Phenserine Extended-Release Formulation for Concussion Treatment

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Solution Overview

Problem

Current treatments for traumatic brain injuries (TBI) and related neurodegenerative diseases lack effective pharmacological interventions to mitigate neuropathological degenerative impairments and prevent anecrotic cell death, leading to significant cognitive and functional deficits with no available drugs to address these issues.

Innovation Solution

The development of extended, controlled-release formulations of phenserine, combined with anti-inflammatory drugs like steroids or NSAIDs, to provide sustained therapeutic concentrations that prevent anecrotic cell death and mitigate pathologies associated with TBI, concussion, and neurodegenerative diseases such as Parkinson's and Alzheimer's.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If conventional immediate-release formulations are used, then peak drug concentration is achieved quickly, but therapeutic effect duration is insufficient to prevent anecrotic cell death

Engineering Contradiction:

Improveduration of therapeutic effectVSAvoidrate of drug concentration achievement

Core Design Contradiction:

Duration of action of moving objectVSSpeed

Solution Approach 1:

The patent applies dynamic dosing through extended-release formulations that progressively release phenserine over time, transforming the static immediate-release profile into a dynamic sustained-release system. This resolves the contradiction by maintaining therapeutic concentrations throughout the critical period needed to prevent anecrotic cell death while still achieving effective concentrations.

Inventive Principle:

Principle #15Dynamics

Solution Approach 2:

The extended-release formulation performs preliminary action by establishing and maintaining therapeutic drug levels before the onset of anecrotic cell death. The sustained-release mechanism ensures drug availability is prepared in advance and continues throughout the vulnerable period, preventing cell death rather than responding after damage occurs.

Inventive Principle:

Principle #10Preliminary action

2Reliability

If high doses are administered to ensure therapeutic coverage, then neuroprotective effect is enhanced, but risk of adverse effects increases

Engineering Contradiction:

Improveneuroprotective efficacyVSAvoidadverse effects

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the temporal parameter of drug delivery by using extended-release formulations. This transforms a high-dose short-duration regimen into a lower-dose long-duration regimen, maintaining neuroprotective efficacy while reducing peak concentrations that cause adverse effects. The parameter change in release kinetics resolves the contradiction between reliability and harmful factors.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The extended-release formulation provides continuous therapeutic action at optimized concentrations, ensuring reliable neuroprotection without the peaks and troughs of immediate-release dosing. This continuous delivery maintains effective drug levels throughout the critical period while avoiding concentration spikes that lead to adverse effects.

Inventive Principle:

Principle #20Continuity of useful action

3Reliability

If multiple dosing administrations are used, then therapeutic coverage is improved, but treatment complexity and patient compliance burden increase

Engineering Contradiction:

Improvetherapeutic coverageVSAvoidtreatment regimen complexity

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The patent merges multiple dosing administrations into a single extended-release formulation. The extended-release mechanism consolidates what would require multiple separate doses into one administration that provides sustained therapeutic coverage, reducing treatment complexity while maintaining reliability.

Inventive Principle:

Principle #5Merging (Combining)

Solution Approach 2:

The extended-release formulation serves multiple functions simultaneously: it provides initial therapeutic coverage, maintains sustained drug levels, and eliminates the need for multiple dosing events. This multi-functionality resolves the contradiction by achieving comprehensive therapeutic coverage through a simplified single-dose regimen.

Inventive Principle:

Principle #6Universality (Multi-functionality)

Data Source

PatentUS10111860B1Compositions and methods for treating concussion

Publication Date: 2018.10.30 ARISTEA TRANSLATIONAL MEDICINE CORP

AI summary

Compositions and methods for mitigating a pathology following brain trauma or at least a portion of a cascade of a pathology associated therewith, including compositions and methods for treating concussion or preventing the onset of anecrotic cell death in neurons. Exemplary compositions for treating concussion include an active compound comprising one or more of: phenserine, a phenserine metabolite, a phenserine prodrug, or combinations thereof; and one or more pharmaceutically acceptable excipients. The one or more excipients can be combined with the active compound to form an extended, controlled-release medicament that delivers a therapeutic concentration of the active compound over a period of time. Exemplary methods include administering a therapeutic dose of the active compound and, optionally, a therapeutically acceptable dose of a second active compound, and, optionally, maintaining the therapeutic doses of the active and optional second active compounds at therapeutically effective concentrations over a period of time.