Choline Succinate Composition for Brain Energy Metabolism

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Solution Overview

Problem

Existing treatments for central nervous system disorders and cognitive impairment due to imbalanced or damaged brain energy metabolism are ineffective due to the lack of transport of succinic acid and its salts across the blood-brain barrier, and there is a need for safe and effective dietary supplements to enhance brain energy metabolism and cognitive function.

Innovation Solution

A composition comprising choline cation, succinate anion, and nicotinamide, or nicotinamide riboside, in a specific molar ratio, which can be administered orally to enhance brain energy metabolism by increasing NADH and ATP production, thereby improving cognitive function and mental endurance.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If succinic acid or its salts are administered orally to treat CNS disorders, then the treatment should improve brain energy metabolism, but the compounds cannot penetrate the blood-brain barrier due to lack of specific transporters

Engineering Contradiction:
Improveeffectiveness of succinate treatmentVSAvoidblood-brain barrier impermeability
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent uses choline as an intermediary carrier to deliver succinate across the blood-brain barrier. Choline succinate acts as a prodrug complex where choline facilitates transport through the BBB, and succinate is released inside the brain to improve energy metabolism. This intermediary approach resolves the contradiction by enabling succinate delivery despite the lack of direct transporters.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the chemical form of succinate from free acid or simple salts to a choline complex. This parameter change in molecular structure enables the compound to interact with choline transport mechanisms at the blood-brain barrier, transforming an impermeable substance into a deliverable therapeutic agent.

Inventive Principle:
Principle #35Parameter changes

2Productivity

If a combination of choline, succinate, and nicotinamide is used to enhance brain energy metabolism, then cognitive function and mental endurance improve, but the complexity of the composition increases

Engineering Contradiction:
Improvebrain energy metabolism efficiencyVSAvoidcomposition complexity
Core Design Contradiction:
ProductivityVSDevice complexity

Solution Approach 1:

The patent combines three complementary compounds (choline, succinate, and nicotinamide) into a single synergistic composition. Each component addresses a different aspect of brain energy metabolism: choline provides acetylcholine precursors, succinate feeds the TCA cycle, and nicotinamide replenishes NAD+ pools. Their merger creates a comprehensive metabolic support system that achieves superior productivity compared to individual components.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The composition is designed to perform multiple functions simultaneously: enhancing ATP production, supporting neurotransmitter synthesis, improving mitochondrial function, and protecting against metabolic stress. This multi-functionality allows a single composition to address various aspects of brain energy metabolism without requiring multiple separate treatments.

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

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 synergistically enhances brain energy metabolism, improving cognitive function, mental endurance, and reducing symptoms associated with imbalanced brain energy metabolism such as fatigue, mood swings, and depression, while being safe for daily use.

Implementation Method 1

Nicotinamide adenine dinucleotide (NAD+) is a coenzyme that serves as a hydrogen carrier NADH/NAD+ between substrates of tricarboxylic acid cycle and complex I mitochondria supporting thus ATP production during the oxidative phosphorylation

Methodology Applied
Scientific EffectNAD+/NADH hydrogen carrier function: Redox Reactions

Implementation Method 2

Succinic acid or salts thereof (succinates) are substrates of mitochondrial complex II. At hypoxia, a condition of a deficiency in oxygen supply of tissues of the body, succinate oxidation may contribute to 70-80% of total oxygen consumption

Methodology Applied
Scientific EffectSuccinate oxidation: Oxidation

Implementation Method 3

Succinate transport across the body is mediated by specific sodium-coupled dicarboxylate-anion transporters of SLC13 family

Methodology Applied
Scientific EffectSodium-coupled dicarboxylate-anion transport: Osmosis

Data Source

PatentEP3644959B1Composition comprising choline, succinate and nicotinamide and its use in brain energy metabolism
Publication Date: 2025.12.10 MITOCHONDRIAL SUBSTRATE INVENTION
  • EP3644959B1 patent drawing

AI summary

The present invention relates to compositions, in particular dietary compositions,that comprise a combination of choline cation and succinate anion (2-) and nicotinamide, and use of these compositions for maintaining and enhancing the brain energy metabolism in a human, and for preventing and treating symptoms and physiological conditions associated with an imbalanced, damaged or slowed brain energy metabolism in a human subject.