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Eutectic crystal of lenvatinib and benzoic acid, and preparation method thereof

A technology of lenvatinib and benzoic acid, applied in the field of medicinal chemistry, can solve the problems of limited clinical application, poor water solubility of lenvatinib mesylate, high cost, etc.

Active Publication Date: 2020-10-20
TIANJIN UNIVERSITY OF TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Most of the lenvatinib currently used in China is imported, which is expensive and unaffordable for ordinary patients, which limits clinical application
In addition, lenvatinib mesylate has poor water solubility and has certain hygroscopicity, so the threshold for preparation process development is high and the cost is relatively high

Method used

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  • Eutectic crystal of lenvatinib and benzoic acid, and preparation method thereof
  • Eutectic crystal of lenvatinib and benzoic acid, and preparation method thereof
  • Eutectic crystal of lenvatinib and benzoic acid, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Weigh 600 mg of lenvatinib and 172 mg of benzoic acid, add 4 mL of acetonitrile and 4 mL of water to obtain a suspension, stir the suspension at room temperature for 1 h, filter, and dry the resulting white solid at 50 ° C to obtain lenvatinib and Solid sample of benzoic acid co-crystal, yield 88.2%.

Embodiment 2

[0042] Weigh 60 mg of lenvatinib and 17.2 mg of benzoic acid, add 1 mL of anisole to obtain a suspension, stir the suspension at room temperature for 12 hours, filter, and dry the obtained white solid at 50°C to obtain lenvatinib Solid sample co-crystallized with benzoic acid.

Embodiment 3

[0044] Weigh 60 mg of lenvatinib and 17.2 mg of benzoic acid, add 10 μL of isopropanol, grind for 30 min at a frequency of 20 Hz, and dry the resulting white solid at 40 ° C to obtain a solid sample of lenvatinib and benzoic acid co-crystal.

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Abstract

The invention discloses a lenvatinib and benzoic acid eutectic crystal and a preparation method thereof, wherein in the eutectic crystal, the molar ratio of lenvatinib to benzoic acid is 1:1, and theeutectic X-ray powder diffraction pattern has characteristic peaks when the 2theta values are 6.4+ / -0.2 degrees, 7.4+ / -0.2 degrees, 12.5+ / -0.2 degrees, 14.7+ / -0.2 degrees, 16.7+ / -0.2 degrees, 17.7+ / -0.2 degrees and 23.8+ / -0.2 degrees. According to the invention, the eutectic preparation method is simple in process, easy to control the crystallization process, good in reproducibility and suitable for industrial production; and compared with lenvatinib mesylate, the eutectic crystal of the invention has low hygroscopicity, high dissolution rate and high apparent solubility, and provides a material basis for improving the stability and oral absorption efficiency of lenvatinib and reducing the process threshold and cost of a preparation.

Description

technical field [0001] The invention relates to the technical field of medicinal chemistry, in particular to a co-crystal of lenvatinib and benzoic 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 pharmaceutical active ingredient, different crystalline forms have different physical and chemical 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, which 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 Lenvatinib is 4-[3-chloro-4-(cyclopropylaminocar...

Claims

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Application Information

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IPC IPC(8): C07D215/48C07C63/06A61P35/00A61P9/00C07C51/43
CPCA61P9/00A61P35/00C07B2200/13C07C63/06C07D215/48
Inventor 陈嘉媚吕文婷
Owner TIANJIN UNIVERSITY OF TECHNOLOGY
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