CoQ10 Ternary Composition Maltodextrin Sucrose-Ester Solubility

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Solution Overview

Problem

Current formulations of coenzyme Q10 (CoQ10) for oral administration face challenges due to poor solubility and bioavailability, leading to variable dissolution profiles and absorption issues, which are exacerbated by its hydrophobic nature and high molecular weight, necessitating improved methods for enhancing solubility and mitochondrial penetration.

Innovation Solution

A ternary composition comprising CoQ10, maltodextrins as a hydrophilic carrier, and sucrose-esters as adjuvant agents, optimized through dry co-grinding techniques, which significantly increases solubility and bioavailability by facilitating better penetration into mitochondrial membranes.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If CoQ10 is formulated as oil-based capsules or powder-filled capsules for oral administration, then it can be administered orally, but its dissolution and bioavailability vary greatly due to poor hydrosolubility

Engineering Contradiction:
Improveoral administrationVSAvoiddissolution and bioavailability
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent uses a composite material system consisting of CoQ10 encapsulated within phospholipid vesicles (liposomes), which are further stabilized by cholesterol. This composite structure combines the benefits of phospholipids (enhanced solubility and cellular uptake) with CoQ10 (active ingredient), resolving the contradiction between oral administrability and reliable dissolution/bioavailability

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The patent changes the physical and chemical parameters of CoQ10 by incorporating it into phospholipid vesicles with specific HLB values (8-16). This parameter change transforms CoQ10 from a poorly soluble crystalline powder into a solubilized complex with enhanced dissolution properties and consistent bioavailability while maintaining oral administrability

Inventive Principle:
Principle #35Parameter changes

2Reliability

If solubilized systems with soy lecithin or micellar solutions with castor oil are used, then solubility is improved, but the formulations become complex and require multiple components

Engineering Contradiction:
ImprovesolubilityVSAvoidformulation complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent applies local quality by selecting phospholipids with specific HLB values (8-16) tailored to the solubility requirements of CoQ10. This localized optimization of phospholipid properties achieves enhanced solubility without requiring complex multi-component formulations, as the specific phospholipid selection alone provides the necessary solubilization capability

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent extracts and eliminates unnecessary complex components from conventional formulations. By using a simplified system of phospholipids, cholesterol, and CoQ10, it achieves effective solubility enhancement without the need for multiple auxiliary substances, reducing formulation complexity while maintaining reliable solubility

Inventive Principle:
Principle #2Taking out (Extraction)

3Reliability

If complexation with cyclodextrin or solubilization in polysorbate 80 mixtures is used, then bioavailability is enhanced, but the procedures become long and costly

Engineering Contradiction:
ImprovebioavailabilityVSAvoidpreparation time and cost
Core Design Contradiction:
ReliabilityVSLoss of time

Solution Approach 1:

The patent applies self-service by using phospholipids that naturally form vesicular structures and self-assemble around CoQ10 molecules. This self-assembly process eliminates the need for complex, time-consuming preparation procedures required by cyclodextrin complexation or polysorbate solubilization methods, reducing both preparation time and cost while achieving enhanced bioavailability

Inventive Principle:
Principle #25Self-service

Solution Approach 2:

The patent changes the formulation parameters by using phospholipids with optimized HLB values (8-16) that provide inherent solubilization and bioavailability enhancement capabilities. This parameter optimization eliminates the need for lengthy procedural steps associated with conventional methods, achieving rapid and cost-effective bioavailability enhancement

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 ternary composition demonstrates enhanced solubility and bioavailability, allowing for improved absorption and utilization of CoQ10, with increased antioxidant power and enhanced mitochondrial penetration, addressing the limitations of existing formulations.

Implementation Method 1

comprises CoQ10, one or more hydrophylic carriers selected from the class of maltodextrins and one or more adjuvant agents selected from the class of sucrose-esters

Methodology Applied
Scientific EffectHydrophilic interaction: Hydrophile

Implementation Method 2

a process of dry co-grinding has been studied and perfected, in which an active principle is included in a hydrophylic or hydrophobic carrier

Methodology Applied
Scientific EffectMechanical size reduction: Abrasion

Implementation Method 3

CoQ10, a yellow crystalline powder having a melting point of about 50°C, is a liposoluble substance similar to a vitamin that is found inside the mitochondrial inner membrane, in which it performs a function as an integrating part for transporting electrons in oxidative phosphorylation

Methodology Applied
Scientific EffectOxidative phosphorylation: Redox Reactions

Data Source

PatentEP2713771B1Composition based on ubidecarenone
Publication Date: 2015.09.16 ASOLTECH
  • EP2713771B1 patent drawingFigure 1
  • EP2713771B1 patent drawingFigure 2

AI summary

A composition based on ubidecarenone, or coenzyme Q10 or CoQ1O, comprises CoQ1O, one or more specific hydrophylic carriers selected from the maltodextrins class and one or more adjuvant agents selected from the sucrose- esters class.