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Drug composition used for treating MRSA and applications thereof

A composition and drug technology, applied in the field of medicine, can solve problems such as difficulty in treating infection, reducing membrane permeability, and changing the target of antibiotics

Active Publication Date: 2020-02-18
THE SECOND HOSPITAL OF HEBEI MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

What's more, MRSA can also use a variety of different mechanisms of action, such as producing modified enzymes, changing the target of antibiotics, reducing membrane permeability, etc., thereby inhibiting other commonly used clinical antibiotics that belong to different structural categories from methicillin. Drugs such as fluoroquinolones, aminoglycosides, macrolides, tetracyclines, etc. have different degrees of drug resistance, which makes it difficult to treat the infection caused by this strain and has a high mortality rate.

Method used

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  • Drug composition used for treating MRSA and applications thereof
  • Drug composition used for treating MRSA and applications thereof
  • Drug composition used for treating MRSA and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0025] tablet

[0026] Compound A 20g talcum powder 10g

[0027] Compound B 12g micronized silica gel 1g

[0028] Microcrystalline Cellulose 25g Magnesium Stearate 1g

[0029] Starch 23g

[0030] A total of 1000 tablets were prepared

[0031] Weigh the prescribed amount of compound A and compound B, fully mix them in a mortar, pass through an 80-mesh sieve, then mix with other excipients in the prescription, pass through a 40-mesh sieve, and directly compress the obtained powder into tablets.

experiment example 1

[0032] In vitro evaluation of the bacteriostatic effect of experimental example 1 pharmaceutical composition of the present invention on MRSA

[0033] The purpose of this experiment is to investigate the in vitro inhibitory effect of the pharmaceutical composition of the present invention on MRSA using the minimum inhibitory concentration (MIC) as an index.

[0034] 1. Experimental materials

[0035] Resazurin was purchased from Shanghai Hualan Chemical Technology Co., Ltd.; Compound A and Compound B were synthesized according to the methods disclosed in patent documents WO2015 / 038661A1 and WO 2011 / 120133A1 respectively; MRSA clinical isolates were obtained from Clinical Pharmacology Research of Peking University Institute; Corning359996-well cell culture plate, purchased from Corning (Corning) Company.

[0036] 2. Experimental method

[0037] In this experiment, the resazurin chromogenic method was used to determine the minimum inhibitory concentration (MIC) of samples agai...

experiment example 2

[0048] Experimental Example 2 Effect of the pharmaceutical composition of the present invention on the death protection rate of mice infected with MRSA

[0049] The purpose of this experiment is to investigate the in vivo therapeutic effect of the pharmaceutical composition of the present invention on MRSA-infected mice.

[0050] 1. Experimental materials

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Abstract

The invention discloses a drug composition used for treating MRSA. The drug composition consists of a component a), a component b) and a component c), wherein the a) is (6-fluoro-4-(6-hydroxy-3-azabicyclo[3.2.0]hept-3-yl)-2-((2-methylpyrimidine-5-yl)oxy)-9H-pyrimido[4,5-b]indole-8-yl)(methyl)carbamic acid((phosphono)oxy)methyl ester, the b) is 3-chloro-5-({1-[(4-methyl-5-oxo-4,5-dihydro-1H-1,2,4-triazole-3-yl)methyl]-2-oxo-4-(trifluoromethyl)-1,2-dihydropyridine-3-yl}oxy)benzonitrile, and the c) is a pharmaceutically acceptable excipient; and the mass ratio of the component a) to the componentb) is 3-7 : 1-5. The drug composition is extremely effective on treating diseases caused by MRSA.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a pharmaceutical composition for treating MRSA and its application. Background technique [0002] MRSA (the English acronym for Methicillin-Resistant Staphylococcus aureus) is called methicillin-resistant Staphylococcus aureus in Chinese, also known as methicillin-resistant Staphylococcus aureus, penicillin-resistant Staphylococcus aureus, anti- Methicillin Staphylococcus aureus, among others, is a major and common pathogen of community and hospital infections, first clinically isolated in 1961 and causing MRSA strains in hospitals around the world in the 1960s Infect. [0003] MRSA is capable of producing a variety of toxins and is highly pathogenic, known as "super bacteria". MRSA can cause infection of blood, skin, soft tissue and various organs of the body. MRSA is characterized by its broad spectrum of drug resistance. As the name implies, in addition to resistance to m...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/675A61K31/4439A61P31/04
CPCA61K31/4439A61K31/675A61P31/04A61K2300/00
Inventor 刘燕谷雨马晓松马薇张翠英
Owner THE SECOND HOSPITAL OF HEBEI MEDICAL UNIV
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