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Eutectic crystal of regorafenib and maleic acid and preparation method thereof

A technology of regorafenib and maleic acid, applied in the field of medicinal chemistry, can solve the problems of poor water solubility of regorafenib monohydrate, high price of regorafenib, and limitations in clinical application, and achieve good reproducibility, The effect of easy control of the crystallization process and high apparent solubility

Active Publication Date: 2020-11-27
TIANJIN UNIVERSITY OF TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the water solubility of regorafenib monohydrate is poor, which limits its application in formulations
In addition, the imported regorafenib marketed in China is expensive, and many patients cannot bear it, which further limits its clinical application.

Method used

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  • Eutectic crystal of regorafenib and maleic acid and preparation method thereof
  • Eutectic crystal of regorafenib and maleic acid and preparation method thereof
  • Eutectic crystal of regorafenib and maleic acid and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Weigh 1000 mg regorafenib and 240 mg maleic acid, add 20 mL n-heptane and 80 μL methanol 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 Rui A solid sample of the cocrystal of gorfenib and maleic acid with a yield of 90.7%.

Embodiment 2

[0037] Weigh 60 mg of regorafenib and 14.4 mg of maleic acid, add 2 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 A solid sample of the cocrystal of regorafenib and maleic acid.

Embodiment 3

[0039] Weigh 60mg of regorafenib and 14.4mg of maleic acid, add 2mL of dichloromethane to obtain a suspension, stir the suspension at room temperature for 48h, filter, and dry the obtained white solid at 40°C to obtain regorafenib Solid sample of Ni and maleic acid cocrystal.

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Abstract

The invention discloses a eutectic crystal of regorafenib and maleic acid and a preparation method thereof. The molar ratio of regorafenib to maleic acid in the eutectic crystal is 1: 1, and an X-raypowder diffraction pattern of the eutectic crystal has characteristic peaks when the 2theta values are 5.9 + / -0.2 degrees, 9.6 + / -0.2 degrees, 11.6 + / -0.2 degrees, 12.4 + / -0.2 degrees, 21.3 + / -0.2 degrees and 25.6 + / -0.2 degrees. The eutectic crystal preparation method provided by the invention is simple in process, easy in control of the crystallization process, good in reproducibility and suitable for industrial production. Compared with the regorafenib monohydrate, the eutectic crystal has higher apparent solubility, and is beneficial to improving the oral absorption efficiency of regorafenib.

Description

technical field [0001] The invention relates to the technical field of medicinal chemistry, in particular to a co-crystal of regorafenib and maleic acid and a preparation method thereof. Background technique [0002] Pharmaceutical active ingredients usually exist in crystalline forms, such as polymorphs, hydrates, solvates, salts, and co-crystals. For the same active pharmaceutical ingredient, different crystalline forms have different physicochemical properties. Therefore, obtaining a suitable crystalline form of a drug is of great importance in the pharmaceutical industry. The drug exists in the form of co-crystal, which can improve the stability, solubility and processability of the active ingredient of the drug, and has significant advantages. Therefore, pharmaceutical co-crystals are an effective means to improve the physicochemical properties of pharmaceutical active ingredients. [0003] The chemical name of Regorafenib is 4-{4-[({[4-chloro-3-(trifluoromethyl)phen...

Claims

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Application Information

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IPC IPC(8): C07D213/81C07C51/43C07C57/145A61K31/44A61P35/00
CPCA61K31/44A61P35/00C07C57/145C07D213/81
Inventor 陈嘉媚贾军龙戴霞林
Owner TIANJIN UNIVERSITY OF TECHNOLOGY
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