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Antibacterial composition containing avibactam and meropenem and application thereof

A meropenem and multipurpose technology, applied in the field of medicine, can solve the problems of reduced clinical effectiveness, non-inhibitable metallo-beta-lactamases, and decreased bacterial sensitivity to drugs, etc.

Pending Publication Date: 2020-12-01
CHIA TAI TIANQING PHARMA GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The Journal of Third Military Medical University, 2013,13,35(23):2498-2501" points out that avibactam can inhibit group A (including ESBLs and KPC enzymes), group C (mainly AmpC enzyme) and part of group D β-lactamase (such as OXA-48), but usually can not inhibit metallo-β-lactamase of group B, the structure of avibactam is shown in formula I
However, due to its widespread use, the bacteria become less sensitive or even resistant to the drug, which reduces the clinical effectiveness.

Method used

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  • Antibacterial composition containing avibactam and meropenem and application thereof
  • Antibacterial composition containing avibactam and meropenem and application thereof
  • Antibacterial composition containing avibactam and meropenem and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Antibacterial activity of meropenem-avibactam

[0050] 1. Antibacterial drugs

[0051] Meropenem (trihydrate) and avibactam sodium were mixed in different concentration ratios (1:1, 2:1, 4:1, 8:1) and fixed concentrations of avibactam (2 μg / ml, 4 μg / ml , 8 μg / ml) mixed to determine the joint antibacterial activity.

[0052] 2. Test bacteria

[0053] Clinically isolated strains producing β-lactamase genotypes of KPC, NDM, OXA, IMP, and VIM.

[0054] 3. Experimental protocol

[0055] According to CLSI (Clinical and Laboratory Standards Institute) M07-A10 (2015 edition), the minimum inhibitory concentration of antibacterial drugs such as meropenem and avibactam against clinical isolates was determined by the Broth-micro dilution method. (MIC). The combined antibacterial activity of different concentrations and ratios was determined by 12×12 checkerboard dilution method (Checkerboard) combined with drug susceptibility test.

[0056] 3.1 Preparation of antibacterial dr...

Embodiment 2

[0077] Antibacterial activity of meropenem-avibactam

[0078] According to the method in Example 1, three groups of meropenem / avibactam concentration ratios of 1:1 and 2:1 and a fixed concentration of avibactam (4 μg / ml) were selected, and the total number of clinical strains below 1050 were determined. Antimicrobial Activity: MRSA, Staphylococcus aureus, Staphylococcus epidermidis, MRSA, MRSA, MRSA, MRSA, MRSA Staphylococcus, Enterococcus faecium, Vancomycin-resistant Enterococcus faecium, Enterococcus faecalis, Pseudomonas aeruginosa, Escherichia coli, Klebsiella pneumoniae, Enterobacter aerogenes, Enterobacter cloacae, carbapenems sensitive or resistant Acinetobacter baumannii, Burkholderia cepacia, Alcaligenes, Stenotrophomonas maltophilia), Haemophilus influenzae (Haemophilus parafluidus, Haemophilus influenzae β- Lactamase (-), Haemophilus influenzae β-lactamase (+)) Citrobacter freundii, Proteus mirabilis, Proteus vulgaris, Morganella morganii, Providencia sp., Serrat ...

Embodiment 3

[0098] Drug efficacy experiment in mice

[0099] 1. Antibacterial drugs

[0100] Get the corresponding medicines and prepare the following 6 groups of medicinal liquids with normal saline:

[0101] Table 5 drug groups

[0102]

[0103] 2. Test bacteria

[0104] Clinical strain of Klebsiella pneumoniae (provided by Huashan Hospital Affiliated to Fudan University);

[0105] 3. Experimental protocol

[0106] 3.1 Determination of Bacterial Toxicity

[0107] Each bacterium was diluted into serial concentrations, and 0.5 ml of ICR mice (body weight 20±2 g) were infected intraperitoneally, observed for 7 days, and the survival of the animals was observed. Results: Klebsiella pneumoniae clinical strain-26 was the most toxic (KPC-producing type).

[0108] 3.2 Determine the minimum lethal concentration (MLD) of the strain:

[0109] Klebsiella pneumoniae clinical strain 26 was diluted into serial concentrations, and 0.5 ml of ICR mice (body weight 20±2 g) were infected intraper...

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PUM

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Abstract

The invention belongs to the technical field of medicines. The invention relates to an antibacterial composition containing avibactam and meropenem and application thereof. Particularly, the inventionprovides application of avibactam or a pharmaceutically acceptable salt thereof and meropenem in preparation of a medicine for treating or preventing bacterial infection, in particular to applicationin preparation of medicines for treating infection caused by escherichia coli, pseudomonas aeruginosa, klebsiella pneumoniae, acinetobacter baumannii and enterobacter aerogenes, and aims to solve theproblem of drug resistance of carbapenem antibiotics.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular, the invention relates to an antibacterial composition containing avibactam and meropenem and its application. Background technique [0002] Avibactam (NXL-4) is a new type of β-lactamase inhibitor. The specificity of amidase production, Yang Fan et al. in "The new β-lactamase inhibitor avibactam and its compound preparation worth looking forward to. Journal of Third Military Medical University, 2013,13,35(23):2498-2501" It is pointed out that avibactam can inhibit group A (including ESBLs and KPC enzymes), group C (mainly AmpC enzyme) and some group D β-lactamases (such as OXA-48), but usually cannot inhibit the metal β-lactamases of group B Lactamase, the structure of avibactam is shown in formula I. [0003] [0004] Avibactam has almost no antibacterial activity, but combined with cephalosporin antibiotics can effectively restore or enhance its activity. The compound prep...

Claims

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Application Information

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IPC IPC(8): A61K31/439A61K31/407A61P31/04
CPCA61K31/439A61K31/407A61P31/04A61K2300/00Y02A50/30
Inventor 程兴栋唐晓闻徐文卫李其德张爱明田心张喜全朱袁兴
Owner CHIA TAI TIANQING PHARMA GRP CO LTD
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