A more stable sodium ozagrel compound and pharmaceutical composition thereof

A technology of ozagrel sodium and compounds, which is applied in the field of preparation of pharmaceutical compounds, can solve the problems of greater than 0.2%, and achieve the effects of good crystal shape, high yield, and low impurity content

Inactive Publication Date: 2011-12-14
贺金凤
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the prior art uses 95% ethanol as the recrystallization solvent. Although the content of sodium ozagrel afte...

Method used

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  • A more stable sodium ozagrel compound and pharmaceutical composition thereof
  • A more stable sodium ozagrel compound and pharmaceutical composition thereof
  • A more stable sodium ozagrel compound and pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] The crude product of sodium ozagrel is dissolved in a mixed solvent of ethyl acetate and methanol=1:1 (v / v) of 8 times its weight, and the active carbon of about 5% (w / v) weight of the solution volume is added, and heated to reflux Temperature, last for 1 hour, place at room temperature for 24 hours, precipitate crystals, obtain crystals after suction filtration, repeat the above steps to obtain the second recrystallization product, wash with ethanol, and dry to obtain pure ozagrel sodium, which is detected by HPLC , the obtained pure ozagrel sodium has a purity of 99.48%, and the content of two unknown impurities is less than 0.1%.

Embodiment 2

[0037]

[0038] Its preparation method is as follows:

[0039] Take 100 g of sodium ozagrel, mix and grind it with PEG-400, dissolve the ground material of sodium ozagrel and PEG-400 with the prepared disodium hydrogen phosphate-sodium dihydrogen phosphate buffer solution with a pH value of 6.5, and add 0.5% activated carbon, heated to 80°C and maintained for 15 minutes, filtered to remove carbon, then added sodium bisulfite, disodium edetate, stirred to dissolve, added disodium hydrogen phosphate-sodium dihydrogen phosphate buffer to 10000ml, added 0.5% activated carbon, boiled, finely filtered with a 0.45 μm microporous membrane, and sterilized with a 0.20 μm microporous membrane, canned, sterilized, and labeled.

Embodiment 3

[0041]

[0042] Its preparation method is as follows:

[0043] Take 100 g of sodium ozagrel, mix and grind it with PEG-400, dissolve the ground material of sodium ozagrel and PEG-400 with the prepared disodium hydrogen phosphate-sodium dihydrogen phosphate buffer solution with a pH value of 6.5, and add 0.5% activated carbon, heated to 80°C and maintained for 15 minutes, filtered to remove carbon, then added sodium bisulfite, disodium edetate, stirred to dissolve, added disodium hydrogen phosphate-sodium dihydrogen phosphate buffer to 10000ml, added 0.5% activated carbon, boiled, finely filtered with a 0.45 μm microporous membrane, and sterilized with a 0.20 μm microporous membrane, canned, semi-sealed, put into a freeze-drying box, freeze-dried, sealed, Label it and pack it.

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PUM

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Abstract

The present invention relates to a more stable sodium ozagrel compound and a pharmaceutical composition, which comprises recrystallizing the crude product sodium ozagrel with ethyl acetate:methanol=1:1 as a solvent for 1-3 times, and simultaneously using activated carbon White crystals are obtained after decolorization.

Description

Technical field: [0001] The invention relates to the preparation of a pharmaceutical compound, especially the preparation of an antiasthma medicine ozagrel sodium compound. Background technique: [0002] Ozagrel sodium is a thromboxane (TX) synthase inhibitor, chemical name: trans-3-4-(1H-imidazolyl-1-methyl)phenyl-2-propenoic acid sodium. [0003] [0004] Sodium ozagrel can prevent prostaglandin H2 (PGH2) from generating thromboxane A2 (TXA2), and promote the transfer of platelet-derived PGH2 to endothelial cells. Endothelial cells are used to synthesize PGI2, thereby improving the abnormal balance of TXA2 and prostaglandin PGI2. In theory, it can inhibit the aggregation of platelets and dilate blood vessels. [0005] Ozagrel sodium can improve the movement disorder in the acute stage of cerebral thrombosis, improve the circulation disorder in the acute stage of cerebral ischemia, and improve the abnormal energy metabolism during cerebral ischemia. Animal experiments...

Claims

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Application Information

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IPC IPC(8): C07D233/56A61K31/4174A61K9/19A61K9/08
Inventor 贺金凤
Owner 贺金凤
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