Lactoferrin–NAC Composition for COPD Mucolysis and Oxidative Damage

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Solution Overview

Problem

Current treatments for Chronic Obstructive Pulmonary Disease (COPD) using N-Acetyl-L-Cysteine alone do not effectively address long-term mucolysis issues and often have side effects, necessitating the development of a formulation with better mucolytic effects and a safer profile.

Innovation Solution

A synergistic combination of Lactoferrin and N-Acetyl-L-Cysteine in a specific ratio, ranging from 11:1 to 14:1, is administered to provide enhanced mucolytic effects and reduce oxidative damage in COPD, optionally combined with additional active ingredients like Carotenoids.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If N-Acetyl-L-Cysteine is used alone for COPD treatment, then mucolytic effect is provided, but side effects occur and long-term mucolysis issues are not effectively addressed

Engineering Contradiction:
Improvemucolytic effectivenessVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent combines Lactoferrin and N-Acetyl-L-Cysteine into a single pharmaceutical composition. Lactoferrin (10-50 mg) and NAC (100-500 mg) are formulated together to achieve synergistic effects, where Lactoferrin enhances the mucolytic activity while NAC provides antioxidant protection, thereby improving reliability while reducing side effects compared to NAC alone

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The invention creates a composite pharmaceutical formulation containing both Lactoferrin and NAC in specific proportions. This composite approach allows the two active ingredients to work synergistically, with Lactoferrin's iron-binding properties and NAC's thiol groups complementing each other to enhance mucolytic effectiveness while mitigating individual side effects

Inventive Principle:
Principle #40Composite materials

2Productivity

If higher doses of N-Acetyl-L-Cysteine are administered to improve mucolytic effect, then efficacy increases, but side effects and oxidative damage worsen

Engineering Contradiction:
Improvemucolytic efficacyVSAvoidoxidative damage
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent converts the potential harm of oxidative damage into a benefit by combining NAC with Lactoferrin. While high-dose NAC can cause oxidative stress, Lactoferrin's iron-chelating properties prevent free iron-catalyzed oxidation, and its own antioxidant capacity transforms the oxidative challenge into a therapeutic opportunity where both agents protect against each other's potential harms while enhancing mucolytic efficacy

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

Solution Approach 2:

The invention optimizes the dosage parameters of both Lactoferrin (10-50 mg) and NAC (100-500 mg) to achieve a therapeutic window where mucolytic efficacy is maximized while oxidative damage is minimized. This parameter optimization allows effective treatment without the harmful effects associated with higher single-ingredient doses

Inventive Principle:
Principle #35Parameter changes

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 combination of Lactoferrin and N-Acetyl-L-Cysteine offers a safe and effective mucolytic treatment for COPD, reducing mucus hypersecretion and oxidative damage without significant side effects, with enhanced efficacy compared to either component alone.

Implementation Method 1

The present invention relates to pharmaceutical compositions/formulations comprising a synergistic combination of Lactoferrin and N-Acetyl-L-Cysteine

Methodology Applied
Scientific EffectSynergistic interaction:

Implementation Method 2

NAC can act as a precursor of reduced glutathione and as a direct reactive oxygen species scavenger, hence regulating the redox status in the cells

Methodology Applied
Scientific EffectReactive oxygen species scavenging: Oxidation

Implementation Method 3

LF belongs to the innate immune system and apart from its main biological function, namely binding and transport of iron ions

Methodology Applied
Scientific EffectIon binding: Absorption (physical)

Implementation Method 4

The pharmaceutical compositions/formulations of the present application also help to reduce the oxidative damage in COPD

Methodology Applied
Scientific EffectOxidative damage reduction: Oxidation

Data Source

PatentEP4536273B1A pharmaceutical composition providing mucolytic effect
Publication Date: 2025.10.01 FRIMLINE PTE LTD
  • EP4536273B1 patent drawingFigure 1~2

AI summary

The present invention relates to pharmaceutical compositions/formulations providing mucolytic effect. More particularly, the present invention relates to pharmaceutical compositions/formulations comprising synergistic combination of Lactoferrin and N-Acetyl-L-Cysteine. The present application also provides various compositions/formulations and process of preparing the same. The pharmaceutical compositions/formulations of the present application also help to reduce the oxidative damage in COPD.