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A kind of lenvatinib and p-hydroxybenzoic acid co-crystal and preparation method thereof

A technology of p-hydroxybenzoic acid and lenvatinib, applied in the field of medicinal chemistry, can solve the problems of poor water solubility of lenvatinib mesylate, difficulty in preparation process development, and limitations in clinical application, and achieve good reproducibility , the crystallization process is easy to control, and the effect of large apparent solubility

Active Publication Date: 2021-12-28
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 general patients, which limits clinical application, and the water solubility of lenvatinib mesylate is poor, making the preparation process development difficult

Method used

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  • A kind of lenvatinib and p-hydroxybenzoic acid co-crystal and preparation method thereof
  • A kind of lenvatinib and p-hydroxybenzoic acid co-crystal and preparation method thereof
  • A kind of lenvatinib and p-hydroxybenzoic acid co-crystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Weigh 60 mg of lenvatinib and 19.4 mg of p-hydroxybenzoic acid, add 1 mL of ethyl acetate to obtain a suspension, stir the suspension at room temperature for 36 hours, filter, and dry the obtained white solid at 50°C to obtain lenvatinib A solid sample of the co-crystal of tinib and p-hydroxybenzoic acid.

Embodiment 2

[0052] Weigh 60 mg of lenvatinib and 19.4 mg of p-hydroxybenzoic acid, add 1 mL of methyl acetate to obtain a suspension, stir the suspension at room temperature for 36 hours, filter, and dry the obtained white solid at 50°C to obtain lenvatinib A solid sample of the co-crystal of tinib and p-hydroxybenzoic acid.

Embodiment 3

[0054] Weigh 30 mg of lenvatinib and 48.5 mg of p-hydroxybenzoic acid, add 1 mL of acetonitrile to obtain a suspension, stir the suspension at room temperature for 36 hours, filter, and dry the obtained white solid at 50 ° C to obtain lenvatinib Solid sample co-crystallized with p-hydroxybenzoic acid.

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Abstract

The invention discloses a co-crystal of lenvatinib and p-hydroxybenzoic acid and a preparation method thereof. This co-crystal contains lenvatinib and p-hydroxybenzoic acid in a molar ratio of 1:1; the X-ray powder diffraction pattern of the co-crystal measured with Cu Kα rays is 6.3±0.2°, 10.6±0.2 °, 12.4±0.2°, 14.6±0.2°, 17.5±0.2°, 18.4±0.2° have characteristic peaks. The present invention converts lenvatinib into a brand-new co-crystal of lenvatinib and p-hydroxybenzoic acid for the first time, and the co-crystal of lenvatinib and p-hydroxybenzoic acid has a faster dissolution rate and a larger apparent Solubility. The preparation method of the co-crystal of lenvatinib and p-hydroxybenzoic acid has simple process, easy control of the crystallization process, good reproducibility, is suitable for industrial production, and has broad application prospects.

Description

technical field [0001] The invention relates to the technical field of medicinal chemistry, in particular to a co-crystal of lenvatinib and p-hydroxybenzoic 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. Drugs exist in the form of co-crystals, which can have significant advantages in improving the stability, solubility and dissolution rate of active ingredients of drugs. Therefore, pharmaceutical co-crystals are usually an effective means to improve the physical and chemical properties of pharmaceutical active ingredients. [0003] The chemical name of Lenvatinib is 4-[3-chloro-4-(cycl...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D215/48C07C51/43C07C65/03A61K31/47A61P35/00A61P29/00
CPCC07D215/48C07C51/43C07C65/03A61P35/00A61P29/00C07B2200/13
Inventor 陈嘉媚吕文婷
Owner TIANJIN UNIVERSITY OF TECHNOLOGY
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