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Sulbactam compound for treating infectious diseases, and preparation method therefor

A technology of infectious diseases and sulbactam sodium, which is applied in the field of medicine, can solve the problems of type I β-lactamase ineffectiveness, poor storage stability, and poor safety in use, and achieves low impurity content, high safety performance, and is not easy to treat. Hygroscopic effect

Inactive Publication Date: 2015-09-02
王雪雁
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The concentration of 2 μg / ml has a strong inhibitory effect on Richmond-Syks Ⅱ, Ⅲ, Ⅳ and Ⅴ type β-lactamases, but has no effect on I type β-lactamases
[0006] The storage stability of sulbactam sodium in the prior art is relatively poor, and its related substances will increase significantly in light and humid environments, and the long-term storage impurity content is relatively low high, poor safety in use, in order to obtain a sulbactam sodium compound with better performance, the present invention is proposed

Method used

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  • Sulbactam compound for treating infectious diseases, and preparation method therefor
  • Sulbactam compound for treating infectious diseases, and preparation method therefor
  • Sulbactam compound for treating infectious diseases, and preparation method therefor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1: Preparation of Sulbactam Sodium Crystals

[0032] 1) Take the crude product of sulbactam sodium, add it into a mixed solution of deionized water and methanol whose volume is 10 times the weight of sulbactam sodium at room temperature, the volume ratio of deionized water and methanol is 6.5:1, and stir until completely dissolve;

[0033] 2) join activated carbon Decolorize and filter to obtain a clear solution;

[0034] 3) Add dropwise a mixed solvent of ethanol and ethyl acetate whose volume is 3 times the weight of sulbactam sodium under stirring at a rotating speed of 10rmp. The volume ratio of ethanol and ethyl acetate is 1:2, and the dropping time is controlled for 10 minutes Add dropwise at a constant speed, after the drop is completed, stir and cool down. The stirring and cooling is to cool down to 0°C for 10 minutes under stirring at a rotating speed of 15rmp, then stand still for 15min, then cool down to -10°C for 30min under stirring at a rotati...

Embodiment 2

[0037] Example 2: Preparation of Sulbactam Sodium Crystals

[0038] 1) Take the crude product of sulbactam sodium, add it into a mixed solution of deionized water and methanol whose volume is 12 times the weight of sulbactam sodium at room temperature, and stir until completely dissolved at a volume ratio of 6.5:1 between deionized water and methanol ;

[0039] 2) join activated carbon Decolorize and filter to obtain a clear solution;

[0040] 3) Add dropwise a mixed solvent of ethanol and ethyl acetate whose volume is 5 times the weight of sulbactam sodium under stirring at a rotating speed of 12rmp. The volume ratio of ethanol and ethyl acetate is 1:2.5, and the dropping time is controlled for 12 minutes Add dropwise at a constant speed, after the drop is completed, stir and cool down. The stirring and cooling is to cool down to 5°C for 10 minutes under stirring at a rotating speed of 17rmp, stand still for 15min, then cool down to -5°C for 30min under stirring at a rot...

Embodiment 3

[0043] Example 3: Preparation of Sulbactam Sodium Crystals

[0044] 1) Take the crude product of sulbactam sodium, add it into a mixed solution of deionized water and methanol whose volume is 15 times the weight of sulbactam sodium at room temperature, the volume ratio of deionized water and methanol is 6.5:1, stir until completely dissolve;

[0045] 2) join activated carbon Decolorize and filter to obtain a clear solution;

[0046] 3) Add dropwise a mixed solvent of ethanol and ethyl acetate whose volume is 7 times the weight of sulbactam sodium under stirring at a rotating speed of 15rmp. The volume ratio of ethanol and ethyl acetate is 1:3.5, and the dropping time is controlled for 15 minutes Add dropwise at a constant speed, after dropping, stir to lower the temperature. The stirring and cooling is to cool down to 10°C for 10 minutes under stirring at a rotating speed of 20 rpm, and then stand still for 15 minutes, then cool down to 0°C for 30 minutes while stirring at ...

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Abstract

The invention discloses a sulbactam compound for treating infectious diseases, and belongs to the field of medical technology. The sulbactam compound is in the form of crystals and is measured through the X-ray diffraction (XRD) measurement process. Characteristic diffraction peaks appear at 8.8, 11.6, 12.4, 14.6, 16.5, 17.1, 17.7, 18.8, 19.1, 19.6, 21.5, 21.9, 23.4, 24.4, 25.3, 26.8, 27.1, 27.6, 28.0, 29.6, 30.6, 30.9, 31.7, 32.7, 33.2, 34.6, 35.6, 36.1, 37.0, 38.2, 40.2, 41.2, 41.9, 42.4, 43.6 and 44.2 parts of an X-ray powder diffraction spectrum, wherein the diffraction angle of the X-ray powder diffraction spectrum is within the range of 20+ / -0.2 degrees. The sulbactam compound and the preparation thereof are difficult in moisture absorption and stable in long-term storage, and greatly improves the medication safety.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a sulbactam sodium compound for treating infectious diseases. Background technique [0002] Sulbactam sodium Chinese alias: (2S,5R)-3,3-Dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate sodium- 4,4-Dioxide; (2S-CIS)-3,3-Dimethyl-7-oxo-4-thio-1-azabicyclo[3,2,0]heptane-2-carboxy Acid 4,4-dioxide sodium salt; English name Sulbactam Sodium; Molecular formula: C8H10NNaO5S; Molecular weight: 255.22; Molecular structural formula is as follows: [0003] [0004] Sulbactam sodium is an irreversible competitive β-lactamase inhibitor, which can inhibit the β-lactamase produced by Gram-positive and negative bacteria (except Pseudomonas aeruginosa), and has an irreversible reaction with the enzyme After the enzyme is inactivated, the activity of the enzyme cannot be restored after the inhibitor is removed. Sulbactam sodium has a strong and irreversible inhibit...

Claims

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Application Information

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IPC IPC(8): C07D499/86C07D499/18A61K31/43A61K9/14A61P31/04
CPCC07D499/86C07D499/18
Inventor 杨希文杨春雪
Owner 王雪雁
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