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Frovatriptan succinate crystal and its pharmaceutical composition and use

A kind of technology of frotriptan succinate and composition, applied in the field of frotriptan succinate crystal and pharmaceutical composition thereof

Inactive Publication Date: 2016-07-27
DIHON PHARMA GROUP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The commercial form of frovatriptan is frovatriptan succinate, and no crystal form has been reported so far

Method used

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  • Frovatriptan succinate crystal and its pharmaceutical composition and use
  • Frovatriptan succinate crystal and its pharmaceutical composition and use
  • Frovatriptan succinate crystal and its pharmaceutical composition and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Add 1.00 g of frovatriptan succinate, 7.5 ml of ethanol, and 2.5 ml of water into a three-necked flask. Heat and stir in an oil bath at 80±2°C. When the solids are completely dissolved, stop heating, filter while hot, and slowly stir the filtrate. After cooling and crystallization, filtration, the filter cake was vacuum dried at 55±5°C for 6 hours to obtain 0.83 g of crystalline powder. Determine the powder X-ray diffraction pattern and data, infrared spectrogram, thermogravimetric analysis pattern and differential scanning pattern, according to the powder X-ray diffraction pattern (see figure 1 ) The characteristic absorption peak 2θ value 7.922, 8.339, 11.179, 15.837, 16.686, 17.525, 18.850, 21.265, 23.662, 24.905, 25.990 and 35.116cm -1 ), infrared spectrogram (see figure 2 , 3399.0, 3183.6, 3064.3, 2935.8, 2841.8,, 1665.7, 1628.0, 1585.5, 1567.9, 1479.5, 1262.0, 888.8, 812.8cm -1 ), thermogravimetric analysis chart (see image 3 ) And differential scanning calorimetr...

Embodiment 2

[0027] Add 1.00g of frovatriptan succinate, 9ml of ethanol, and 3ml of water into a three-necked flask. Heat and stir in an oil bath at 80±2℃. When the solid is completely dissolved, stop heating, filter while it is hot, and slowly cool the filtrate while stirring. Crystallized, filtered, and the filter cake was vacuum dried at 55±5°C for 6 hours to obtain 0.70 g of crystalline powder.

Embodiment 3

[0029] Add 1.00g of frovatriptan succinate, 6ml of ethanol and 2ml of water into a three-necked flask, heat and stir in an oil bath at 80±2℃ until the solids are dissolved, stop heating, filter while hot, and slowly cool the filtrate to crystallize while stirring. After filtering, the filter cake was vacuum dried at 55±5°C for 6 hours to obtain 0.67 g of crystalline powder.

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Abstract

The invention discloses a frovatriptan succinate crystal. The frovatriptan succinate crystal has characteristic absorption peaks at reflection angles 2 theta of 7.922, 8.339, 11.179, 15.837, 16.686, 17.525, 18.850, 21.265, 23.662, 24.078, 24.905, 25.155, 25.990 and 35.116cm<-1> in a X-ray power diffraction (XRPD) graph. The invention also relates to a pharmaceutical composition for treating migraine. The pharmaceutical composition contains the frovatriptan succinate crystals and one or more medicinal excipients. The invention also relates to a use of the frovatriptan succinate crystal in preparation of a drug for treating migraine.

Description

Technical field [0001] The invention belongs to the technical field of medicinal chemistry, and specifically relates to a frovatriptan succinate crystal and a pharmaceutical composition and application thereof. technical background [0002] Frotriptan is a second-generation triptan drug, a selective 5HT 1B And 5HT 1D Receptor subtype agonist, and 5HT 1B And 5HT 1D The receptor has a high affinity for 5HT 1B Its affinity is the strongest among the triptan drugs, and its mechanism of action is mainly to treat migraine by inhibiting the excessive expansion of the extracerebral and intracranial arteries. [0003] Frotriptan was first developed by GlaxoSmithKine and then transferred to Venalis. It was first listed in the United States in June 2002 under the trade name FROVA (EndoPharmaceuticals acquired the agency rights of this product in the United States). It is clinically used in adults with or without aura The acute treatment of migraine attacks is now available in many European co...

Claims

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Application Information

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IPC IPC(8): C07D209/88C07C55/10C07C51/41A61K31/403A61P25/06
Inventor 官敬博李蕾蕾马燕如陈正伟
Owner DIHON PHARMA GROUP
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