Nu-8 Antimicrobial Compound Topical Formulation for Wound Care

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Solution Overview

Problem

Current antimicrobial compounds face challenges in effectively treating wounds and ulcers, particularly diabetic foot ulcers, due to limitations in antimicrobial activity and compatibility with topical administration routes, especially at lower pH levels, leading to contact irritation and reduced efficacy.

Innovation Solution

The use of sodium ((2R,3S,5R)-5-(4-amino-2-oxopyrimidin-1(2H)-yl)-3-((butoxyoxidophosphor-yl)oxy)tetrahydrofuran-2-yl)methyl butyl phosphate, referred to as Nu-8, which exhibits high biological activity at higher pH levels, is administered topically in various formulations such as lotions, gels, or creams, providing effective antimicrobial action against a broad spectrum of microbes, including slow-growing bacteria and fungi.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current antimicrobial compounds are administered topically at lower pH levels, then antimicrobial activity is improved, but contact irritation increases and efficacy is reduced

Engineering Contradiction:
Improveantimicrobial activityVSAvoidcontact irritation
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent modifies the chemical structure of antimicrobial compounds by introducing specific substituents (e.g., fluorine atoms at positions 2 and 4, chlorine at position 3) to alter their pH-dependent behavior. This structural modification enables the compounds to maintain effective antimicrobial activity at lower pH levels while reducing contact irritation, thus resolving the contradiction between reliability and harmful factors.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention creates composite antimicrobial compounds that combine multiple functional groups and substituents within a single molecular structure. These composite structures integrate the pH-sensitive antimicrobial functionality with irritation-reducing characteristics, allowing simultaneous achievement of high reliability and low harmful effects when administered topically.

Inventive Principle:
Principle #40Composite materials

2Reliability

If current antimicrobial compounds are used for treating wounds and ulcers, then antimicrobial action is provided, but compatibility with topical administration is reduced

Engineering Contradiction:
Improveantimicrobial actionVSAvoidcompatibility with topical administration
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent systematically varies key parameters of the antimicrobial compound structure, including the introduction of fluorine atoms at positions 2 and 4 and chlorine at position 3, to optimize the balance between antimicrobial potency and topical compatibility. These parameter changes result in compounds that are both effective and suitable for topical administration in wound and ulcer treatments.

Inventive Principle:
Principle #35Parameter changes

3Productivity

If antimicrobial compounds with high activity are administered, then microbial burden is reduced, but irritation and reduced efficacy occur

Engineering Contradiction:
Improvemicrobial burden reductionVSAvoidtreatment efficacy
Core Design Contradiction:
ProductivityVSReliability

Solution Approach 1:

The invention fine-tunes the chemical parameters of antimicrobial compounds to achieve optimal performance. By introducing specific substituents (fluorine at positions 2 and 4, chlorine at position 3), the compounds attain high productivity in reducing microbial burden while maintaining reliability of treatment efficacy, eliminating the contradiction between these two factors.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS11377468B2Antimicrobial compounds, compositions, and uses thereof
Publication Date: 2022.07.05 LAKEWOOD AMEDEX INC
  • US11377468B2 patent drawing
  • US11377468B2 patent drawing
  • US11377468B2 patent drawing

AI summary

A method of treating an infection of at least one of a wound or a ulcer in a patient in need thereof according to an embodiment includes administering to the patient an effective amount of a compound having the formula:or a pharmaceutically acceptable salt thereof.