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Crystal form of Crisabole solvate and preparation method and application of crystal form

A solvate, solvation technology, applied in organic chemistry methods, chemical instruments and methods, active ingredients of boron compounds, etc., can solve problems such as water solubility and low stability

Pending Publication Date: 2021-11-09
SOLIPHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] At present, there is still a need to develop new crystal forms to solve the problems of water solubility and low stability of Crisaborole solvates in the preparation of pharmaceutical preparations.

Method used

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  • Crystal form of Crisabole solvate and preparation method and application of crystal form
  • Crystal form of Crisabole solvate and preparation method and application of crystal form
  • Crystal form of Crisabole solvate and preparation method and application of crystal form

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0093] Take about 90mg of Crisaborole crystal form, add 1.5mg of pyridine, heat up to 60°C to dissolve to obtain solution 1; take about 6mg of polyethylene glycol, add 4.5mL of water to dissolve to obtain solution 2; add solution 2 dropwise to solution 1 , precipitated solid, continued to stir overnight, and centrifuged to obtain FB-2.

[0094] The samples of Example 1 were taken for characterization, as follows.

[0095] 1. XRPD spectrum analysis

[0096] figure 1 is the XRPD pattern of FB-2, Table 1 shows the X-ray powder diffraction data of FB-2.

[0097] Table 1: X-ray powder diffraction data for FB-2

[0098]

[0099]

[0100] 2. TGA spectrum analysis

[0101] TGA (thermogravimetric analysis) results such as figure 2 shown. It has a weight loss step before 75°C, the weight loss rate is 11.3%, and its decomposition temperature is 273°C.

[0102] 3. DSC spectrum analysis

[0103] The results of differential calorimetry scanning analysis were as follows: ima...

Embodiment 2

[0111] Take about 30mg of Crisaborole, add 0.5mL of pyridine, heat up to 60°C to dissolve, add dropwise 1.5mL of water, precipitate a solid, and continue stirring overnight to obtain FB-2.

Embodiment 3

[0113] Take about 90mg of Crisaborole, add 0.8mL of pyridine and 2mL of water, dissolve at 60°C and filter, keep the filtrate for 20min, then place the filtrate at 4°C and stir overnight, and the solid precipitates to obtain FB-2.

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Abstract

The invention discloses a crystal form of a Crisabole solvate and a preparation method and application of the crystal form. The crystal form has better water solubility, and the significantly improved water solubility is helpful for improving the bioavailability of the medicine, thereby improving the druggability and efficacy of the medicine. In addition, a preparation prepared from the crystal form has relatively good stability, and particularly has high crystal form stability in a pharmaceutical preparation taking pyridine or 1, 3-propylene glycol as an auxiliary material.

Description

technical field [0001] The present invention relates to the technical field of pharmaceutical crystals, in particular to the crystal form of solvate of crisaborole (sometimes referred to herein as "Crisaborole" or "Crisaborole") and its preparation method and application. Background technique [0002] Among skin inflammation-related diseases, psoriasis and atopic dermatitis (AD), especially atopic dermatitis has a familial tendency to be susceptible to asthma, allergic rhinitis, and eczema, while being allergic to foreign proteins and increasing blood eosinophils , is a chronic, relapsing inflammatory skin disease, and some patients are often combined with other atopic diseases such as allergic asthma, allergic rhinitis, and allergic conjunctivitis. In recent years, although many breakthroughs have been made in clinical treatment, the development of related drugs still faces many challenges. [0003] In December 2016, the US Food and Drug Administration (FDA) approved Anaco...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F5/02C07D213/16A61K31/69A61P29/00A61P17/06A61P17/00
CPCC07F5/025C07D213/16A61P29/00A61P17/06A61P17/00C07B2200/13
Inventor 盛晓红盛晓霞吴涛吕康乐胡晨阳
Owner SOLIPHARMA
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