Serotonin Surge Protector Formulations Using Gel-Forming Polymers

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Solution Overview

Problem

Current pharmaceutical formulations of proserotonergic agents do not effectively prevent or minimize the risk of serotonin syndrome, a potentially life-threatening adverse drug experience caused by excessive serotonin levels, especially in cases of accidental or intentional overdose and co-ingestion with other serotonergic agents.

Innovation Solution

Development of serotonin surge protector (SSP) formulations that incorporate polymeric and nonpolymeric gel forming agents, viscosity enhancing agents, and high melting point waxes to resist crushing, dissolving, or extraction, thereby reducing the peak concentration and area under the plasma concentration time curve of proserotonergic agents, thus minimizing the incidence and severity of serotonin syndrome.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If proserotonergic agents are administered to treat depression or other conditions, then therapeutic effect is achieved, but risk of serotonin syndrome increases due to excessive serotonin levels

Engineering Contradiction:

Improvetherapeutic effectVSAvoidserotonin syndrome risk

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

A gel-forming polymer is introduced as an intermediary substance between the proserotonergic agent and the patient's system. The polymer forms a gel that controls the release rate of the active ingredient, mediating the delivery to prevent excessive serotonin levels while maintaining therapeutic efficacy

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention changes the physical state and release parameters of the proserotonergic agent by incorporating it into a gel matrix. This modifies the release kinetics from immediate to controlled/sustained release, preventing peak concentration spikes that could cause serotonin syndrome

Inventive Principle:

Principle #35Parameter changes

2Duration of action of moving object

If proserotonergic agents are formulated for extended release, then duration of action increases, but peak concentration may still be excessive in cases of overdose or co-ingestion

Engineering Contradiction:

Improveduration of actionVSAvoidpeak concentration

Core Design Contradiction:

Duration of action of moving objectVSQuantity of substance

Solution Approach 1:

The invention uses a composite material system consisting of the proserotonergic agent embedded within a gel-forming polymer matrix. This composite structure provides both extended duration of action through sustained release and limits peak concentration through the gel's controlled release mechanism, even in overdose scenarios

Inventive Principle:

Principle #40Composite materials

3Ease of manufacture

If conventional pharmaceutical formulations are used, then ease of manufacture is maintained, but ability to prevent serotonin syndrome is insufficient

Engineering Contradiction:

Improveformulation simplicityVSAvoidprevention of serotonin syndrome

Core Design Contradiction:

Ease of manufactureVSReliability

Solution Approach 1:

The invention modifies the physical parameters of the formulation by using gel-forming polymers that can be incorporated into conventional pharmaceutical manufacturing processes. This maintains ease of manufacture while fundamentally changing the release characteristics to prevent serotonin syndrome

Inventive Principle:

Principle #35Parameter changes

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

SSP formulations effectively reduce the peak concentration and systemic exposure of proserotonergic agents, preventing serotonin syndrome by forming viscous gels that deter rapid release or extraction, thereby minimizing the risk of serotonin syndrome in therapeutic and non-medical settings.

Implementation Method 1

Methodology Applied

Scientific EffectGel formation: Gel

Implementation Method 2

Methodology Applied

Scientific EffectViscosity enhancement:

Data Source

PatentUS8329744B2Methods of preventing the serotonin syndrome and compositions for use thereof

Publication Date: 2012.12.11 RELMADA THERAPEUTICS INC

AI summary

The present invention is directed at methods for preventing or minimizing the intensity of the serotonin syndrome in humans and lower animals which comprises administering proserotonergic agents and serotonin surge protectors. The present invention is also directed to pharmaceutical compositions comprising proserotonergic agents and serotonin surge protectors useful for carrying out the method of the present invention.