Pharmaceutical Composition for Resistant Bacterial Infections

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Solution Overview

Problem

The increasing problem of partial and total resistance to therapeutic agents leads to the need for higher doses, resulting in undesirable side effects and toxicity, especially in immunocompromised patients, and can lead to multi-drug resistance, making treatment of infections caused by resistant germs challenging.

Innovation Solution

A pharmaceutical composition combining a first therapeutically active substance, such as carvacrol or alpha-ionone, with a second antibiotic substance, like amoxicillin, to potentiate the antibiotic's activity, allowing for lower doses and effective treatment of resistant bacterial infections.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If the dose of therapeutic agent is increased to overcome partial resistance, then the therapeutic effectiveness is improved, but the toxicity and side effects increase

Engineering Contradiction:
Improvetherapeutic effectivenessVSAvoidtoxicity and side effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent combines a known antibiotic with a naturally occurring compound (carvacrol, carvacrol, thymol, or eugenol) to create a synergistic effect. This combination allows the antibiotic to work more effectively at lower doses, thereby maintaining therapeutic effectiveness while reducing toxicity and side effects associated with high-dose monotherapy.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The invention changes the dosing parameters by using sub-inhibitory concentrations of the natural compound in combination with reduced doses of the antibiotic. This parameter change achieves the desired therapeutic effect while staying below the toxic threshold, effectively resolving the contradiction between effectiveness and safety.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If the dose of therapeutic agent is continuously increased to overcome resistance, then the therapeutic effectiveness is maintained, but the development of total and multi-drug resistance accelerates

Engineering Contradiction:
Improvetherapeutic effectivenessVSAvoidbacterial resistance development
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent converts the potentially harmful effect of resistance development into a benefit by using a multi-component approach. The natural compound (carvacrol, carvacrol, thymol, or eugenol) works through a different mechanism than traditional antibiotics, thereby bypassing existing resistance mechanisms and preventing the selection of resistant mutants while maintaining therapeutic effectiveness.

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

Solution Approach 2:

The invention creates a composite therapeutic agent combining a conventional antibiotic with a natural compound. This composite approach addresses resistance by utilizing multiple mechanisms of action, where the natural compound enhances the antibiotic's effectiveness and prevents resistance development, thereby maintaining long-term therapeutic reliability without accelerating resistance.

Inventive Principle:
Principle #40Composite materials

3Reliability

If high doses of therapeutic agents are administered to treat resistant infections, then the immediate therapeutic effect is improved, but the long-term prognosis and life expectancy of immunocompromised patients deteriorate

Engineering Contradiction:
Improveimmediate therapeutic effectVSAvoidlong-term prognosis and life expectancy
Core Design Contradiction:
ReliabilityVSDuration of action of moving object

Solution Approach 1:

The patent merges a conventional antibiotic with a natural compound (carvacrol, carvacrol, thymol, or eugenol) to achieve both immediate and long-term therapeutic benefits. The combination provides rapid effectiveness at low doses while minimizing toxicity, thereby improving both short-term outcomes and long-term prognosis for immunocompromised patients.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The invention optimizes dosing parameters by using low doses of the antibiotic in combination with sub-inhibitory concentrations of the natural compound. This parameter optimization achieves immediate therapeutic effects while reducing cumulative toxicity, thereby extending the treatment duration and improving long-term life expectancy without compromising immediate effectiveness.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentEP1879655B1Pharmaceutical composition comprising an anti-bacterial agent and an active ingredient selected from carveol, carvacrol, alpha-ionone, beta-ionone, and thymol
Publication Date: 2014.11.26 ADVANCED SCIENTIFIC DEVELOPMENTS
  • EP1879655B1 patent drawing

AI summary

The invention relates to a pharmaceutical composition comprising at least one first active therapeutic substance selected among carveol, thymol, eugenol, borneol, carvacrol, alpha-ionone, beta-ionone, as well as isomers, derivatives and mixtures thereof, and comprising at least one second active therapeutic substance that is an antibiotic.