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Levorotatory morinidazole crystal form and preparation method thereof and application of medicinal composition of levorotatory morinidazole crystal form

A technology of levomorphinidazole and morpholinidazole, its application in the treatment of anaerobic infection and various other diseases, the application of crystal forms in pharmaceutical compositions, the crystal form of levomorphinidazole and its In the field of preparation, it can solve problems that affect the stability, solubility, and clinical efficacy of pharmaceutical preparations

Inactive Publication Date: 2017-05-24
HC SYNTHETIC PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Levomorphinidazole is the left-handed form of Morpholinidazole. There is no relevant literature report on the crystal form of Levomorphinidazole. For medicines, different crystal forms may have different physical and chemical properties, such as solubility, melting point, and stability. These properties will directly affect the stability and solubility of pharmaceutical preparations, and even affect the most important clinical curative effect

Method used

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  • Levorotatory morinidazole crystal form and preparation method thereof and application of medicinal composition of levorotatory morinidazole crystal form
  • Levorotatory morinidazole crystal form and preparation method thereof and application of medicinal composition of levorotatory morinidazole crystal form
  • Levorotatory morinidazole crystal form and preparation method thereof and application of medicinal composition of levorotatory morinidazole crystal form

Examples

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Comparison scheme
Effect test

Embodiment 1

[0034] Example 1: Preparation of morpholinidazole crystal form

[0035] Take 10g of Levomorpholinidazole, add 50ml of ethyl acetate, heat to 60℃ and stir to dissolve, then add 0.5g of activated carbon to decolor, keep stirring for 30 minutes and filter, the filtrate will crystallize at 20℃, filter, and dry to obtain 9.2g Levo Morpholinidazole, yield 92%, X-ray powder diffraction pattern (XRPD) as figure 1 Shown.

Embodiment 2

[0036] Example 2: Preparation of morpholinidazole crystal form

[0037] Take 10g of Levomorpholinidazole, add 50ml of ethanol, heat to 60℃ and stir to dissolve, then add 0.1g activated carbon to decolor, keep stirring for 60 minutes and filter, the filtrate is crystallized at -20℃, filtered, and dried to obtain 9.4g Levomorph Linnidazole, the yield is 94%, the X-ray powder diffraction pattern (XRPD) is as figure 2 Shown.

Embodiment 3

[0038] Example 3: Preparation of L-morpholinidazole crystal form

[0039] Take 10g of Levomorpholinidazole, add 50ml of methanol, heat to 60℃ and stir to dissolve, then add 0.5g of activated carbon for decolorization, keep stirring for 20 minutes and filter, the filtrate will stand at 0℃ to crystallize, filter and dry to obtain 8.9g Levo Morpholinidazole, the yield is 89%, the X-ray powder diffraction pattern (XRPD) is as image 3 Shown.

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Abstract

The invention provides a levorotatory morinidazole crystal form and further provides a preparation method of the levorotatory morinidazole crystal form. Besides, a medicinal composition containing the levorotatory morinidazole crystal form is used for resisting to anaerobic bacteria or trichomonas or amebic protozoa.

Description

Technical field [0001] The invention belongs to the technical field of chemical drug crystallization, and particularly relates to a crystal form of L-morpholinidazole and a preparation method thereof. The invention also relates to the application of a crystal form of L-morpholinidazole in a pharmaceutical composition and the application of the crystal form and composition in the treatment of anaerobic infections and various other diseases. Background technique [0002] Nitroimidazole antibacterial drugs, the traditional compounds are metronidazole, ornidazole and secnidazole. Metronidazole, as a fungicide, has a broad spectrum of anti-anaerobic bacteria, and is highly sensitive to Bacteroides fragilis, Eubacteria, Clostridium perfringens, and peptococcus, peptostreptococcus, melanophora, porphyrin The monospores are moderately sensitive, but are less sensitive to non-spore Gram-positive bacilli. Tinidazole (tinidazole) has the same antibacterial spectrum and antibacterial effec...

Claims

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Application Information

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IPC IPC(8): C07D233/95A61K31/5377A61P31/04A61P33/02
CPCC07B2200/13C07D233/95
Inventor 张起愿
Owner HC SYNTHETIC PHARMA CO LTD