Axitinib crystal form

A technology of Axitinib and Ni crystal, which is applied in the field of Axitinib crystal form, can solve the problems of solubility, thermal stability, photostability, dissolution rate and bioavailability that cannot well meet the requirements of pharmaceutical preparations, and achieve Good light stability, improved drug bioavailability, and good solubility effects

Active Publication Date: 2022-01-18
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Since the known crystal forms of axitinib cannot well meet the requirements of pharmaceutical preparations in terms of solubility, thermal stability, photostability, dissolution rate, bioavailability, etc., more crystal forms need to be developed. On the one hand, provide more axitinib crystal forms for drug application; on the other hand, it is also necessary to develop axitinib crystal forms that are more suitable for industrial production and have high economic benefits

Method used

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  • Axitinib crystal form
  • Axitinib crystal form
  • Axitinib crystal form

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044]Add about 1g of axitinib to 30ml of glacial acetic acid, heat to 50°C and stir to dissolve, then add about 90ml of diethyl ether and continue to keep warm at 50°C and stir for 1 hour. crystallization; after the crystallization is completed, filter and dry to obtain the crystal form of axitinib with a yield of 97.8% and a purity of 99.92%.

Embodiment 2

[0046] Add about 1g of axitinib to 20ml of N,N-dimethylformamide, heat to 60°C and stir to dissolve, then add about 80ml of diethyl ether and continue to keep warm at 60°C and stir for 2 hours. After the reaction is over, the temperature of the reaction solution is cooled Stir and crystallize at 0-5°C; after the crystallization is completed, filter and dry to obtain the crystal form of axitinib with a yield of 97.2% and a purity of 99.93%.

Embodiment 3

[0048] Add about 1g of axitinib to 50ml of dimethyl sulfoxide, heat to 30°C and stir to dissolve, then add about 100ml of methyl ether and continue to keep warm at 30°C and stir for 1 hour. After the reaction is complete, the temperature of the reaction solution is cooled to -5 Stir and crystallize at ~0°C; after the crystallization is completed, filter and dry to obtain the crystalline form of axitinib with a yield of 96.5% and a purity of 99.90%.

[0049] Axitinib crystal form characterization

[0050] The X-ray powder diffraction test instrument involved in the present invention and test condition: X-ray powder diffractometer: PANalytical EMPYREA; Cu-Kα; Sample table: flat panel; Incident light path: BBHD; Diffraction light path: PLXCEL; Voltage 45kv, electric current 40mA; Divergence slit: 1 / 4; Anti-scatter slit: 1; Solar slit: 0.04rad; Step size: 0.5s; Scanning range: 3~50°. The characteristic peaks in the corresponding X-ray secretion diffraction pattern (Cu-Kα) are det...

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Abstract

The invention provides an axitinib crystal form, and relates to the technical field of crystal form medicine molecules. The axitinib crystal form is radiated by Cu-K alpha, wherein an X-ray diffraction pattern expressed by 2 theta has characteristic peaks at 7.45 + / -0.2 degrees, 10.39 + / -0.2 degrees, 11.96 + / -0.2 degrees, 12.43 + / -0.2 degrees, 14.86 + / -0.2 degrees, 15.05 + / -0.2 degrees, 17.44 + / -0.2 degrees, 18.78 + / -0.2 degrees, 19.17 + / -0.2 degrees, 19.65 + / -0.2 degrees, 23.92 + / -0.2 degrees, 24.47 + / -0.2 degrees, 25.06 + / -0.2 degrees, 26.81 + / -0.2 degrees and 28.03 + / -0.2 degrees. the invention also provides a related preparation method and application. The axitinib crystal form disclosed by the invention is insensitive to illumination and relatively good in solubility, and by utilizing the axitinib crystal form to prepare a medicine, the bioavailability can be increased, and the medicine effect can be improved.

Description

technical field [0001] The invention relates to the technical field of crystal drug molecules, in particular to a crystal form of axitinib. Background technique [0002] In recent years, studies have found that different crystal forms of drugs can change their physical and chemical properties (density, hardness, solubility, stability, optical and electrical properties, etc.), dissolution rate, biological effects, etc. It has important practical value in science. Crystalline drug molecules include polymorphs, hydrates, solvates, and salts of drug molecules. Through drug crystallization, not only can the crystallographic parameters of crystalline drug molecules be clarified, but also the type of solvent molecules in the crystal form can be determined. And the number (such as: crystal water molecules), plays a very important role in understanding and mastering the spatial arrangement and physical and chemical properties of drug molecules. [0003] Axitinib is white or off-whi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/06A61K31/4439A61P35/00
CPCC07D401/06A61P35/00C07B2200/13
Inventor 张贵民刘建设翟立海王聚聚
Owner LUNAN PHARMA GROUP CORPORATION
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