Abuse-Resistant Opioid Composition with Clay Matrix

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Solution Overview

Problem

Current opioid analgesic compositions are vulnerable to abuse through routes like snorting, inhalation, and parenteral administration, and they experience dose dumping when co-ingested with alcohol, posing safety risks and challenges in maintaining controlled release mechanisms.

Innovation Solution

A composition comprising narcotic analgesics in a liquid or semi-solid matrix with clays, controlled release agents, and oily or waxy substances, along with nasal irritants, to prevent abuse and dose dumping by creating a physicochemical barrier that discourages crushing, dissolving, and inhalation, while maintaining integrity during transit in the gastrointestinal tract.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional opioid analgesic compositions are used, then therapeutic efficacy is achieved, but they are vulnerable to abuse through snorting, inhalation, and parenteral administration

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidabuse potential
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent incorporates nasal irritants that cause discomfort when the formulation is snorted or inhaled, converting the harmful abuse route into an unpleasant experience that deters abuse while maintaining therapeutic efficacy through oral administration

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

Solution Approach 2:

The patent uses a composite formulation containing opioid analgesic, clay, controlled release agent, and oily or waxy substance that work together to prevent abuse through multiple mechanisms while maintaining controlled release and therapeutic effect

Inventive Principle:
Principle #40Composite materials

2Duration of action of moving object

If extended release opioid formulations are used, then controlled release is achieved, but they experience dose dumping when co-ingested with alcohol

Engineering Contradiction:
Improvecontrolled release durationVSAvoidrelease mechanism stability
Core Design Contradiction:
Duration of action of moving objectVSReliability

Solution Approach 1:

The patent uses clay as an intermediary material that interacts with alcohol to prevent the disruption of the controlled release mechanism, acting as a buffer that maintains formulation integrity even in the presence of alcohol

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The composite formulation combines controlled release agents with clay and oily or waxy substances to create a robust matrix that resists alcohol-induced dose dumping while maintaining extended release characteristics

Inventive Principle:
Principle #40Composite materials

3Object-affected harmful factors

If opioid formulations are made abuse-resistant by crushing and dissolving prevention, then abuse potential is reduced, but ease of manufacture and formulation complexity increase

Engineering Contradiction:
Improveabuse potentialVSAvoidformulation complexity
Core Design Contradiction:
Object-affected harmful factorsVSDevice complexity

Solution Approach 1:

The patent merges multiple anti-abuse mechanisms (clay inclusion, controlled release agent, oily or waxy substance, nasal irritant) into a single integrated formulation that prevents abuse through multiple pathways without requiring complex multi-component systems

Inventive Principle:
Principle #5Merging (Combining)

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

The composition significantly reduces abuse potential and prevents dose dumping in the presence of alcohol, ensuring controlled release and safety by making it difficult to extract the drug through illicit routes and maintaining therapeutic efficacy.

Implementation Method 1

liquid or semi-solid matrix or magma or paste

Methodology Applied
Scientific EffectViscosity:

Implementation Method 2

pseudoplastic or thixotropic nature

Methodology Applied
Scientific EffectThixotropy: Thixotropy

Implementation Method 3

controlled release agents

Methodology Applied
Scientific EffectControlled release:

Implementation Method 4

pharmaceutically acceptable nasal irritants when present bring about nasal irritation and annoyance feeling

Methodology Applied
Scientific EffectIrritation:

Implementation Method 5

prevents and makes it harder for dose dumping of opioid agonists or narcotic analgesics in the presence of alcohol

Methodology Applied
Scientific EffectAlcohol resistance:

Data Source

PatentUS10960077B2Abuse and alcohol resistant drug composition
Publication Date: 2021.03.30 1001112561 ONTARIO INC

AI summary

A liquid or semi-solid matrix or magma or paste which is non-newtonian, thixotropic and pseudoplastic and composed of one or more controlled release agent, and/or one or more clays such as bentonite and/or one or more fillers in a non aqueous vehicle, and optionally materials selected from disintegrants, humectants, surfactants and stabilizers. The composition and physicochemical properties makes it harder or prevents dose dumping of narcotic analgesics in the presence of alcohol and harder to abuse opiod agonists or narcotic analgesics and discourages drug abuse via crushing, milling or grinding the dosage form to powder or heating the dosage form to vapour and snorting or inhalation by the nasal route or dissolving to abuse via the parenteral route.