Lenvatinib and p-hydroxybenzoic acid eutectic 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, difficult formulation process development, clinical application limitations, etc., and achieves good reproducibility , the crystallization process is easy to control, the effect of large apparent solubility

Active Publication Date: 2020-06-05
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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  • Lenvatinib and p-hydroxybenzoic acid eutectic crystal and preparation method thereof
  • Lenvatinib and p-hydroxybenzoic acid eutectic crystal and preparation method thereof
  • Lenvatinib and p-hydroxybenzoic acid eutectic 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 lenvatinib and p-hydroxybenzoic acid eutectic crystal and a preparation method thereof. The eutectic crystal comprises lenvatinib and p-hydroxybenzoic acid in a molar ratio of 1: 1, an X-ray powder diffraction pattern of the eutectic crystal measured by Cu K alpha rays has characteristic peaks when diffraction angles 2theta are 6.3+/-0.2 degrees, 10.6+/-0.2 degrees, 12.4+/-0.2 degrees, 14.6+/-0.2 degrees, 17.5+/-0.2 degrees and 18.4+/-0.2 degrees. According to the preparation method, the lenvatinib is converted into a brand-new lenvatinib and p-hydroxybenzoic acid eutectic crystal for the first time, and the lenvatinib and p-hydroxybenzoic acid eutectic crystal has a relatively high dissolution rate and relatively high apparent solubility. The preparation method of the lenvatinib and p-hydroxybenzoic acid eutectic crystal is simple in process, easy to control the crystallization process, good in reproducibility, suitable for industrial production and wide in application prospect.

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 Applications(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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