Co-administering Rosiglitazone and EPA to Reduce Triglycerides

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Solution Overview

Problem

Current treatments for cardiovascular diseases, particularly those involving rosiglitazone, often increase the risk of heart attacks and fail to effectively manage triglyceride levels and cardiovascular events.

Innovation Solution

Administering a pharmaceutical composition comprising eicosapentaenoic acid or its derivatives, either alone or in combination with rosiglitazone, to reduce triglycerides and mitigate cardiovascular risks, with a formulation that includes ethyl eicosapentaenoate as the primary fatty acid component, ensuring a steady state plasma concentration of rosiglitazone and minimizing alterations to its pharmacokinetic parameters.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If rosiglitazone is administered to treat cardiovascular diseases, then cardiovascular disease treatment is improved, but the risk of heart attacks increases and triglyceride levels are not effectively managed

Engineering Contradiction:

Improvecardiovascular disease treatmentVSAvoidheart attack risk

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

EPA acts as an intermediary substance that modifies the metabolic effects of rosiglitazone. The patent combines rosiglitazone with EPA to achieve cardiovascular protection while avoiding the harmful effects of rosiglitazone monotherapy, particularly heart attack risk and triglyceride elevation

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent creates a composite therapeutic regimen combining two substances (rosiglitazone and EPA) to achieve effects that neither substance can provide alone, while avoiding the adverse effects of the individual components

Inventive Principle:

Principle #40Composite materials

2Reliability

If rosiglitazone is administered to treat cardiovascular diseases, then cardiovascular disease treatment is improved, but triglyceride levels are not effectively managed

Engineering Contradiction:

Improvecardiovascular disease treatmentVSAvoidtriglyceride levels

Core Design Contradiction:

ReliabilityVSQuantity of substance

Solution Approach 1:

EPA serves as a mediator that counteracts the triglyceride-elevating effect of rosiglitazone while preserving its cardiovascular benefits. The combination therapy uses EPA to modulate lipid metabolism in a way that prevents triglyceride accumulation

Inventive Principle:

Principle #24Intermediary (Mediator)

3Reliability

If eicosapentaenoic acid is co-administered with rosiglitazone, then triglyceride levels are reduced and cardiovascular risk is decreased, but the pharmacokinetic profile of rosiglitazone must be maintained within a specific range

Engineering Contradiction:

Improvetriglyceride reduction and cardiovascular risk decreaseVSAvoidrosiglitazone plasma concentration

Core Design Contradiction:

ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent optimizes the dosage parameters of both EPA and rosiglitazone to achieve the desired therapeutic effect while maintaining rosiglitazone plasma concentrations within 70-135% of baseline values. This involves carefully controlling the amounts and timing of administration

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentUS10966968B2Co-administration of rosiglitazone and eicosapentaenoic acid or a derivative thereof

Publication Date: 2021.04.06 AMARIN PHARMACEUTICALS IRELAND LIMITED(IE)

AI summary

In various embodiments, the present invention provides methods of treating and/or preventing cardiovascular-related disease and, in particular, a method of reducing triglycerides in a subject on rosiglitazone therapy, the method comprising administering to a subject in need thereof a pharmaceutical composition comprising eicosapentaenoic acid or a derivative thereof.