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Idelalisib amorphous substance and preparation method thereof

An amorphous and spectroscopic technology, used in drug combinations, antipyretics, antitumor drugs, etc., can solve problems such as large doses, unsuitable for medicinal use, and achieve good dispersion, good physical stability and chemical stability. , the effect of fast dispersion

Inactive Publication Date: 2015-09-09
SHANGHAI FANGNAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The crystal form of Adelibu tablets listed is the mixed crystal form of Form I and Form II. The dose of the drug is 100 mg and 150 mg. As an anti-tumor drug, the dose of the drug is relatively large. The patent The other four crystal forms are solvates, which are not suitable for pharmaceutical use

Method used

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  • Idelalisib amorphous substance and preparation method thereof
  • Idelalisib amorphous substance and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Suspend Adlib (50 mg) in tetrahydrofuran (750 μl) and stir to dissolve at room temperature. The above solution was added to n-heptane (10 ml) cooled to -25°C, a white solid was precipitated under stirring, filtered, and dried to obtain 45 mg of a solid, and the X-ray powder diffraction pattern was as follows: figure 1 As shown, there is no sharp diffraction peak in the X-ray powder diffraction spectrum represented by degree 2θ, and there are two broad peaks between 2.0 and 50.0 in degree 2θ.

Embodiment 2

[0045] Suspend Adlib (50 mg) in dichloromethane (750 μl) and stir to dissolve at room temperature. The above solution was added to n-heptane (10 ml) cooled to -80°C, a white solid was precipitated under stirring, filtered, and dried to obtain 47 mg of a solid, ie, the amorphous form of Adlib.

Embodiment 3

[0047]Suspend Adlib (30 mg) in N,N-dimethylformamide (90 μl) and stir to dissolve at room temperature. The above solution was added to water (450 microliters) heated to 80°C, and a white solid was precipitated under stirring, which was filtered and dried to obtain 27 mg of a solid, ie the amorphous form of Adlib.

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Abstract

The invention relates to an idelalisib amorphous substance and a preparation method thereof. According to the invention, Cu-Kalpha radiation is used, no sharp diffraction peak in a spectrum is diffracted by X-ray powder expressed by degree 2 theta, wherein X-ray powder diffraction is shown in a graph 1. The invention also provides a preparation method of the idelalisib amorphous substance. The idelalisib amorphous substance increase the dissolvability of idelalisib and is in favor of increasing the biological utilization degree of a medicinal preparation, compared with current crystal form idelalisib, solubility is obviously increased, the idelalisib amorphous substance is in favor of absorbing the medicines by the body, so that medicine can better perform clinical disease treatment effect. Under the condition of accelerated testing on the idelalisib amorphous substance, good physical stability and chemical stability can be kept. The preparation method of the idelalisib amorphous substance has the advantages of simple operation and easy realization.

Description

technical field [0001] The invention relates to an amorphous substance of Adlib and a preparation method thereof. Background technique [0002] Idelalisib, the chemical name is 5-fluoro-3-phenyl-2-[(1S)-1-(9H-purin-6-ylamino)propyl]-4(3H)-quinazole Phenone, its structure is shown in formula (I): [0003] [0004] Adlib (trade name Zydelig) is a selective phosphoinositide 3-kinase delta (PI3K-delta, P110-delta) inhibitor developed by Gilead Science. On July 23, 2014, the U.S. Food and Drug Administration (FDA) approved three indications of Adlib: in combination with rituximab (Rituxan) for the treatment of relapsed chronic lymphocytic leukemia (CLL), as a monotherapy Drug therapy for relapsed follicular B-cell non-Hodgkin's lymphoma (FL) and relapsed small lymphocytic lymphoma (SLL). The FDA has accelerated approval for the latter two indications, and the patients have received at least two previous systemic treatments. [0005] Adlib is the first marketed oral, select...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D473/34
CPCC07D473/34A61P29/00A61P35/00A61P37/00
Inventor 熊志刚资春鹏胡涛张席妮
Owner SHANGHAI FANGNAN PHARMA
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