Omega-3 Fatty Acid Amides Lowering Triglycerides and LDL-C

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Solution Overview

Problem

Current omega-3 fatty acid formulations, such as ethyl esters, effectively lower triglycerides but raise LDL-C levels, increasing the risk of cardiovascular diseases, whereas there is a need for a treatment that simultaneously lowers both triglycerides and LDL-C without adverse effects.

Innovation Solution

Formulations containing omega-3 fatty acid amides, particularly ethanolamine amides of eicosapentaenoic (EPA) and docosahexaenoic (DHA) acids, combined with tocotrienols, which are administered orally to lower triglycerides and LDL-C levels without raising LDL cholesterol.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If omega-3 fatty acid ethyl esters are administered to lower triglycerides, then triglyceride levels are reduced, but LDL-C levels are increased

Engineering Contradiction:
Improvetriglyceride levelsVSAvoidLDL-C levels
Core Design Contradiction:
Quantity of substanceVSObject-generated harmful factors

Solution Approach 1:

The patent changes the chemical parameter of the omega-3 fatty acid formulation from ethyl esters to amides (specifically ethanolamine amides). This parameter change fundamentally alters the metabolic pathway and physiological effects, enabling the formulation to lower both triglycerides and LDL-C simultaneously without the adverse LDL-C raising effect of traditional ethyl ester formulations.

Inventive Principle:
Principle #35Parameter changes

2Temperature

If current antihypertensive drugs are used to reduce blood pressure, then blood pressure is lowered, but pulse rate is increased and side effects occur

Engineering Contradiction:
Improveblood pressureVSAvoidpulse rate increase and side effects
Core Design Contradiction:
TemperatureVSObject-generated harmful factors

Solution Approach 1:

The omega-3 fatty acid amide formulation performs multiple therapeutic functions simultaneously: it lowers blood pressure, reduces triglycerides, and decreases LDL-C levels. This multi-functionality eliminates the need for separate medications for each condition, avoiding the side effects and pulse rate increases associated with conventional antihypertensive drugs.

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

Data Source

PatentUS9295658B2Second generation fatty acid compositions, formulations, and methods of use and synthesis thereof
Publication Date: 2016.03.29 ATOSSA THERAPEUTICS INC

AI summary

An orally administered fatty acid composition for the treatment of cardiovascular diseases, and a method of treating same, are provided. The compound includes 5Z,8Z,11Z,14Z,17Z-eicosapentaenoic ethanolamide (EPA ethanolamide), 4Z,7Z,10Z,13Z,16Z,19Z-docosahexaenoic ethanolamide (DHA ethanolamide), and at least one tocotrienol. The EPA ethanolamide and the DHA ethanolamide are preferably each substantially in a range of 100-900 mg per dosage form. The at least one tocotrienol is substantially in a range of 10-500 mg per dosage form. The at least one tocotrienol includes at least one of α-tocotrienol, β-tocotrienol, γ-tocotrienol, or δ-tocotrienol and is preferably substantially tocopherol-free. The composition may take the form of a medical food or a pharmaceutical preparation. A preferred formulation of the composition includes approximately 525 mg EPA ethanolamide, approximately 315 mg DHA ethanolamide, and approximately 50 mg δ-tocotrienol. The EPA and DHA ethanolamides may be synthesized from fatty acid triglycerides.