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Pharmaceutical compound for treating digestive system diseases, and preparation method thereof

A technology for digestive system diseases and pharmaceutical compounds, applied in the field of medicine, can solve problems affecting safety, low purity, poor solubility, etc., achieve the effects of improved dissolution rate and stability, simple and easy-to-operate preparation method, and mild reaction conditions

Inactive Publication Date: 2017-09-15
HUNAN QIWEI TECH CO LTD
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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 digestive system diseases, and preparation method thereof
  • Pharmaceutical compound for treating digestive system diseases, and preparation method thereof
  • Pharmaceutical compound for treating digestive system diseases, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Embodiment 1, the preparation of fumaric acid vonoprazan dihydrate

[0057] 1) Dissolve 100 g of crude vonoprazan fumarate in (1500 ml) a mixed solvent of dimethyl sulfoxide and water (dimethyl sulfoxide: water = 2:1), stir and heat at a speed of 220 rpm Dissolve the crude product completely until the solution is clear and filter;

[0058] 2) Slowly lower the temperature of the solution obtained above at a rate of 3°C every 10 minutes. When it drops to 0°C, add 6000ml of pre-cooled purified water to the solution at a flow rate of 2.0mL / min until the crystals appear, and continue to cool down to -20 Crystallize at ℃, heat and stir until the crystallization is complete, and grow the crystal for 2 hours;

[0059] 3) The crystals were collected by suction filtration, washed with a small amount of purified water, and dried in vacuum at 50° C. for 4 hours to obtain 99.90 g of white crystalline powder with a yield of 99.90% and a purity of 99.98%.

[0060] The X-ray powder d...

Embodiment 2

[0061] Embodiment 2, the preparation of fumaric acid vonoprazan dihydrate

[0062] 1) Dissolve 100 g of crude vonoprazan fumarate in 2000 ml of a mixed solvent of dimethyl sulfoxide and water (dimethyl sulfoxide: water = 3:1), stir and heat at a speed of 250 rpm to make the crude product Dissolve completely until the solution is clear and filter;

[0063] 2) Slowly lower the temperature of the solution obtained above at a rate of 1°C every 10 minutes. When it drops to -5°C, add 6000ml of pre-cooled purified water to the solution at a flow rate of 2.2mL / min until the crystals appear, and continue to cool down to - Crystallize at 15°C, heat and stir until the crystallization is complete, and grow the crystal for 4 hours;

[0064] 3) The crystals were collected by suction filtration, washed with a small amount of purified water, and dried in vacuum at 45° C. for 5 hours to obtain 99.91 g of white crystalline powder with a yield of 99.91% and a purity of 99.99%.

[0065] The X-r...

Embodiment 3

[0066] Embodiment 3, the preparation of fumaric acid vonoprazan dihydrate

[0067] 1) Dissolve 100 g of crude vonoprazan fumarate in 1800 ml of a mixed solvent of dimethyl sulfoxide and water (dimethyl sulfoxide: water = 3:1), stir and heat at a speed of 240 rpm to make the crude product Dissolve completely until the solution is clear and filter;

[0068]2) Slowly lower the temperature of the solution obtained above at a rate of 2°C every 10 minutes. When it drops to -3°C, add 6300ml of pre-cooled purified water to the solution at a flow rate of 2.5mL / min until the crystals appear, and continue to cool down to - Crystallize at 15°C, heat and stir until the crystallization is complete, and grow the crystal for 3 hours;

[0069] 3) The crystals were collected by suction filtration, washed with a small amount of purified water, and dried in vacuum at 45° C. for 5 hours to obtain 99.94 g of white crystalline powder with a yield of 99.94% and a purity of 99.99%.

[0070] The X-ra...

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Abstract

The invention belongs to the technical field of medicine and discloses a medicinal compound for treating digestive system diseases and a preparation method thereof. The provided vonoprazan fumaric acid dihydrate has high purity and good stability, and its diffraction angle is 2θ±0.2° The indicated X-ray powder diffraction pattern shows the Characteristic diffraction peak, the X-ray powder diffraction spectrogram that uses Cu-Kα ray measurement to obtain is shown in Figure 1, is completely different from the prior art, finds that the fumaric acid vonoprazan dihydrate obtained by the present invention is pleasantly surprised by experiments The solubility of the substance was significantly improved. The dissolution rate and stability of the composition tablet prepared from the vonoprazan fumarate dihydrate of the present invention are significantly improved, and are very 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 diseases of the digestive system and a preparation method thereof, in particular to vonoprazan fumarate dihydrate 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 stabi...

Claims

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Application Information

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IPC IPC(8): C07D401/12
CPCC07D401/12C07B2200/13
Inventor 朱社凤
Owner HUNAN QIWEI TECH CO LTD
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