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Ozagrel meglumine salt and its composition, preparation method and use

A technology of meglumine salt and meglumine salt, which can be used in the preparation of organic compounds, the preparation of aminohydroxy compounds, drug combination and other directions, can solve the problems of staying, poor taste and the like

Inactive Publication Date: 2017-02-22
SHENYANG J & HEALTH PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0020] While studying the injection of ozagrel salt, the present invention also studied the oral liquid preparation, and unexpectedly found that the mouthfeel of the existing ozagrel salt is not good when taken orally, especially the oral liquid, after taking it, there is a smell

Method used

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  • Ozagrel meglumine salt and its composition, preparation method and use
  • Ozagrel meglumine salt and its composition, preparation method and use
  • Ozagrel meglumine salt and its composition, preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0079] Preparation of ozagrel meglumine salt:

[0080] At 10-15°C, add 60.00g (0.263mol) of meglumine to 95% ethanol, stir and heat to reflux, add 57.17g (0.250mol) of Ozagrel solid, the reaction solution is clear, keep warm and react, the reaction ends naturally When the temperature reaches 10-15°C, continue to stir and crystallize, filter with suction, rinse the filter cake with ethanol, and dry the filter cake at 40°C with blast to obtain a white powder. Add the crude product of ozagrel meglumine salt into 400ml of 50% ethanol at room temperature, heat and reflux until completely dissolved, then naturally cool down to room temperature and continue to stir and crystallize for 5h, filter with suction, rinse the filter cake with absolute ethanol, and keep the filter cake at 40°C Blow drying to obtain a white crystalline powder with a yield of 98.40 g, a yield of 92.77%, and a content of 100.2%. MS[M-H] - :422.02

[0081] 1 H-NMR (400MHz, DMSO-d 6 )δ (ppm): 7.75 (1H, s), 7...

Embodiment 2

[0085] Preparation of ozagrel meglumine salt:

[0086] At 10-15°C, add 60.00g (0.263mol) of meglumine to 90% methanol, stir and heat to reflux, add 41.31g (0.181mol) of Ozagrel solid, the reaction solution is clear, keep warm and react, the reaction ends naturally Lower the temperature to 10-15°C, continue to stir and crystallize, filter with suction, wash the filter cake with methanol, and dry the filter cake at 40°C with blast to obtain a white powder. Add the crude product of ozagrel meglumine salt into 300ml of 50% ethanol at room temperature, heat and reflux until completely dissolved, then naturally cool down to room temperature and continue to stir and crystallize for 5 hours, filter with suction, rinse the filter cake with methanol, and dry the filter cake by air at 40°C A white crystalline powder was obtained with a yield of 67.02 g, a yield of 87.44%, and a content of 99.7%.

Embodiment 3

[0088] Preparation of ozagrel meglumine salt

[0089] At 10-15°C, add 60.00g (0.263mol) of meglumine to 80% isopropanol, stir and heat to reflux, add 52.20g (0.229mol) of Ozagrel solid, the reaction solution is clear, keep warm for reaction, and react After the end, it will naturally cool down to 10-15°C, continue to stir and crystallize, filter with suction, rinse the filter cake with isopropanol, and dry the filter cake with air at 40°C to obtain a white powder. Add the crude product of ozagrel meglumine salt into 300ml of 50% ethanol at room temperature, heat and reflux until completely dissolved, then naturally cool down to room temperature and continue to stir and crystallize for 5h, filter with suction, rinse the filter cake with isopropanol, and keep the filter cake at 40°C Blow drying to obtain a white crystalline powder with a yield of 83.98 g, a yield of 86.72%, and a content of 99.3%.

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Abstract

The invention provides ozagrel meglumine salt with functions of anti-platelet aggregation and vasospasm relieving. Composition suitable for clinical application is prepared from the salt. The composition has high long-term placement stability and good water solubility and can be prepared to form injection preparations, and the injection preparations comprise an aseptic powder injection preparation, a vial injection, a large volume parenteral and a freeze-dried injection preparation for injection.

Description

technical field [0001] The present invention relates to a medicine with anti-platelet aggregation effect, in particular to a ozagrel salt, more specifically to ozagrel meglumine and its composition, and a preparation method of ozagrel meglumine salt, which belongs to medicine field of chemical and pharmaceutical preparations. Background technique [0002] Acute thrombotic cerebral infarction (CI) is a general term for ischemic stroke, including cerebral thrombosis, lacunar infarction, and cerebral embolism, accounting for about 70% of all strokes. Disorders cause brain lesions. All age groups have the disease, but it is more common in middle-aged and above, especially in hypertensive patients. The clinical features are rapid onset and high mortality, and about 75% of the survivors will lose their labor force to varying degrees. [0003] Ozagrey, the structure is as follows: [0004] [0005] Ozagrel is a thromboxane synthase inhibitor, which can specifically inhibit t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D233/60C07C213/08C07C215/10A61K31/4174A61P9/10A61P7/02A61P9/00
CPCC07D233/56
Inventor 史秀兰
Owner SHENYANG J & HEALTH PHARMA
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