CoQ10 and Vitamin A Formulation Using Vitamin E Antioxidants

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Solution Overview

Problem

The body's ability to convert the oxidized form of CoQ10 (ubiquinone) to its active reduced form (ubiquinol) declines with age, and existing supplements primarily provide ubiquinone, which is inefficient for individuals with compromised conversion capabilities, and there is a need to protect vitamin A from oxidation to its toxic form (retinoic acid).

Innovation Solution

Vitamin E (tocotrienol and tocopherol) is used to reduce ubiquinone to ubiquinol in situ and protect retinol from oxidation to retinoic acid, either in combination with ubiquinol or ubiquinone in formulations like softgels, ensuring the active forms of CoQ10 and vitamin A are maintained.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Stability of the object's composition

If ubiquinone is provided in supplements, then storage stability is improved, but conversion efficiency to active ubiquinol decreases with age

Engineering Contradiction:
Improvestorage stability of CoQ10VSAvoidconversion efficiency to ubiquinol
Core Design Contradiction:
Stability of the object's compositionVSProductivity

Solution Approach 1:

The patent applies preliminary action by pre-converting ubiquinone to ubiquinol in the formulation before administration. The softgel contains ubiquinol that has been reduced from ubiquinone in advance, eliminating the need for in-body conversion. This is achieved through controlled reduction processes during manufacturing, ensuring the active form is already present when the supplement is taken.

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The patent applies parameter changes by altering the oxidation state of CoQ10 from ubiquinone (oxidized) to ubiquinol (reduced form). This chemical parameter change ensures the supplement delivers the active form directly. The formulation utilizes different oxidation states to optimize both stability during storage and bioactivity in the body.

Inventive Principle:
Principle #35Parameter changes

2Quantity of substance

If vitamin A is provided in formulations, then nutritional value is improved, but oxidation to toxic retinoic acid increases

Engineering Contradiction:
Improvevitamin A contentVSAvoidoxidation to retinoic acid
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent applies the intermediary principle by using vitamin E (tocopherol and/or tocotrienol) as an antioxidant mediator that protects vitamin A from oxidation. Vitamin E acts as a sacrificial antioxidant that donates electrons to prevent vitamin A from oxidizing to toxic retinoic acid, thereby preserving the nutritional value while eliminating the harmful effect.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent applies preliminary anti-action by incorporating antioxidants (vitamin E, tocopherol, tocotrienol) into the formulation in advance to prevent oxidation of vitamin A before it can occur. This preventive measure is built into the softgel formulation, where antioxidants are positioned to protect vitamin A from oxidative damage during storage and after administration.

Inventive Principle:
Principle #9Preliminary anti-action

3Productivity

If ubiquinol is provided directly, then conversion capability is improved, but oxidation stability deteriorates

Engineering Contradiction:
Improveconversion capability to active formVSAvoidoxidation stability
Core Design Contradiction:
ProductivityVSStability of the object's composition

Solution Approach 1:

The patent applies the intermediary principle by using antioxidants (vitamin E, tocopherol, tocotrienol) as mediators that protect ubiquinol from oxidation. These antioxidants act as protective intermediaries between ubiquinol and oxygen, preventing the conversion back to ubiquinone and maintaining the active reduced form throughout storage and digestion.

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

This approach effectively converts a significant percentage of ubiquinone to ubiquinol and prevents the formation of toxic retinoic acid, ensuring the body receives the active forms of CoQ10 and vitamin A, enhancing energy transduction and reducing oxidative stress.

Implementation Method 1

Vitamin E (tocotrienol and tocopherol) is used to reduce ubiquinone to ubiquinol in situ

Methodology Applied
Scientific EffectRedox reaction: Redox Reactions

Implementation Method 2

protect retinol from oxidation to retinoic acid

Methodology Applied
Scientific EffectOxidation protection: Oxidation

Data Source

PatentUS9949938B2CoQ10 (ubiquinone, ubiquinol), vitamin A (retinoid acid, retinol), vitamin E (tocotrienol, tocopherol) and methods of use
Publication Date: 2018.04.24 AMERICAN RIVER NUTRITION LLC
  • US9949938B2 patent drawing
  • US9949938B2 patent drawing
  • US9949938B2 patent drawing

AI summary

CoQ10 and vitamin E are both lipid-soluble nutrients with redox potential. Tocopherol and/or tocotrienol protect CoQ10 from oxidative damage and reduce ubiquinone in situ. Specifically, vitamin E protects the oxidation of ubiquinol to ubiquinone ex vivo and reduces ubiquinone to ubiquinol in situ. Vitamin Es with higher ratio of tocotrienol-to-tocopherol cause a higher ratio of ubiquinol-to-ubiquinone. Additionally tocopherol and/or tocotrienol protect vitamin A oxidation from retinol to retinoic acid.