Myramistin Composition Reducing Toxicity While Maintaining Antimicrobial Activity

Resolve Bottlenecks,
Find Innovative SolutionsGenerate Solutions

Solution Overview

Problem

Current pharmaceutical compositions using quaternary ammonium salts and tertiary amine derivatives have limitations such as high toxicity, limited range of action, and inefficiency in treating bacterial infections, especially when used internally or as spermicidal preparations, and they cannot be effectively combined with other medications due to complex compound formation.

Innovation Solution

A composition comprising Benzyldimethyl(3-[myristoylamino]-propyl) ammonium chloride in combination with dimethyl(3-[myristoylamino]-propyl) amine oxide or amine, using suitable pharmaceutical solvents like water or alcohol, with specific ratios to enhance efficacy and reduce toxicity and irritant effects, allowing for broader application including internal use and combination with other medications.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If quaternary ammonium salts are used as pharmaceutical compositions, then antimicrobial activity is achieved, but toxicity increases

Engineering Contradiction:

Improveantimicrobial activityVSAvoidtoxicity

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent combines quaternary ammonium salt (myramistin) with tertiary amine derivative (amine oxide or amine) to create a multi-component composition. This merging of substances with different properties achieves synergistic antimicrobial effect while the tertiary amine component helps reduce the toxicity and irritant effects of the quaternary ammonium salt.

Inventive Principle:

Principle #5Merging (Combining)

Solution Approach 2:

The invention creates a composite pharmaceutical composition containing multiple active ingredients (quaternary ammonium salt plus tertiary amine derivative) in specific ratios. This composite approach allows the composition to exhibit enhanced antimicrobial activity while reducing harmful side effects compared to using single substances alone.

Inventive Principle:

Principle #40Composite materials

2Reliability

If amidoamines are used in compositions for treating fungal infections, then antifungal effectiveness is achieved, but efficiency against bacterial infections decreases

Engineering Contradiction:

Improveantifungal effectivenessVSAvoidefficiency against bacterial infections

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent creates a composition that performs multiple functions: the quaternary ammonium salt provides broad-spectrum antimicrobial activity including antibacterial and antifungal effects, while the tertiary amine derivative enhances antifungal effectiveness. Together, they create a universal composition effective against both fungal and bacterial infections, as well as exhibiting immunomodulatory, anesthetic, and anti-inflammatory properties.

Inventive Principle:

Principle #6Universality (Multi-functionality)

3Reliability

If quaternary ammonium salts are used at higher concentrations to increase effectiveness, then antimicrobial activity improves, but irritant effects increase

Engineering Contradiction:

Improveantimicrobial activityVSAvoidirritant effects

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent optimizes the concentration parameters of both active ingredients, using quaternary ammonium salt at 0.008-5.0% and tertiary amine derivative at 0.00005-1.0%. This parameter optimization achieves effective antimicrobial activity while minimizing irritant effects. The synergistic interaction allows lower effective concentrations compared to using quaternary ammonium salt alone at high doses.

Inventive Principle:

Principle #35Parameter changes

4Device complexity

If single-component preparations are used, then simplicity is maintained, but range of action is limited

Engineering Contradiction:

Improvepreparation simplicityVSAvoidrange of action

Core Design Contradiction:

Device complexityVSAdaptability or versatility

Solution Approach 1:

The multi-component composition achieves universality by combining substances with complementary properties. The quaternary ammonium salt provides broad-spectrum antimicrobial activity, while the tertiary amine derivative adds enhanced antifungal effects and immunomodulatory properties. This creates a single preparation that can treat various infectious and inflammatory conditions including urogenital, intestinal, and nasopharyngeal diseases, as well as providing protection against sexually transmitted diseases.

Inventive Principle:

Principle #6Universality (Multi-functionality)

Data Source

PatentEP2536400B1Medicament comprising myramistin

Publication Date: 2014.09.24 MEGAINPHARM

AI summary

The invention relates to a pharmaceutical including benzyldimethyl(3-[myristoylamino]propyl)ammonium chloride in the monohydrate form or in unhydrated form. The pharmaceutical further comprises dimethyl(3-[myristoylamino]propyl)ammonium oxide and/or dimethyl(3-[myristoylamino]propyl)amine in the appropriate pharmaceutical solvent.