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New crystal form of axitinib fumarate and preparation method thereof

A technology of nifumarate and axitinib, applied in the field of medicinal chemistry, can solve the problems of limited oral bioavailability, poor photostability of axitinib, clinical application limitations, etc., and achieves easy control and good crystallization process. Effects of photostability, large apparent solubility

Inactive Publication Date: 2021-01-05
TIANJIN UNIVERSITY OF TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The axitinib currently used in China is all imported, which is expensive and unaffordable for ordinary patients, which limits its clinical application
In addition, axitinib has poor photostability, belongs to BCS class II drugs, and has poor water solubility, which limits its oral bioavailability

Method used

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  • New crystal form of axitinib fumarate and preparation method thereof
  • New crystal form of axitinib fumarate and preparation method thereof
  • New crystal form of axitinib fumarate and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Weigh 386 mg of axitinib and 174.1 mg of fumaric acid, add 10 mL of n-heptane and 50 μL of ethanol to obtain a suspension, stir the suspension at room temperature for 4 h, filter, and dry the obtained white solid at 40 ° C to obtain A solid sample of axitinib fumarate salt form B, with a yield of 90.6%.

Embodiment 2

[0039] Weigh 38.6 mg of axitinib and 17.4 mg of fumaric acid, add 1 mL of n-heptane and 10 μL of methanol to obtain a suspension, stir the suspension at room temperature for 24 hours, filter, and dry the obtained white solid at 40 ° C to obtain Solid sample of axitinib fumarate form B.

Embodiment 3

[0041] Weigh 38.6 mg of axitinib and 17.4 mg of fumaric acid, add 1 mL of n-heptane and 10 μL of ethanol to obtain a suspension, stir the suspension at room temperature for 24 hours, filter, and dry the obtained white solid at 40 ° C to obtain Solid sample of axitinib fumarate form B.

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Abstract

The invention discloses a new crystal form of axitinib fumarate and a preparation method thereof. In the new crystal form, the molar ratio of axitinib to fumaric acid is 1: 1.5, and the X-ray powder diffraction pattern of the crystal form has characteristic peaks when the 2 theta value is 7.1 + / -0.2 degrees, 12.5 + / -0.2 degrees, 15.1 + / -0.2 degrees, 17.4 + / -0.2 degrees and 23.4 + / -0.2 degrees. Thecrystal form preparation method provided by the invention is simple in process, easy in crystallization process control, good in reproducibility and suitable for industrial production. The new crystal form of the axitinib fumarate is remarkably improved in the aspects of light stability and dissolution property, and is beneficial to improving the safety and oral bioavailability of axitinib.

Description

technical field [0001] The invention relates to the technical field of medicinal chemistry, in particular to a new crystal form of axitinib fumarate and a preparation method thereof. Background technique [0002] The chemical name of Axitinib is N-methyl-2-[[3-[(1E)-2-(2-pyridyl)vinyl]-1H-indazol-6-yl]thio ] benzamide, its chemical structural formula is: [0003] Axitinib is a second-generation VEGFR inhibitor that can selectively inhibit the activity of vascular endothelial growth factor VEGF-1, VEGF-2, and VEGF-3 receptors to exert anti-cancer effects. The drug was developed by Pfizer under the trade name On January 27, 2012, it was approved by the FDA for the treatment of early to advanced kidney cancer, and in September of the same year, it was approved by the EMA for marketing in Europe. Currently, the drug is used in several countries for the treatment of advanced renal cell carcinoma. Patent US20060094763 discloses crystal forms I, II, III, IV, VI, VII, VIII an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/06C07C51/43C07C57/15A61K31/4439A61P35/00A61P9/00
CPCC07D401/06C07C51/43A61K31/4439A61P35/00A61P9/00C07B2200/13C07C57/15
Inventor 陈嘉媚任伯颖王洁
Owner TIANJIN UNIVERSITY OF TECHNOLOGY
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