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Organic salt of pyritinol and its prepn process

A technology of organic acid salt and pyrithione, which is applied in the field of preparation of pyrithione organic acid salt, and can solve the problems such as the use limitation of pyrithione hydrochloride

Inactive Publication Date: 2007-11-07
GUANGDONG ZHONGKE DRUG R&D
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

More side effects lead to certain restrictions on the use of pyrithione hydrochloride for injection

Method used

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  • Organic salt of pyritinol and its prepn process
  • Organic salt of pyritinol and its prepn process
  • Organic salt of pyritinol and its prepn process

Examples

Experimental program
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Effect test

Embodiment 1

[0016] Embodiment 1: the synthesis of nicotinic acid pyrithione salt

[0017] Take 24.6g of nicotinic acid, fully dissolve in 300ml of anhydrous benzene, heat and stir until completely dissolved, add 40.5g of pyrithione under the state of complete dissolution, heat and reflux the mixture for 3 hours, TLC thin layer identification reaction is complete (developing agent: acetic acid Ethyl ester: ethanol: glacial acetic acid = 5: 6: 0.6), after cooling slightly, add 200ml of absolute ethanol, put the mixture into the refrigerator to fully cool, and filter out white crystals by suction filtration, wash the solid with a small amount of cold anhydrous ether. Vacuum-dried at 65°C to obtain 62.1 g of nicotinic acid pyrithione salt with a yield of 89.7%. The contents of niacin and pyrithione were determined by acid-base titration, and the water content was determined by Karl Fischer method. The result is: niacin 37.2%, pyrithione 62.0%, water 5.8%, close to the theoretical value, cont...

Embodiment 2

[0018] Embodiment 2: the synthesis of pyrithione fumarate

[0019] Take 11.6g of fumaric acid, fully dissolve it in 300ml of anhydrous benzene, heat and stir until it is completely dissolved, add 40.5g of pyrithione in the fully dissolved state, heat and reflux the mixture for 3 hours, TLC thin layer identification reaction is complete (developing agent: Ethyl acetate: ethanol: glacial acetic acid = 5: 4: 0.8), after cooling slightly, add 200ml of absolute ethanol, put the mixture in the refrigerator to fully cool, and filter out white crystals by suction filtration, wash the solid with a small amount of cold anhydrous ether. Vacuum-dried at 65°C to obtain 49.9 g of pyrithione fumarate, with a yield of 88.9%. The content of fumaric acid and pyrithione was determined by acid-base titration, and the moisture content was determined by Karl Fischer method. The result is: 20.8% fumaric acid, 72.7% pyrithione, 6.5% water, close to the theoretical value, containing 2 crystal waters....

Embodiment 3

[0020] Embodiment 3: the synthesis of glucuronic acid pyrithione salt

[0021] Get 42.4g of glucuronic acid, fully dissolve in 300ml of anhydrous benzene, heat and stir until fully dissolved, add 40.5g of pyrithione under fully dissolved state, heat and reflux the mixture for 3 hours, TLC thin layer identification reaction is complete (developing agent: Ethyl acetate: ethanol: glacial acetic acid = 6: 3: 0.8), after cooling slightly, add 200ml of absolute ethanol, put the mixture into the refrigerator to fully cool, and filter out white crystals by suction filtration, wash the solid with a small amount of cold anhydrous ether. Vacuum-dried at 65°C to obtain 75.9 g of pyrithione glucuronate, with a yield of 87.8%. The content of glucuronic acid and pyrithione was determined by acid-base titration, and the moisture content was determined by Karl Fischer method. The result is: glucuronic acid 49.0%, pyrithione 46.8%, water 4.2%, close to theoretical value, containing 2 crystal w...

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Abstract

The present invention relates to organic salt of pyritinol as shown for treating cerebral concussion, brain trauma, encephalitis, meningitis sequelae and senile dementia. The organic salt exists in hydrate and is named as 3, 3-(dithio methylene) bis(5-hydroxy-6-methyl-pyridyl methane) organic salt chemically. The organic salt is salt of nicotinic acid, lactobionic acid, malic acid, etc. Experiments show that the organic acid and pyritinol have synergistic effect of protecting cardiac muscle, and the nicotinate of pyritinol is especially hopeful in developing pyritinol medicine.

Description

technical field [0001] The invention relates to a salt of pyrithione, which is used for treating concussion syndrome, traumatic brain injury, encephalitis, sequela of meningitis, senile dementia, etc., and the preparation method and medical application of the pyrithione organic acid salt. Background technique [0002] Pyritinol is a synthetic powerful antioxidant and smart drug. In living organisms, normal oxidation processes (plus a small amount of ion scattering) generate highly reactive free radicals that can easily react with and damage other molecules, some of which are anti-infective in the body , Pyritinol can prevent the oxidation of other chemical substances and has an antioxidant effect. Pyritinol, also known as smart medicine, is a substance that enhances thinking ability. These substances enhance the exercise of intelligence in various ways, thereby supporting cognition, sobriety, memory, good mood, promoting the utilization of oxygen and glucose, promoting the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/444A61P25/00A61P25/28
Inventor 陈文展王伟
Owner GUANGDONG ZHONGKE DRUG R&D
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