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Crystal form of pyritinol maleate and preparation method thereof

A technology of acid pyrithione and maleic acid, applied in the field of medicine, can solve problems such as the lack of research reports on the crystal form of pyrithione maleate

Inactive Publication Date: 2015-12-16
ZHEJIANG YONGNING PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In the process of studying pyrithione maleate, the inventor also unexpectedly obtained a new crystal form of pyrithione maleate, and there is no research on the crystal form of pyrithione maleate in the prior art According to reports, the crystal form has obvious X-ray powder diffraction pattern characteristics, and the preparation method is simple, and the chemical stability is excellent

Method used

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  • Crystal form of pyritinol maleate and preparation method thereof
  • Crystal form of pyritinol maleate and preparation method thereof
  • Crystal form of pyritinol maleate and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Dissolve 3.8g of maleic acid in 100ml of ethanol, heat up to 60°C to dissolve, add 5.0g of pyrithione, stir to dissolve, react for 1 hour, cool and crystallize, filter, and dry the solid under reduced pressure at 50°C to obtain White crystalline solid pyrithione maleate crystal form A4.9g. X-ray powder diffraction analysis, such as figure 1 , and its 2θ values ​​are shown in the table below.

[0029]

[0030]

[0031]

Embodiment 2

[0033] Dissolve 3.8g of maleic acid in 100ml of acetone, heat up to 45°C to dissolve, add 5.0g of pyrithione, stir to dissolve, react for 1.5 hours, cool and crystallize, filter, and dry the solid under reduced pressure at 50°C to obtain White crystalline solid 5.2g. X-ray powder diffraction of the dry product shows pyrithione maleate as crystalline form A.

Embodiment 3

[0035] Dissolve 3.8g of maleic acid in 100ml of isopropanol, heat up to 60°C to dissolve, add 5.0g of pyrithione, stir to dissolve, react for 2 hours, cool and crystallize, filter, and dry the solid under reduced pressure at 50°C , to obtain 5.1 g of white crystalline solid. X-ray powder diffraction of the dry product shows pyrithione maleate as crystalline form A.

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Abstract

The invention discloses a novel crystal form of 3,3-(dithiobis methylene)bis(5-hydroxy-6-methyl-pyridyl methane) dimaleic acid, namely pyritinol maleate, and a preparation method thereof, wherein the novel crystal form is A form of pyritinol maleate. The A form of pyritinol maleate has stable physical and chemical properties, and is suitable for long-term storage and applies to preparation.

Description

technical field [0001] The present invention relates to a new crystal form of pyrithione maleate (i.e. 3,3-(dithiomethylene) bis(5-hydroxyl-6-methyl-pyridine) dimaleic acid) and its Preparation method, as well as pharmaceutical composition and medical use. Belonging to the field of medical technology Background technique [0002] The main application form of pyrithione is pyrithione hydrochloride, also known as brain rejuvenation, pyrithione hydrochloride can promote glucose and amino acid metabolism in the brain, improve systemic assimilation, increase carotid blood flow, and enhance brain function , It also has a stimulating effect on the limbic system and reticular structure. It is clinically used for dizziness, pain, insomnia, memory loss, inattention, and emotional changes in sequelae of traumatic brain injury, encephalitis, and meningitis; it is also used for cerebral arteriosclerosis and senile dementia mental symptoms. Pyritinol hydrochloride currently on the mark...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D213/66C07C51/41C07C57/145A61K31/444A61P25/28A61P9/10A61P25/20A61P25/00
Inventor 叶天健陈鑫洪亮候安伟
Owner ZHEJIANG YONGNING PHARMA
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