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Antibacterial agent and beta-lactam enzyme inhibitor composition and application thereof

A technology of lactamase and composition, which is applied in the direction of antibacterial drugs, drug combinations, active ingredients of heterocyclic compounds, etc., to achieve the effect of solving the drug resistance of mezlocillin and enhancing the bactericidal effect

Inactive Publication Date: 2019-12-20
REYOUNG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The technical problem solved by the present invention is: to overcome the deficiencies in the prior art, provide a kind of antibacterial agent and β-lactamase inhibitor composition, protect mezlocillin from being hydrolyzed by β-lactamase, enhance its bactericidal effect, solve The problem of bacterial resistance to mezlocillin is solved; meanwhile, the present invention also provides its application, which can be used to prepare mezlocillin-sensitive bacteria and the respiratory system, urinary system, digestive system, gynecological and Drugs for Genital Infections

Method used

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  • Antibacterial agent and beta-lactam enzyme inhibitor composition and application thereof
  • Antibacterial agent and beta-lactam enzyme inhibitor composition and application thereof
  • Antibacterial agent and beta-lactam enzyme inhibitor composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] The antibacterial agent and β-lactamase inhibitor composition comprises the following components in mass percentage: 80% of mezlocillin sodium; 20% of avibactam sodium.

[0021] Preparation:

[0022] (1) Weighing ingredients

[0023] Take avibactam sodium and mezlocillin sodium respectively by prescription quantity;

[0024] (2) mixed

[0025] Add all the avibactam sodium into the mixer, and then add a part of mezlocillin sodium in equal increments, the amount added is 25% of the total mass of mezlocillin sodium, set the speed of the mixer to 10rpm, mix for 10min, and then add the remaining Measure mezlocillin sodium, keep the rotating speed and continue mixing for 15 minutes to obtain mixed powder;

[0026] (3) Aseptic packaging

[0027] According to the content of the mixed powder, the theoretical loading volume is converted, and the aseptic packaging is carried out. Press C 21 h 25 N 5 o 8 S 2 Calculate repackable specifications such as:

[0028] 0.1g, 0.5...

Embodiment 2

[0031] The antibacterial agent and β-lactamase inhibitor composition comprises the following components in mass percentage: 75% of mezlocillin sodium; 25% of avibactam sodium.

[0032] Preparation:

[0033] (1) Weighing ingredients

[0034] Take avibactam sodium and mezlocillin sodium respectively by prescription quantity;

[0035] (2) mixed

[0036] Add all the avibactam sodium into the mixer, then add part of the mezlocillin sodium in an equal amount, the amount added is 33.33% of the total mass of the mezlocillin sodium, set the speed of the mixer to 10rpm, mix for 10min, and then add the remaining Measure mezlocillin sodium, keep the rotating speed and continue mixing for 15 minutes to obtain mixed powder;

[0037] (3) Aseptic packaging

[0038] According to the content of the mixed powder, the theoretical loading volume is converted, and the aseptic packaging is carried out. Press C 21 h 25 N 5 o 8 S 2 Calculate repackable specifications such as:

[0039] 0.1g,...

Embodiment 3

[0042] The antibacterial agent and β-lactamase inhibitor composition comprises the following components in mass percentage: 83% of mezlocillin sodium; 17% of avibactam sodium.

[0043] Preparation:

[0044] (1) Weighing ingredients

[0045] Take avibactam sodium and mezlocillin sodium respectively by prescription quantity;

[0046] (2) mixed

[0047] Add all the avibactam sodium into the mixer, and then add part of the mezlocillin sodium in an equal amount, the addition amount is 30.12% of the total mass of the mezlocillin sodium, set the mixer speed to 10rpm, mix for 10min, and then add the remaining Measure mezlocillin sodium, keep the rotating speed and continue mixing for 15 minutes to obtain mixed powder;

[0048] (3) Aseptic packaging

[0049] According to the content of the mixed powder, the theoretical loading volume is converted, and the aseptic packaging is carried out. Press C 21 h 25 N 5 o 8 S 2 Calculate repackable specifications such as:

[0050] 0.1g,...

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Abstract

The invention belongs to the field of anti-infective medicines, and particularly relates to an antibacterial agent and beta-lactam enzyme inhibitor composition and an application thereof. The composition comprises A: mezlocillin or pharmaceutically-acceptable salt thereof, and preferably mezlocillin sodium; and B, avabatan or pharmaceutically-acceptable salt thereof, and preferably avabatan, wherein the mass ratio of the A to the B is (10-1) to (1-10). According to the composition disclosed by the invention, the mezlocillin is protected by the avabatan from being hydrolyzed by beta-lactamase,so that sterilizing effects can be reinforced, the problem that bacteria are drug resistant to the mezlocillin can be solved, and the composition can be used for preparing medicines for the respiratory system, the urinary system, the digestive system, department of gynecology and reproduction organ infection, caused by mezlocillin sensitive bacteria and beta-lactamase producing drug-resistance bacteria.

Description

technical field [0001] The invention belongs to the field of anti-infection drugs, and in particular relates to a composition of an antibacterial agent and a β-lactamase inhibitor and application thereof. Background technique [0002] Semi-synthetic penicillin antibiotics have been widely used clinically, and have achieved therapeutic effects that are difficult to achieve with traditional antibiotics. However, due to the long-term and extensive clinical use of antibiotics, and even the abuse of antibiotics, bacteria have become increasingly resistant to antibiotics. Mezlocillin is a semi-synthetic broad-spectrum benzamidocillin antibiotic, which is effective against Pseudomonas aeruginosa, Escherichia coli, Klebsiella pneumoniae, Proteus, Enterobacter, Citrobacter, Serratia, and Acinetobacter And Gram-positive cocci sensitive to penicillin all have antibacterial effect, and large doses have bactericidal effect. The antibacterial activity against Escherichia coli, Enterobac...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/431A61K31/551A61K9/19A61P31/04A61P11/00A61P13/00A61P1/00A61P15/00
CPCA61K9/0019A61K9/19A61K31/431A61K31/551A61P1/00A61P11/00A61P13/00A61P15/00A61P31/04A61K2300/00
Inventor 苗得足胡清文李雪改曾丽丽
Owner REYOUNG PHARMA
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