Cholesterol Absorption Inhibitor and Omega-3 Fatty Acid Combination

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Solution Overview

Problem

Current treatments for cardiovascular disease (CVD) often fail to effectively reduce multiple risk factors associated with the condition, particularly due to non-compliance with lifestyle modifications and side effects from existing medications, and there is a lack of a single composition that can broadly apply to the population in developed countries.

Innovation Solution

A novel composition combining a cholesterol absorption inhibitor, such as ezetimibe, with a specific omega-3 fatty acid formulation containing a high ratio of Eicosapentaenoic acid (EPA) to Docosahexaenoic acid (DHA) (5.7:1 to 6.3) to enhance lipid profiles and mitigate CVD risk factors, administered orally to achieve sustained vasodilatory effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Adaptability or versatility

If cholesterol absorption inhibitors and omega-3 fatty acids are used separately, then some risk factors are reduced, but multiple CVD risk factors cannot be effectively addressed simultaneously

Engineering Contradiction:
Improveability to address multiple CVD risk factorsVSAvoideffectiveness of treatment
Core Design Contradiction:
Adaptability or versatilityVSReliability

Solution Approach 1:

The patent combines cholesterol absorption inhibitors (ezetimibe) and omega-3 fatty acids into a single pharmaceutical composition. This merging allows the composition to simultaneously address multiple CVD risk factors including total cholesterol, LDL cholesterol, triglycerides, and blood pressure, thereby resolving the contradiction between versatility and reliability in treating CVD.

Inventive Principle:
Principle #5Merging (Combining)

2Reliability

If lifestyle modifications are recommended, then CVD risk factors can be reduced, but patient non-compliance limits effectiveness

Engineering Contradiction:
Improveeffectiveness of risk factor reductionVSAvoidpatient compliance
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent merges multiple therapeutic agents (ezetimibe and omega-3 fatty acids) into a single pharmaceutical composition that can be administered as one daily dose. This simplifies the treatment regimen significantly compared to multiple separate medications or complex lifestyle modifications, thereby improving patient compliance while maintaining reliability in reducing CVD risk factors.

Inventive Principle:
Principle #5Merging (Combining)

3Reliability

If existing medications are used, then some lipid parameters improve, but side effects limit their use

Engineering Contradiction:
Improvelipid parameter improvementVSAvoidmedication side effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent uses omega-3 fatty acids as an intermediary substance that works synergistically with ezetimibe to improve lipid parameters. Omega-3 fatty acids provide cardioprotective effects through anti-inflammatory and vasodilatory mechanisms, allowing the composition to achieve reliable lipid parameter improvement with a reduced side effect profile compared to conventional medications alone.

Inventive Principle:
Principle #24Intermediary (Mediator)

Data Source

PatentUS8952000B2Cholesterol absorption inhibitor and omega 3 fatty acids for the reduction of cholesterol and for the prevention or reduction of cardiovascular, cardiac and vascular events
Publication Date: 2015.02.10 PIVOTAL THERAPEUTICS
  • US8952000B2 patent drawing
  • US8952000B2 patent drawing
  • US8952000B2 patent drawing

AI summary

A composition and a method of treatment utilizing a combination of lipid lowering cholesterol absorption inhibitors, e.g. azetidinones, with mixtures of an omega-3 fatty acid formulation containing about 90% or more omega 3 fatty acids by weight including a combination of Eicosapentaenoic acid (EPA), Docosapentaenoic acid (DPA) and Docosahexaenoic acid (DHA) in a weight ratio of EPA:DHA of from 5.7 to 6.3, wherein the sum of the EPA, DHA and DPA represent about 82% by weight of the total formulation and about 92% of the total omega 3 fatty acid content of the composition are taught. EPA+DHA are about 80% of the total formulation and about 89% of the total omega 3 fatty acid content of the composition. The formulation may further contain specific amounts of arachidonic acid (AA), stearidonic acid (SDA), and alpha-linolenic acid (ALA).