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Fidaxomicin crystal form I and preparation method thereof

A technology of fidaxomicin and crystal form, applied in the field of fidaxomycin crystal form I and preparation thereof, can solve problems such as poor crystal form stability, shortened product shelf life, etc., achieves low cost, short time consumption, avoids human body the effect of damage

Active Publication Date: 2014-06-25
NCPC NEW DRUG RES & DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

After research, it was found that the stability of the crystal form was poor, and after being stored at 40°C for 30 days, a degradation peak appeared in liquid chromatography detection, which shortened the shelf life of the product

Method used

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  • Fidaxomicin crystal form I and preparation method thereof
  • Fidaxomicin crystal form I and preparation method thereof
  • Fidaxomicin crystal form I and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Take 1 gram of fidaxomicin and dissolve it ultrasonically with 30 ml of n-heptane-methyl ethyl ketone (1:1) solution. After the dissolution is complete, place it at room temperature for 7 days. After drying for 1 hour, the crystalline form I of Fidaxomycin was obtained.

[0038] The XRD value of the prepared Fidaxomycin crystal form I is shown in Table 1, and the spectrum is as follows figure 1 As shown, the figure shows: in the X-ray powder diffraction diagram at 4.22°, 7.60°, 8.17°, 9.51°, 10.07°, 11.07°, 11.51°, 12.85°, 13.28°, 15.47°, 16.24°, 18.55° , 19.78°, 20.15°, 20.80°, 21.47°2θ have X-ray powder diffraction peaks.

[0039] The TGA and DSC spectra for detecting Fidaxomycin crystal form I are as follows: figure 2 shown.

[0040] Fidaxomycin crystal form I prepared by the present invention has X-ray powder diffraction characteristic peaks at 4.22°, 8.17°, 9.51°, 11.07°, 11.51°, 12.8°, 13.3°, 16.24°, 20.80° and 21.47°2θ , and there are no descriptions of thes...

Embodiment 2

[0042] Take 1 gram of fidaxomicin, dissolve it ultrasonically with 40 ml of 35% acetone aqueous solution, place it at 0°C for 5 days after the dissolution is complete, perform vacuum filtration after crystallization, and vacuum-dry the filter cake in a 40°C oven for 4 hours to obtain Fidaxomicin Form I.

Embodiment 3

[0044] Take 1 gram of fidaxomicin and dissolve it with 100 ml of isopropanol under heating at 50°C. After the dissolution is complete, cool to 10°C and crystallize for 24 hours. , and the filter cake was vacuum-dried in an oven at 40° C. for 6 hours to obtain crystalline form I of Fidaxomycin.

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Abstract

The invention discloses a fidaxomicin crystal form I and a preparation method thereof. An X-ray powder diffraction spectrum of the crystal form has X-ray powder diffraction peaks at 2theta of 4.22 degrees, 7.60 degrees, 8.17 degrees, 9.51 degrees, 10.07 degrees, 11.07 degrees, 11.51 degrees, 12.85 degrees, 13.28 degrees, 15.47 degrees, 16.24 degrees, 18.55 degrees, 19.78 degrees, 20.15 degrees, 20.80 degrees and 21.47 degrees. The crystal form provided by the invention is stable, simple in preparation method, strong in maneuverability, and applicable to industrial production.

Description

technical field [0001] The present invention relates to a crystal form of a compound and a crystallization method thereof, more precisely relates to crystal form I of fidaxomicin and a preparation method thereof. Background technique [0002] Fidaxomicin is a new macrolide antibiotic with an 18-membered ring structure produced by the fermentation of D. aurantiacus. It is mainly resistant to Gram-positive aerobic and anaerobic bacteria, Clostridium difficile, and also has good antibacterial effect on methicillin-resistant Staphylococcus aureus, Clostridium perfringens and Enterococcus. Fidaxomicin is mainly used clinically for the treatment of diseases caused by Clostridium difficile infection. It has the advantages of low tendency to develop resistance, long-lasting post-antibiotic effect, low cross-resistance and few adverse reactions. [0003] [0004] Fidaxomicin is a polymorphic compound, usually in the form of white needles, snowflake crystals or amorphous powder. ...

Claims

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Application Information

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IPC IPC(8): C07H17/08C07H1/06A61K31/7048A61P31/04
Inventor 任风芝张雪霞段宝玲陈书红李晓露佟杰王海燕李宁李丽红胡卫国
Owner NCPC NEW DRUG RES & DEV
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