Coenzyme Q10 Solid Dispersion Amorphization
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Coenzyme Q10 supplementation is limited by its poor pharmacokinetic properties, particularly low oral bioavailability due to its crystalline form and high lipophilicity, which hinders absorption into systemic circulation.
Innovation Solution
A solid dispersion of Coenzyme Q10 with phospholipids and cellulosic or polymeric materials is prepared, enhancing amorphization and solubility, and facilitating gastrointestinal absorption and membrane crossing, thereby improving bioavailability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If Coenzyme Q10 is administered in crystalline form, then it maintains stability, but oral bioavailability is very low due to high lipophilicity and low solubility
Solution Approach 1:
The patent transforms Coenzyme Q10 from crystalline to amorphous form by incorporating it into solid dispersion matrices (hydrophilic polymers, lipids, or surfactants). This parameter change in physical state increases solubility and dissolution rate while maintaining stability through the stabilizing effect of the dispersion matrix, thereby improving oral bioavailability without sacrificing stability
Solution Approach 2:
The patent creates composite solid dispersion systems combining Coenzyme Q10 with hydrophilic polymers (e.g., HPMC, PVP), lipids (e.g., lecithin, triglycerides), or surfactants. These composite materials provide both stability from the matrix structure and improved solubility/bioavailability through the hydrophilic nature of the dispersing medium
2Quantity of substance
If Coenzyme Q10 is formulated to increase solubility, then oral bioavailability improves, but the crystalline structure is lost
Solution Approach 1:
The patent intentionally changes the physical state parameter from crystalline to amorphous by using solid dispersion technology. The amorphous form provides superior solubility and bioavailability, while the stability is maintained through incorporation into stabilizing matrices that prevent degradation and maintain the amorphous state
Solution Approach 2:
The patent introduces intermediary substances (hydrophilic polymers, lipids, surfactants) that act as mediators between the lipophilic Coenzyme Q10 and the aqueous gastrointestinal environment. These intermediaries solubilize CoQ10 and facilitate its dissolution and absorption without requiring the CoQ10 to maintain its crystalline structure
3Ease of operation
If high lipophilicity of Coenzyme Q10 is maintained, then membrane permeability is enhanced, but solubility in gastrointestinal fluids is reduced
Solution Approach 1:
The patent changes the solubility parameter by transforming CoQ10 from crystalline to amorphous form and incorporating it into hydrophilic matrices. This increases aqueous solubility in gastrointestinal fluids while the amorphous nature and matrix composition preserve membrane permeability characteristics
Solution Approach 2:
The patent develops composite solid dispersions using combinations of hydrophilic polymers, lipids, and surfactants that create a dual-function system: the hydrophilic components increase solubility in gastrointestinal fluids while the lipid components and amorphous structure maintain membrane permeability for optimal absorption
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 solid dispersion increases oral bioavailability and stability of Coenzyme Q10, allowing for more effective absorption and systemic circulation, as demonstrated by improved pharmacokinetic parameters in rat studies.
Implementation Method 1
preparing a solid dispersion of Coenzyme Q10 and phospholipids, in the presence of other ingredients such as cellulose derivatives... allows a high degree of amorphization of Coenzyme Q10, determining an increased solubility, a faster dissolution rate
Implementation Method 2
The role of phospholipids may not be limited to facilitate the dispersion of Coenzyme Q10 in the gastro-intestinal fluids
Implementation Method 3
can also have the effect of enhancing the capacity of Coenzyme Q10 to cross the lipid-rich biomembranes and to reach the circulation
Implementation Method 4
The above mentioned cellulosic derivatives and other polymeric materials can contribute to stabilize the amorphous form of Coenzyme Q10 in order to avoid its re-crystallization in the less bioavailable crystalline form
Data Source
AI summary
The invention relates to a solid dispersion comprising Coenzyme Q10 and a phospholipid, in the presence of a cellulosic derivative and/or a polymeric material selected from the group consisting of polyvinylpyrrolidone, polyvinyl acetate, poly (methacrylic acid, methyl methacrylate), poloxamers, chitosan, alginates, hyaluronic acid, pectin, pullulan, cyclodextrins, starch polymers, D-alpha-tocopheryl polyethylene glycol 1000 succinate.