Orobuccal D-galactose Composition Bypassing Hepatic Metabolism

Solution Overview

Problem

Current treatments for neurodegenerative diseases associated with altered mitochondrial function, such as multiple sclerosis and Alzheimer's, face challenges in effectively delivering D-galactose across the blood-brain barrier and maintaining its efficacy due to enzymatic conversion to glucose in the liver, leading to inadequate myelin metabolism support.

Innovation Solution

A buccal or sublingual composition combining D-galactose with coenzyme Q10 and optional reduced glutathione, designed for rapid absorption through the oral mucosa, bypassing the hepatic first-pass effect, to enhance neuroprotection and metabolic support for myelin, potentially improving symptoms of chronic-degenerative diseases.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If D-galactose is administered orally, then it can be delivered to the body, but it is converted to glucose by the liver through enzymatic action, reducing its efficacy for myelin metabolism

Engineering Contradiction:
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent uses the oral mucosa as an intermediary absorption route. Instead of direct oral administration where the substance passes through the liver, the composition is applied to the oral mucosa which absorbs D-galactose directly into the bloodstream, bypassing hepatic first-pass metabolism and maintaining its efficacy for myelin metabolism.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent extracts D-galactose from the digestive system pathway and delivers it directly to the systemic circulation through oral mucosal absorption. This removes the harmful intermediate step of hepatic conversion to glucose, allowing D-galactose to reach the brain and myelin directly.

Inventive Principle:
Principle #2Taking out (Extraction)

2Reliability

If D-galactose is administered to support myelin metabolism in neurodegenerative diseases, then neuroprotection can be achieved, but the blood-brain barrier prevents effective delivery

Engineering Contradiction:
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The oral mucosa serves as an intermediary absorption site that bypasses the blood-brain barrier obstacle. By absorbing D-galactose into the systemic circulation through the highly vascularized oral mucosa, the substance can reach the brain through normal physiological processes without being blocked by the blood-brain barrier.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Quantity of substance

If lactose is hydrolyzed by lactase to release D-galactose, then D-galactose becomes available, but many adults have lost lactase functionality

Engineering Contradiction:
Core Design Contradiction:
Quantity of substanceVSAdaptability or versatility

Solution Approach 1:

The patent extracts D-galactose from the lactose-hydrolysis pathway that requires functional lactase. By providing D-galactose directly in a form that can be absorbed through the oral mucosa, it bypasses the need for lactase enzyme functionality, making it accessible to adults who have lost this enzymatic capability.

Inventive Principle:
Principle #2Taking out (Extraction)

4Quantity of substance

If D-galactose is administered in high doses to overcome metabolic conversion, then more substrate is available, but side effects may increase

Engineering Contradiction:
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The oral mucosa acts as an efficient intermediary absorption route with high bioavailability. This allows lower doses of D-galactose to achieve therapeutic levels in the blood and brain, avoiding the need for high doses that would be required if administered orally and subject to hepatic first-pass metabolism, thereby reducing potential side effects.

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 composition demonstrates increased efficacy in clinical settings for chronic-degenerative diseases by direct absorption into the bloodstream, providing enhanced bioavailability and neuroprotection, with no reported side effects, and can be used as a complementary therapy to standard treatments.

Implementation Method 1

A buccal or sublingual composition combining D-galactose with coenzyme Q10 and optional reduced glutathione, designed for rapid absorption through the oral mucosa, bypassing the hepatic first-pass effect

Methodology Applied
Scientific EffectAbsorption: Absorption (physical)

Implementation Method 2

D-gal can also exert a metabolic role, as a substrate for ectopic oxidative phosphorylation described for myelin

Methodology Applied
Scientific EffectOxidative phosphorylation:

Data Source

PatentEP3243509B1Orobuccal absorption composition for neuro-protection
Publication Date: 2019.04.17
  • EP3243509B1 patent drawingFigure 1

AI summary

It is hereby described an orobuccal absorption composition for the neuro-protection containing D-galactose in association with coenzyme Q10 and, optionally, reduced glutathione. In particular said composition is used as a food supplement or functional food or food for special medical purposes or medicament, for example in an orosoluble and/or slightly effervescent formulation for sublingual or orobuccal administration.