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Novel pregabalin crystalline form and its preparing process

A technology of pregabalin and crystal form, which is applied to the composition containing it and its preparation, the field of new crystal forms, and achieves the effects of good stability, controllable product quality and good crystal form stability

Inactive Publication Date: 2005-07-06
FUKANGREN BIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is no public report on the crystal form of pregabalin in the existing literature

Method used

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  • Novel pregabalin crystalline form and its preparing process
  • Novel pregabalin crystalline form and its preparing process
  • Novel pregabalin crystalline form and its preparing process

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Add 5 grams of pregabalin into a 250ml flask, add 90ml of isopropanol and 30ml of water, heat to 70-75°C to dissolve, filter while hot, cool to 0°C to crystallize, leave overnight, filter, wash with isopropanol, Vacuum drying at 40° C. for 12 hours yielded a new crystal form of pregabalin with a purity of 88%.

Embodiment 2

[0032] Add 5 grams of pregabalin into a 250ml flask, add 120ml of ethanol and 30ml of water, heat to 70-75°C to dissolve, filter while hot, cool to 0°C to crystallize, leave overnight, filter, wash with ethanol, vacuum at 40°C After drying for 12 hours, a new crystal form of pregabalin with a purity of 84% was obtained.

Embodiment 3

[0034] Add 5 grams of pregabalin to a 250ml flask, add 80ml propanol and 30ml water, heat to 70-75°C to dissolve, filter while hot, cool to 0°C to crystallize, leave overnight, filter, wash with propanol, 40°C After vacuum drying for 12 hours, a new crystal form of pregabalin with a purity of 85% was obtained.

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PUM

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Abstract

The invention relates to a novel crystalline form of pregabalin drug for treating epilepsy and neuropathic pain and its preparation method. Compared to others pregabalin with agraphitic form and other forms, pregabalin with the novel crystalline form has good stability and is suitable for mass production. Pregabalin with the novel crystalline form uses Cu-Ka radiation and its X-ray powder diffraction has characteristic peak at 9.5(9.3), 12.3(7.2), 16.7(5.3), 18.4(4.8), 19.9(4.5) and 23.3(3.8) with the coordinate of 2-theta and interplanar spacing (d).

Description

Technical field: [0001] The invention relates to a crystal form of medicine for treating epilepsy and neuropathic pain, especially a new crystal form of pregabalin, a composition containing it and a preparation method thereof. Background technique: [0002] The chemical name of pregabalin is (+)-4-amino-3(S)-isobutylbutyric acid. Pregabalin is a gamma-aminobutyric acid (GABA) receptor antagonist, similar to gabapentin (gabapentin), which is also a 3-alkyl substitution of GABA, but compared with gabapentin, this product has a lower dose and more frequent doses. Less, less side effects and other advantages. Clinical research for the treatment of epilepsy, neuropathic pain and other disorders such as anxiety and depression. Related information disclosures include: world patents WO9638405, WO9640617, WO04054565, WO03066040, WO03061656, WO03020273; Drugs of the Future1999, 24 (8): 826-870. There is no public report on the crystal form of pregabalin in the existing literature. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/197A61P25/04A61P25/08C07C229/08
Inventor 姚勇敢
Owner FUKANGREN BIO PHARMA
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