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Morpholinidazole crystal and its preparation method and medical application

A morpholinidazole and crystal technology, which is applied in the field of morpholinidazole crystals and its preparation, can solve the problems of poor sensitivity of non-spore Gram-positive bacilli and the like, and achieve the effect of superior stability

Active Publication Date: 2017-07-25
JIANGSU HANSOH PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As a fungicide, metronidazole has a broad spectrum of anti-anaerobic bacteria, is highly sensitive to Bacteroides fragilis, Eubacterium, and Clostridium perfringens, and is resistant to Peptococcus, Peptostreptococcus, Previo melanogen, and porphyrin Moderately sensitive to monocysts, less sensitive to non-spore-forming gram-positive bacilli

Method used

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  • Morpholinidazole crystal and its preparation method and medical application
  • Morpholinidazole crystal and its preparation method and medical application
  • Morpholinidazole crystal and its preparation method and medical application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] (1) 20g of morpholinidazole crude product is dissolved in 20ml of sulfuric acid aqueous solution of 3mo / L, stirs 2h and reacts and becomes salt, then adds gac 2g decolouring 0.5h, filters;

[0033] (2) adjust the pH to 7.5 with the filtrate obtained in the previous step, and the morpholinidazole is free to become a base and separate out, and filter;

[0034] (3) Add the filter cake obtained in the previous step into 160ml of acetone, heat to 50°C, keep stirring for 0.5h, filter while it is hot, then cool to 30°C, stir and crystallize, filter, wash with ice water, and dry to obtain a yellow color Linidazole crystals 18g. After testing, the XRPD pattern of morpholinidazole crystal is as follows: figure 1 shown.

Embodiment 2

[0036] (1) 20g morpholinidazole crude product is dissolved in 20ml of aqueous nitric acid solution of 6mo / L, stirs 2h and reacts into salt, then adds gac 2g decolouring 0.5h, filters;

[0037] (2) adjust the pH to 8.0 with the filtrate obtained in the previous step, and the morpholinidazole is free to become a base and separate out, and filter;

[0038] (3) Add the filter cake obtained in the previous step into 200ml of acetone, heat to 55°C, keep stirring for 0.5h, filter while it is hot, then cool to 10°C, stir and crystallize, filter, wash with ice water, and dry to get yellow Linidazole crystals 18g. After testing, the XRPD pattern of morpholinidazole crystals is basically as follows: figure 1 shown.

Embodiment 3

[0040] (1) 20g of morpholinidazole crude product is dissolved in 20ml of aqueous hydrochloric acid solution of 6mo / L, stirs 2h and reacts into salt, then adds gac 2g decolouring 0.5h, filters;

[0041] (2) adjust the pH to 8.0 with the filtrate gained in the previous step, and the morpholinidazole is free to become a base and separate out, and filter;

[0042] (3) Add the filter cake obtained in the previous step into 200ml of acetone, heat to 55°C, keep stirring for 0.5h, filter while hot, then cool to 20°C, stir to crystallize, filter, wash with ice water, and dry to get yellow Linidazole crystals 19g. After testing, the XRPD pattern of morpholinidazole crystals is basically as follows: figure 1 shown.

[0043] 2. Stability research

[0044] The crystal form samples obtained in Example 1 were placed under high temperature (60°C), high humidity (25°C / RH92.5%), and light conditions for 30 days, and the crystal form detection results are shown in the table below:

[0045] ...

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Abstract

The invention discloses a morinidazole crystal and a preparation method and medical application thereof. Particularly, an x-ray powder diffraction pattern of the morinidazole crystal includes 2thelta characteristic peaks with the degrees of 10.2, 16.3, 17.3, 19.7, 21.7, 24.3, 27.2 and 29.5. The morinidazole crystal is high in stability and fluidity and suitable for pharmaceutical preparation requirements.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a crystal of morpholinidazole, a preparation method thereof and a medical application thereof. Background technique [0002] Chemotherapy for anaerobic infections usually begins with empirical therapy. Since most anaerobic infections are mixed infections with aerobic bacteria, the goal of chemotherapy must also consider the coexisting aerobic bacteria. The sensitivity of the main anaerobic bacteria to traditional chemotherapy drugs is listed in Table 1 below. [0003] Table 1 Sensitivity of anaerobic bacteria to chemotherapeutic drugs [0004] [0005] [0006] [Note] Sensitivity rate +++: 90%-100%; ++: 70%-89%; +: 50%-69%; -: <50% [0007] Drugs with strong antibacterial activity against most anaerobic bacteria include metronidazole, chloramphenicol, and imipenem / cilastat β-lactam antibiotic β-lactamase inhibitor mixture. [0008] Nitroimidazole antibiotics, the traditional c...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D233/95A61K31/5377A61P31/04A61P33/02
CPCC07D233/95
Inventor 吕爱锋王瑞军李琴王春玲
Owner JIANGSU HANSOH PHARMA CO LTD
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