrate and a preparation method thereof. The vonoprazan fumarate-hydrate is high in purity and good in stability, and has characteristic diffraction peaks at 3.21 degrees, 5.62 degrees, 6.53 degrees, 9.12 degrees, 14.43 degrees, 15.53 degrees, 18.61 degrees, 21.72 degrees, 24.61 degrees and 27.71 degrees in an X-ray powder diffraction pattern represented by 2theta+0.2 degrees. The X-ray powder diffraction pattern measured by using a Cu-Kalpha ray is as shown in a formula 1. Different with the prior art, through experiments, the solubleness of the vonoprazan fumarate-hydrate obtained by the invention is remarkably improved surprisingly. The invention also discloses the preparation method of the vonoprazan fumarate-hydrate. The preparation method is simple and easy to operate, mild in reaction condition and suitable for large-scaled production. A composition troche prepared from the vonoprazan fumarate-hydrate provided by the invention is remarkably improved in dissolution rate and stability, and is quite suitable for clinical application.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a medicinal compound for treating peptic ulcer and a preparation method thereof, in particular to vonoprazan fumarate monohydrate and a preparation method thereof. Background technique [0002] Vonoprazan fumarate, chemical name 1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylformazan Amine fumarate, its molecular formula is: C 17 h 16 FN 3 o 2 S·C 4 h 4 o 4 , molecular weight: 461.46, chemical structure as shown in formula I. Vonoprazan fumarate is a new type of proton pump inhibitor, which can be used as a therapeutic drug for acid secretion inhibitors, tumor diseases or autoimmune diseases. As proton pump inhibitors such as omeprazole can effectively inhibit gastric acid secretion, but the instability in acidic conditions and the effect caused by metabolic enzyme polymorphisms and drug interactions are scattered. Excellent stability under certain...

Claims

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Application Information

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IPC IPC(8): C07D401/12A61K31/4439A61K9/20A61P1/04A61P35/00A61P37/06
CPCC07D401/12A61K9/2004C07B2200/13
Inventor 王绪飞赵桂增黄小为王向锋
Owner 刘德鹏
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