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Axitinib vanillic acid eutectic salt and preparation thereof

A technology of axitinib and co-, axitinib, applied in the direction of carboxylate preparation, medical preparations containing active ingredients, separation/purification of carboxylic acid compounds, etc., can solve the problem of inability to judge the mode of action of API and CCF, No problems such as the structural information of the resveratrol complex are given, and the effects of good photostability, regular crystal form, and uniform particle size are achieved

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 vanillic acid eutectic salt and preparation thereof
  • Axitinib vanillic acid eutectic salt and preparation thereof
  • Axitinib vanillic acid eutectic salt and preparation thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0043] Add about 0.8g axitinib, 0.27g vanillic acid to 120ml ethanol / formic acid / water (V 乙醇 :V 甲酸 :V 水 =5:2:1) in the mixed solution, heated to 65-70 °C to dissolve, stirred and refluxed for 5 hours, cooled to 10-15 °C, temperature-controlled crystallization, crystallization was completed, filtered, the filter cake was washed with ethanol, dried, Axitinib-vanillic acid co-crystal salt was obtained, with a purity of 99.55%.

Embodiment 2

[0045] Add about 0.8g axitinib and 0.17g vanillic acid to 100ml methanol / formic acid / water (V 甲醇 :V 甲酸 :V 水 =1:1:1) in the mixed solution, heated to 60~65℃ to dissolve, stirred and refluxed for 6 hours, then cooled to 15~20℃, temperature controlled for crystallization, crystallization was completed, filtered, the filter cake was washed with methanol, dried, Axitinib-vanillic acid co-crystal salt was obtained, with a purity of 99.52%.

Embodiment 3

[0047] Add about 0.8g axitinib, 0.34g vanillic acid to 160ml isopropanol / formic acid / water (V 异丙醇 :V 甲酸 :V 水 =10:3:1) in the mixed solution, heated to 60~70 ℃ to dissolve, stirred and refluxed for 3 hours, cooled to 20~30 ℃, temperature controlled crystallization, crystallization was completed, filtered, and the filter cake was washed with isopropanol, After drying, axitinib-vanillic acid co-crystal salt was obtained with a purity of 99.48%.

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Abstract

The invention provides axitinib-vanillic acid eutectic salt, and relates to the technical field of crystal form drug molecules. The eutectic salt is radiated by Cu-K alpha, and an X-ray diffraction spectrum represented by 2 theta has characteristic peaks at 7.94 + / -0.2 degrees, 9.38 + / -0.2 degrees, 11.96 + / -0.2 degrees, 12.89 + / -0.2 degrees, 16.53 + / -0.2 degrees, 17.20 + / -0.2 degrees and 27.03 + / -0.2 degrees; crystal measurement parameters are as follows: a triclinic system and a space group are P-1; the cell parameters are as follows: alpha is equal to 68.228 (2) degrees, beta is equal to 65.302 (3) degrees, gamma is equal to 73.341 (3) degrees, and the related preparation method and application are provided. The axitinib-vanillic acid eutectic salt 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-vanillic acid co-crystal salt. 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 a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/06C07C65/21C07C51/41C07C51/43A61P35/00A61K31/4439
CPCC07D401/06C07C65/21A61P35/00C07B2200/13
Inventor 张明明翟立海许秀艳余军厚
Owner LUNAN PHARMA GROUP CORPORATION
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