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Anti-infective compound, preparations and application thereof

An anti-infection and composition technology, applied in the directions of antibacterial drugs, medical preparations containing active ingredients, organic active ingredients, etc., to achieve the effects of good tissue distribution, significant effect, and improved sensitivity

Pending Publication Date: 2018-09-07
THE SECOND XIANGYA HOSPITAL OF CENT SOUTH UNIV
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  • Abstract
  • Description
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Problems solved by technology

Moreover, the resistance of Klebsiella pneumoniae to colistin and tigecycline is also increasing year by year. [7，8] , polymyxin and aminoglycoside nephrotoxicity, and increased all-cause mortality in patients treated with tigecycline limit clinical application

Method used

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  • Anti-infective compound, preparations and application thereof
  • Anti-infective compound, preparations and application thereof
  • Anti-infective compound, preparations and application thereof

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Embodiment Construction

[0045] In vitro antibacterial activity verification of the present invention

[0046] 1. Isolation and identification of pathogenic bacteria

[0047] 1. Isolation of pathogenic bacteria

[0048] A total of 40 carbapenem-resistant Klebsiella pneumoniae (CRKP) strains isolated from different clinical patients (August 2016 to April 2017) were collected. CRKP passed the Phonenix Bacteria Identification Drug Susceptibility System (Becton Dickinson, USA) For identification, the strains were stored in a -80°C refrigerator for later use, and the American standard strains Escherichia coli ATCC 25922, Klebsiella pneumoniae ATCC BAA-1705 and BAA-1706 were used as quality control strains.

[0049] 2. In vitro sensitivity test

[0050] Initial drug susceptibility was verified by the Phonenix system, and the verified antibiotics were as follows: carbapenems (imipenem, meropenem), piperacillin / tazobactam, ampicillin, ampicillin / sulbactam, amoxicillin Penicillin / clavulanic acid, aminoglyco...

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Abstract

The invention belongs to the field of anti-infective medicines, and specifically discloses a cefepime and avibactam compound component for injection. The compound component is a mixture of cefepime and avibactam in a mass ratio of 8-1:1-8. The compound component has a good synergistic effect after mixing according to the above ratio, and the synergy rate of the cefepime and the avibactam is up to100%, which is better than other combinations; the sensitivity to drug-resistant bacteria can be significantly improved, MIC50 (>512 mcg / Ml) and MIC90 (>512 mcg / ml) of CRKP to the cefepime are reducedto MIC50 (4 mcg / ml) and MIC90 (32 mcg / ml), the activity is increased by 103 times and 16 times respectively, and the compound component greatly improves the effectiveness of drugs. Meanwhile, at least three molecules in the cefepime have tetravalent nitrogen atoms which can form zwitterions, the tissue distribution (especially brain tissues) is good, and the penetrating ability to an enterobacterium membrane is better than the same type of cephalosporin.

Description

technical field [0001] The invention relates to a compound prescription for treating drug-resistant bacteria infection such as carbapenem-resistant Klebsiella pneumoniae (CRKP). Background technique [0002] Klebsiella pneumoniae (Klebsiella pneumoniae, KP) belongs to Gram-negative enterobacteria, and is the most important group of bacteria in the genus Klebsiella. According to the "National Bacterial Resistance Surveillance Report 2015", Klebsiella pneumoniae ranks second in the detection rate of Gram-negative bacterial infections, accounting for 19.8%. It can cause severe infection through iatrogenic ways, and is a common conditional pathogen in clinical practice, mainly causing pneumonia, sepsis, urinary tract inflammation and other diseases. Since the first report of carbapenem-resistant Klebsiella pneumoniae (CRKP) in 1996, CRKP has gradually become prevalent in various regions, especially among people exposed to health care. And due to more and more invasive medical ...

Claims

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Application Information

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IPC IPC(8): A61K31/551A61K31/546A61P31/04
CPCA61K31/546A61K31/551A61P31/04A61K2300/00
Inventor 刘艺平向大雄王敏方平飞杨芳博向旭东胡敏曹伟赵程程
Owner THE SECOND XIANGYA HOSPITAL OF CENT SOUTH UNIV
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