Pantoprazole sodium compound and pharmaceutical composition thereof

A technology of pantoprazole sodium and its compound, which is applied in the field of pantoprazole sodium compound and its pharmaceutical composition, which can solve the problems of fewer dosage forms, restrictions on the use of pantoprazole sodium, complex process requirements, etc., and achieve high quality The effect of stability

Active Publication Date: 2013-04-03
湖北美林药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In order to solve this problem, prior art generally solves this problem from preparation technology, and often technology requires strict and complicated, has limited the use of pantoprazole sodium in preparation, also has from some research attempts to solve this problem from crystal structure research. problem, but the obtained pantoprazole sodium compound supports less dosage forms, which limits the use of pantoprazole sodium, and the commonly used pharmaceutical dosage forms of pantoprazole sodium include powder injection, tablet, and capsule. This dosage form has respective advantages for different types of patients; The inventor has unexpectedly obtained a kind of pantoprazole sodium entity compound in crystalline form in the long-term large amount of research process, and this pantoprazole sodium entity compound contains a crystal water, The compound can be prepared into various dosage forms according to the content of the present invention, and maintains extremely high stability, which is obviously better than commercially available varieties, and greatly improves the safety and effectiveness of pantoprazole sodium use

Method used

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  • Pantoprazole sodium compound and pharmaceutical composition thereof
  • Pantoprazole sodium compound and pharmaceutical composition thereof
  • Pantoprazole sodium compound and pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0082] The preparation of embodiment 1 pantoprazole sodium compound

[0083] 1. Mix pantoprazole with methanol and chloroform mixture (volume ratio 10:1) at a weight ratio of 1:8, stir at 600 rpm for 30 minutes, and keep the temperature at 25°C.

[0084] 2. Add sodium hydroxide equimolar to pantoprazole, continue to stir at 25° C. with a speed of 600 rpm, and react for 4 hours.

[0085] 3. At 25°C, while stirring at 400 rpm, slowly (60ml / min) add chloroform, which is 6 times the weight of the mixture of methanol and chloroform, to 2, and lower the temperature to 8°C, keep it for 6 hours, and filter , Dry the filter cake at 35°C to constant weight.

[0086] 4. Mix the dry product in 3 with the mixture of ethanol, ether, and chloroform (volume ratio 10:1:3) in a weight ratio of 1:9, stir at 800 rpm for 1 hour, and keep the temperature at 35°C.

[0087] 5. At 35°C, while stirring at 800 rpm, slowly (60ml / min) add a mixture of chloroform and ether that is 6 times the weight o...

Embodiment 2

[0089] The preparation of embodiment 2 pantoprazole sodium compound

[0090] 1. Mix pantoprazole with methanol and chloroform mixture (volume ratio 10:1) at a weight ratio of 1:8, stir at 800 rpm for 30 minutes, and keep the temperature at 26°C.

[0091]2. Add sodium hydroxide equimolar to pantoprazole, continue to stir at 26° C. with 800 rpm, and react for 4 hours.

[0092] 3. At 26°C, while stirring at a speed of 500 rpm, slowly (70ml / min) add chloroform that is 6 times the weight of the mixture of methanol and chloroform to 2, and lower the temperature to 7°C, keep it for 6 hours, and filter , Dry the filter cake at 36°C to constant weight.

[0093] 4. Mix the dry product in 3 with the mixture of ethanol, ether and chloroform (volume ratio 10:1:3) in a weight ratio of 1:9, stir at 900 rpm for 1 hour, and keep the temperature at 36°C.

[0094] 5. At 36°C, while stirring at 900 rpm, slowly (40ml / min) add a mixture of chloroform and ether whose weight is 6 times that of the...

Embodiment 3

[0097] The preparation of embodiment 3 pantoprazole sodium compound

[0098] 1. Mix pantoprazole with methanol and chloroform mixture (volume ratio 10:1) at a weight ratio of 1:8, stir at 700 rpm for 30 minutes, and keep the temperature at 24°C.

[0099] 2. Add sodium hydroxide equimolar to pantoprazole, continue to stir at 24° C. with a speed of 700 rpm, and react for 4 hours.

[0100] 3. At 24°C, slowly (40ml / min) add chloroform, which is 6 times the weight of the mixture of methanol and chloroform, to 2 while stirring at a speed of 500 rpm, and lower the temperature to 9°C, keep it for 6 hours, and filter , Dry the filter cake at 36°C to constant weight.

[0101] 4. Mix the dry product in 3 with the mixture of ethanol, ether, and chloroform (volume ratio 10:1:3) in a weight ratio of 1:9, stir at 1000 rpm for 1 hour, and keep the temperature at 34°C.

[0102] 5. At 34°C, while stirring at 1000 rpm, slowly (70ml / min) add a mixture of chloroform and ether whose weight is ...

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Abstract

The invention relates to a pantoprazole sodium compound which is a crystal and is determined by X-ray powder diffraction. Characteristic peaks of the pantoprazole sodium compound are shown to be 7.2, 9.1, 11.0, 11.8, 14.7, 16.1, 18.4, 21.0, 23.5 and 25.2 at 2thet in a map. The invention also relates to a preparation method and a pharmaceutical composition of the pantoprazole sodium compound. The pharmaceutical composition comprises injection powder injection, enteric-coated tablet or enteric-coated capsule. Compared with the prior, the prepared pantoprazole sodium compound and the pharmaceutical composition thereof have obvious advantage in terms of quality stability.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a pantoprazole sodium compound and a pharmaceutical composition thereof. Background technique [0002] Pantoprazole sodium chemical name 5-difluoromethoxy-2-[(3,4-dimethoxy-2-pyridyl)methyl]sulfinyl-1H-benzoimidazole sodium salt, proton pump Inhibitory drugs, suitable for acute upper gastrointestinal bleeding such as duodenal ulcer, gastric ulcer, acute gastric mucosal lesions, and compound gastric ulcer. Because pantoprazole sodium has the chemical structure of sulfinylbenzimidazole, its stability is easily affected by various factors such as light, oxidizing and reducing components, and heavy metal ions. The content and related substances are very unstable, and the solution is easy to Discoloration, the existing commercially available pantoprazole sodium preparations are composed of general excipients and other auxiliary materials, so there are strict requirements...

Claims

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Application Information

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IPC IPC(8): C07D401/12A61K31/4439A61K9/14A61K9/20A61K9/48A61P1/04
Inventor 李美林胡成忠
Owner 湖北美林药业有限公司
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