EPA DHA Ethyl Ester Preconcentrate for Bioavailability
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Solution Overview
Problem
Current compositions of omega-3 fatty acids, such as eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA), face challenges in solubilization, digestion, and bioavailability due to the carboxylic acid functional group, which hinders their absorption across cell membranes, and existing delivery systems may not enhance their hydrolysis and absorption effectively.
Innovation Solution
A pharmaceutical preconcentrate comprising a fatty acid oil mixture with at least 75% EPA and DHA in ethyl ester or triglyceride form, combined with surfactants like polysorbate 20 and polysorbate 80, and potentially ethanol as a co-surfactant, forming self-nanoemulsifying, self-microemulsifying, or self-emulsifying drug delivery systems to improve solubility and absorption.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If omega-3 fatty acids are administered in conventional forms, then they can be delivered to subjects, but their solubility and bioavailability are limited due to the carboxylic acid functional group hindering absorption
Solution Approach 1:
The patent converts omega-3 fatty acids from carboxylic acid form to ethyl ester form, changing the chemical parameter to improve absorption. This esterification removes the problematic carboxylic acid functional group while maintaining the essential fatty acid structure, thereby enhancing bioavailability without sacrificing therapeutic effect
Solution Approach 2:
The patent introduces surfactants as intermediary substances to facilitate the absorption of omega-3 fatty acids. These surfactants act as mediators between the hydrophobic fatty acid molecules and the aqueous environment in the digestive system, enabling improved solubility and cellular uptake
2Ease of operation
If conventional delivery systems are used for omega-3 fatty acids, then administration is simple, but hydrolysis and absorption are not enhanced effectively
Solution Approach 1:
The patent performs preliminary esterification of the omega-3 fatty acids before administration, converting them to ethyl esters that are pre-prepared for better absorption. This preliminary chemical modification ensures that when the substance reaches the digestive system, it is already in an optimized state for hydrolysis and uptake, eliminating the need for complex delivery systems
3Device complexity
If omega-3 fatty acids are administered without modification, then the formulation is simple, but solubility is insufficient
Solution Approach 1:
The patent changes the chemical parameter of omega-3 fatty acids by converting carboxylic acid groups to ethyl ester groups. This parameter change fundamentally alters the solubility characteristics, transforming the substance from poorly soluble to sufficiently soluble in physiological conditions, while maintaining formulation simplicity
Solution Approach 2:
The patent employs surfactants as intermediary agents to enhance solubility. These surfactants create micellar structures that encapsulate the hydrophobic omega-3 fatty acid molecules, allowing them to dissolve in aqueous environments without requiring complex formulation techniques
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 preconcentrate enhances the hydrolysis, solubility, and bioavailability of EPA and DHA, facilitating their absorption and providing therapeutic benefits for conditions like irregular plasma lipid levels, cardiovascular functions, and immune functions, while maintaining stability and ease of administration.
Implementation Method 1
at least one surfactant
Implementation Method 2
enhances the hydrolysis
Data Source
AI summary
A preconcentrate comprising a fatty acid oil mixture that contains EPA and DHA, preferably in the form of ethyl ester or triglyceride, and at least one surfactant. The preconcentrates are capable of forming a self-nanoemulsifying drug delivery system, a self-microemulsifying drug delivery system or a self-emulsifying drug delivery system (SNEDDS, SMEDDS or SEDDS) in an aqueous solution. The application is also directed to a food supplement preconcentrate.