Crystal form of pralatrexate, pharmaceutical composition containing pralatrexate, and preparation method and application of pralatrexate

A technology of crystal forms and drugs, which is applied in the direction of drug combinations, pharmaceutical formulas, and medical preparations containing active ingredients, can solve the problems of poor stability and low purity of crystal forms, and achieve good stability, simple preparation methods, and easy solvents. The effect

Active Publication Date: 2015-03-18
SHANGHAI INST OF PHARMA IND CO LTD +2
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AI Technical Summary

Problems solved by technology

[0009] The technical problem to be solved by the present invention is to overcome defects such as low purity and poor stability of the crystalline form of pralatrexate in the prior art, and provide a crystalline form of pralatrexate, a pharmaceutical composition containing it, and a preparation method thereof and application

Method used

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  • Crystal form of pralatrexate, pharmaceutical composition containing pralatrexate, and preparation method and application of pralatrexate
  • Crystal form of pralatrexate, pharmaceutical composition containing pralatrexate, and preparation method and application of pralatrexate
  • Crystal form of pralatrexate, pharmaceutical composition containing pralatrexate, and preparation method and application of pralatrexate

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preparation example Construction

[0028] Pratroxa preparation method: according to DeGraw et al. in the literature "Synthesis and Antitumor Activity of 10-Propargyl-10-deazaaminopterin" J. Med. Chem. 36: 2228-2231 (1993) provided the preparation method of the preparation method.

[0029] The preparation method of the crystalline form of Pratroxa: heating and dissolving Pratroxa in a good solvent, then adding anti-solvent until turbidity appears, cooling and crystallization.

Embodiment 1

[0033] Take 15.0g of Pratroxa (purity 98.01%) and add 100ml N,N-dimethylformamide, heat to 50℃, stir for 10 minutes, add 50ml acetonitrile dropwise, cool naturally to crystallize, and keep at room temperature 25℃ for 4 hours Continue to crystallize, filter, rinse the filter cake with 30 ml of acetonitrile, and dry the filter cake in vacuum at 50° C. to obtain 12.1 g of the crystal form of Pratroxa (purity 99.68%).

Embodiment 2

[0035] Take 15.0g of Pratroxa (purity 97.91%) and add 50ml of N,N-dimethylformamide, raise the temperature to 80°C, stir for 10 minutes, add 25ml of acetonitrile dropwise, cool naturally to crystallize, and keep at room temperature 25°C for 4 hours Continue to crystallize, filter, rinse the filter cake with 30 ml of acetonitrile, and dry the filter cake in vacuum at 50° C. to obtain 13.3 g of the crystal form of Pratroxa (purity: 99.52%).

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Abstract

The invention discloses a crystal form of pralatrexate, a pharmaceutical composition containing the pralatrexate, and a preparation method and an application of the pralatrexate. According to the crystal form, in an X-ray powder diffraction pattern using a radiation source as Cu-Kalpha, characteristic absorption peaks are formed at the diffraction angles 2theta of 8.29 degrees, 15.73 degrees, 16.72 degrees, 17.21 degrees, 18.46 degrees, 19.01 degrees, 21.38 degrees, 25.25 degrees and 25.56 degrees; and the error range of 2theta is +/-0.2 degrees. The preparation method of the crystal form disclosed by the invention comprises the following steps: heating and dissolving pralatrexate into a good solvent; and dropwise adding an anti-solvent until turbidity is achieved, naturally cooling, and devitrifying, so as to obtain the crystal form. The crystal form of the pralatrexate disclosed by the invention has the advantages of high purity, good stability and the like.

Description

Technical field [0001] The invention relates to a crystal form of Pratroxa, a pharmaceutical composition containing the same, and a preparation method and application thereof. Background technique [0002] Among the small molecule pharmaceutical compounds, there are many compounds in the form of different crystalline or polymorphic mixtures or solvates. They have different physical and chemical properties, and their solubility, stability, and spectral characteristics. Because of its different characteristics, the choice of raw materials with high purity and good stability in the formulation plays a vital role in the production of drugs. [0003] Pratroxa is (2S)-2-[[4-[(1RS)-1-[(2,4-Diaminopteridine-6-yl)methyl]-3-butynyl]benzoyl ]Amino]Glutaric acid is the common name, its structural formula is: [0004] [0005] Pratroxa is the first drug approved to market for the treatment of relapsed and refractory peripheral T-cell lymphoma. It is currently being studied in medicine for its u...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D475/08A61K31/519A61P35/00
CPCC07D475/08
Inventor 胡志袁哲东刘航
Owner SHANGHAI INST OF PHARMA IND CO LTD
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