Antioxidant Solution for Oxidative Stress Reduction

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Solution Overview

Problem

Oxidative stress and cell activation lead to severe tissue destruction in various diseases, including renal and liver failure, and current treatments are inadequate in effectively managing these conditions, particularly in extracorporeal settings and cell culture systems.

Innovation Solution

A solution comprising N-acetyl-cysteine, gluconic acid, vitamin C, and optionally glutathione, with or without human serum albumin, is administered to reduce oxidative stress and cell activation by scavenging reactive oxygen species, either through infusion into the blood circuit or addition to dialysis fluid, optimizing concentrations to achieve significant inhibition of free radical formation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If single antioxidants (e.g., N-acetyl-cysteine) are administered to scavenge reactive oxygen species, then oxidative stress is reduced, but the effectiveness is insufficient due to lack of synergistic interaction

Engineering Contradiction:
Improveeffectiveness of oxidative stress reductionVSAvoidinsufficient scavenging effect
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The patent combines multiple antioxidants (N-acetyl-cysteine, gluconic acid, and optionally glutathione and vitamin C) into a single formulation to achieve synergistic effects. The combination of these compounds with different mechanisms of action enhances the overall scavenging of reactive oxygen species compared to using any single antioxidant alone, directly addressing the insufficiency of single-agent treatments.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The invention creates a composite antioxidant system comprising multiple substances with complementary properties. N-acetyl-cysteine provides direct scavenging, gluconic acid enhances glutathione synthesis, and optional additions like glutathione and vitamin C provide additional scavenging pathways. This composite approach creates a more robust and reliable antioxidant effect than individual components alone.

Inventive Principle:
Principle #40Composite materials

2Reliability

If multiple antioxidants are combined to achieve synergistic effect, then oxidative stress reduction is enhanced, but the formulation complexity increases

Engineering Contradiction:
Improvesynergistic oxidative stress reductionVSAvoidformulation complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent develops a multi-functional formulation where each component serves multiple purposes: N-acetyl-cysteine directly scavenges radicals and serves as a precursor for glutathione synthesis, gluconic acid enhances glutathione production and has mild scavenging properties, and optional glutathione and vitamin C provide additional scavenging capacity. This multi-functionality justifies the combination while maximizing therapeutic benefit.

Inventive Principle:
Principle #6Universality (Multi-functionality)

Solution Approach 2:

The invention optimizes the concentration parameters of each antioxidant component to achieve synergistic effects while maintaining formulation simplicity. By carefully selecting concentrations within specific ranges, the patent ensures that the combination produces enhanced effects without requiring overly complex formulation procedures or additional excipients.

Inventive Principle:
Principle #35Parameter changes

3Adaptability or versatility

If antioxidants are administered systemically, then oxidative stress is reduced throughout the body, but the specificity to target tissues is reduced

Engineering Contradiction:
Improvesystemic coverageVSAvoidtarget tissue specificity
Core Design Contradiction:
Adaptability or versatilityVSMeasurement precision

Solution Approach 1:

The patent utilizes glutathione as an intermediary substance that is enhanced by gluconic acid and N-acetyl-cysteine. Glutathione serves as a key mediator that operates both systemically and at the cellular level, allowing the formulation to achieve broad coverage while maintaining the ability to target specific tissues through its role in cellular antioxidant defense systems.

Inventive Principle:
Principle #24Intermediary (Mediator)

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The solution effectively inhibits free radical formation and reduces cell activation signals, demonstrating a synergistic effect when combined with human serum albumin, and shows applicability in both static and dynamic systems, including extracorporeal treatments, thereby mitigating tissue destruction and organ malfunction.

Implementation Method 1

N-acetyl-cysteine and gluconic acid, vitamin C and optionally glutathione... to reduce oxidative stress and cell activation by scavenging reactive oxygen species

Methodology Applied
Scientific EffectFree radical scavenging: Oxidation

Data Source

PatentEP2040689B1Solution comprising n-acetylcysteine and gluconic acid, and methods to reduce, treat and/or prevent oxidative stress and cell activation
Publication Date: 2010.12.01 GAMBRO LUNDIA AB
  • EP2040689B1 patent drawingFigure 1
  • EP2040689B1 patent drawingFigure 2
  • EP2040689B1 patent drawingFigure 3

AI summary

The present invention concerns a solution and methods to reduce, treat and/or prevent oxidative stress and cell activation. According to the invention the solution gives rise to the following concentrations of constituents within a blood flow of 0.1-18 mM N-acetyl-cysteine, optionally of 0.01-0.21 mM vitamin C, optionally of 2-26 mM gluconic acid and optionally of 0.01-5 mM glutathione. According to the invention the methods comprises adding a solution according to the invention in an extracorporeal setting through the membrane by adding the solution to the dialysis fluid, or by infusion of a solution according to the invention, either by bolus injection, continuous injection or a combination thereof.