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Axitinib and glutaric acid eutectic crystal

A technology of axitinib and co- and axitinib, which is applied in the field of axitinib-glutaric acid co-crystal, can solve the problem of inability to judge the mode of action of API and CCF, and does not give the structure information of resveratrol complex and other problems, to achieve the effect of good photostability of eutectic, regular crystal form and uniform particle size.

Active Publication Date: 2022-07-01
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] At present, research reports on axitinib co-crystals are relatively rare. Only patent CN201910657224.2 reports a series of co-crystal complexes composed of histamine release inhibitors resveratrol and protein kinase inhibitors, including a resveratrol A co-crystal complex composed of resveratrol and axitinib at a molar ratio of 0.494 was attempted to prepare a co-crystal with a synergistic antihistamine effect; Determine the mode of action of API and CCF in the complex

Method used

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  • Axitinib and glutaric acid eutectic crystal
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  • Axitinib and glutaric acid eutectic crystal

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Add about 0.4g axitinib and 0.16g glutaric acid to 100ml isopropanol / formic acid (V 异丙醇 :V 甲酸 =3:1) in the mixed solution, heated to 55~60 ℃ to dissolve, stirred and refluxed for 4 hours, then cooled to 15~20 ℃, temperature-controlled crystallization, crystallization was completed, filtered, the filter cake was washed with isopropanol, dried, Axitinib-glutaric acid co-crystal was obtained with a purity of 99.52%.

Embodiment 2

[0044] Add about 0.4 g of axitinib and 0.13 g of glutaric acid to 120 ml of methanol / formic acid (V 甲醇 :V 甲酸 =2:1) ​​in the mixed solution, heated to 50-60 ℃ to dissolve, stirred and refluxed for 5 hours, then cooled to 10-15 ℃, temperature-controlled crystallization, crystallization was completed, filtered, the filter cake was washed with methanol, and dried to obtain Syntinib-glutaric acid co-crystal, purity 99.48%.

Embodiment 3

[0046] Add about 0.4 g of axitinib and 0.20 g of glutaric acid to 180 ml of ethanol / formic acid (V 乙醇 :V 甲酸 =5:1) in the mixed solution, heated to 65-70 ℃ to dissolve, stirred and refluxed for 5 hours, cooled to 20-30 ℃, temperature-controlled crystallization, crystallization was completed, filtered, the filter cake was washed with ethanol, and dried to obtain a Syntinib-formic acid-glutaric acid co-crystal, purity 99.46%.

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Abstract

The invention provides an axitinib glutaric acid eutectic crystal, and relates to the technical field of crystal form drug molecules. The eutectic is radiated by Cu-K alpha, and an X-ray diffraction spectrum represented by 2 theta has characteristic peaks at 7.78 + / -0.2 degrees, 13.01 + / -0.2 degrees, 13.83 + / -0.2 degrees, 19.29 + / -0.2 degrees, 20.30 + / -0.2 degrees, 23.98 + / -0.2 degrees and 26.04 + / -0.2 degrees; crystal measurement parameters are as follows: a triclinic system and a chiral space group are P-1; according to the invention, the crystal cell parameters are as follows: alpha is equal to 111.5610 (10) degrees, beta is equal to 91.4540 (10) degrees, gamma is equal to 94.1680 (10) degrees, and the related preparation method and application are provided. The axitinib glutaric acid eutectic crystal disclosed by the invention is good in stability and relatively high in solubility and permeability.

Description

technical field [0001] The invention relates to the technical field of crystal drug molecules, in particular to an axitinib-glutaric acid co-crystal. Background technique [0002] Axitinib is a white or off-white powder, and its chemical name is: 6-[2-(methylcarbamoyl)phenylsulfanyl]-3-E-[2-(pyridin-2-yl)ethene base]indazole, the molecular formula is C 22 H 18 N 4 OS, molecular weight is 386.48, CAS number is 319460-85-0, and the structure is as follows: [0003] [0004] The original manufacturer of axitinib is Pfizer, which was first approved by the FDA in the United States in January 2012. On April 29, 2015, axitinib was approved by the CFDA for adult patients with advanced renal cell carcinoma (RCC) who had failed prior therapy with a tyrosine kinase inhibitor or cytokine. Axitinib is currently listed in many countries, including the United States, Europe, Canada, Australia, South Korea, Japan, etc., and has become one of the standard treatment options for advanc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/06C07C55/12C07C51/41C07C51/43A61K31/4439A61P35/00
CPCC07D401/06C07C55/12C07C51/412C07C51/43A61P35/00C07B2200/13Y02P20/55
Inventor 翟立海张明明张朝花王聚聚
Owner LUNAN PHARMA GROUP CORPORATION
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