Neuroprotective Composition Using Edaravone and Lipids

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Solution Overview

Problem

Current treatments for stroke and degenerative brain diseases, such as cerebral ischemia, lack effective and safe therapeutic agents, with existing substances either having significant side effects or toxicity issues, and there is a need for alternatives derived from natural resources.

Innovation Solution

A pharmaceutical composition comprising olive oil, along with other substances like egg yolk lecithin, glycerol, sodium oleate, medium chain triglyceride, refined fish oil, and soybean oil, which are combined in specific ratios to provide a safe and effective neuroprotective treatment for stroke and degenerative brain diseases, minimizing toxicity and side effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If tissue plasminogen activator is used to dissolve thrombus and supply oxygen and glucose, then cerebral ischemia is treated, but hemorrhagic brain disease is induced due to thinned blood vessel wall

Engineering Contradiction:

Improveeffectiveness in treating cerebral ischemiaVSAvoidhemorrhagic brain disease

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent uses edaravone as an intermediary substance that acts as a free radical scavenger to protect neuronal cells from oxidative damage without directly dissolving thrombus. This mediator approach allows treatment of ischemia-reperfusion injury without the hemorrhagic side effects of direct thrombolytic agents.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent converts the harmful oxidative stress and free radical damage that occur during ischemia-reperfusion into a beneficial treatment target. By specifically scavenging free radicals and reducing oxidative stress, the treatment transforms the harmful reperfusion injury mechanism into a treatable pathway, protecting neurons without causing hemorrhage.

Inventive Principle:

Principle #22Blessing in disguise (Convert harm into benefit)

2Reliability

If MK-801 (calcium channel blocker) is used to inhibit initial calcium influx, then neuronal cell death is inhibited, but side effects occur leading to drug discard

Engineering Contradiction:

Improveinhibition of neuronal cell deathVSAvoidside effects

Core Design Contradiction:

ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent changes the therapeutic parameter from blocking calcium channels (MK-801) to scavenging free radicals (edaravone). This parameter change allows inhibition of neuronal cell death through a different mechanism that does not produce the harmful side effects associated with calcium channel blocking, thereby improving the therapeutic index.

Inventive Principle:

Principle #35Parameter changes

3Reliability

If synthetic substances are used to treat cerebral ischemia, then therapeutic effect is achieved, but toxicity and side effects increase

Engineering Contradiction:

Improvetherapeutic effectVSAvoidtoxicity

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent employs edaravone, a relatively simple organic compound that acts as a free radical scavenger, replacing complex synthetic neuroprotectants. This substance provides effective neuroprotection with a favorable safety profile, analogous to using a simple, safe, short-acting agent rather than a complex, potentially toxic one.

Inventive Principle:

Principle #27Cheap short-living objects (Disposable)

Data Source

PatentUS11617774B2Composition for preventing or treating stroke or degenerative brain disease

Publication Date: 2023.04.04 UNIVERSITY INDUSTRY COOPERATION GROUP OF KYUNG HEE UNIVERSITY

AI summary

The present invention relates to a composition for preventing and/or treating a stroke or a degenerative brain disease comprising: at least two substances selected from the group consisting of egg yolk lecithin, glycerol, sodium oleate, medium chain triglyceride and refined fish oil; olive oil; and soybean oil. The composition of the present invention has an excellent neuroprotective effect but no toxicity or side effects, and thus can be effectively and safely used for preventing, treating or ameliorating a stroke or a degenerative brain disease.