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Amorphous crystal form of voriconazole disodium phosphate

A technology of voriconazole disodium phosphate and voriconazole phosphate, which is applied in the field of pharmaceutical crystal forms, and can solve the problems of amorphous voriconazole disodium phosphate, etc.

Inactive Publication Date: 2018-02-02
天地人和生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

At present, there is no literature report on amorphous voriconazole disodium phosphate

Method used

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  • Amorphous crystal form of voriconazole disodium phosphate
  • Amorphous crystal form of voriconazole disodium phosphate
  • Amorphous crystal form of voriconazole disodium phosphate

Examples

Experimental program
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Embodiment 1

[0048] The preparation of embodiment 1 amorphous voriconazole phosphate disodium

[0049] Take 10g of voriconazole disodium phosphate, add 70ml of ethanol: isopropanol (1:9), heat to dissolve at 60°C, filter, freeze at -20°C for static crystallization, filter, and blow dry at 20-30°C to obtain voriconazole phosphate Disodium amorphous crystal form, moisture 24.8%, powder X-ray diffraction pattern see figure 1 .

Embodiment 2

[0050] Example 2 Preparation of Amorphous Voriconazole Disodium Phosphate

[0051] Take voriconazole disodium phosphate 10g, add N,N-dimethylformamide: isopropanol (1:9) 100ml, heat to dissolve at 60°C, filter, stir and crystallize at 0°C, filter, and blow dry at 20-30°C , to obtain voriconazole disodium phosphate amorphous crystal form, moisture 20.1%, powder X-ray diffraction pattern see figure 2 .

Embodiment 3

[0052] Example 3 Preparation of Amorphous Voriconazole Disodium Phosphate

[0053] Take 10g of voriconazole disodium phosphate, add 50ml of ethanol:ethyl acetate (1:5), heat to dissolve at 60°C, filter, freeze at -20°C and stir to crystallize, filter, and blow dry at 20-30°C to obtain voriconazole phosphate di Sodium amorphous crystal form, moisture 25.1%, powder X-ray diffraction pattern see image 3 .

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Abstract

The invention discloses an amorphous crystal form of voriconazole disodium phosphate. The chemical purity and the crystal form purity of the amorphous voriconazole disodium phosphate are both lager than 98%. In addition, the invention also discloses a preparation method of the amorphous voriconazole disodium phosphate, and further discloses a pharmaceutical composition containing the amorphous voriconazole disodium phosphate and an application of the composition in preparing medicines for treating fungal infection.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical crystal forms, and relates to the discovery of a new crystal form of amorphous voriconazole disodium phosphate; more specifically, it relates to an amorphous voriconazole disodium phosphate, a preparation method thereof and a pharmaceutical composition. Background technique [0002] Voriconazole is a broad-spectrum triazole antifungal agent indicated for the following: treatment of invasive aspergillosis, treatment of severe invasive infections caused by fluconazole-resistant Candida species (including Candida krusei), treatment of Severe infections caused by Actinomycetes and Fusarium species This product should be used primarily for the treatment of progressive, potentially life-threatening infections in immunocompromised patients. Voriconazole phosphate is the prodrug of voriconazole, which can be rapidly hydrolyzed into voriconazole in the body to take effect. Since voriconazole has v...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/6558A61K31/675A61P31/10
CPCC07B2200/13C07F9/65583
Inventor 张起愿刘晓鹏
Owner 天地人和生物科技有限公司
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