Morphine Naloxone Matrix Abuse Deterrent Formulation

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Solution Overview

Problem

Current treatments for opiate dependency, such as methadone, have varying effects and significant side-effects, and existing formulations can be easily separated by addicts for improper use, leading to challenges in preventing non-oral abuse and maintaining effective substitution therapy.

Innovation Solution

A non-separable combination of morphine and an opiate antagonist with low oral bioavailability, specifically morphine and naloxone, is administered only orally, preventing non-oral abuse by ensuring that if taken improperly, withdrawal symptoms occur due to the antagonist's full effect, and the formulation is designed to prevent mechanical or visual separation of the active ingredients.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of manufacture

If a semipermeable wall dosage form with separated opioid and antagonist layers is used, then the opioid can be obtained through separation measures, but the risk of non-oral abuse increases

Engineering Contradiction:

Improveease of manufactureVSAvoidnon-oral abuse

Core Design Contradiction:

Ease of manufactureVSObject-affected harmful factors

Solution Approach 1:

The patent combines the opioid and antagonist into a single homogeneous matrix without physical separation layers. This merging prevents addicts from mechanically separating the components to obtain pure opioid, thereby eliminating the abuse pathway while maintaining the substitution therapy function.

Inventive Principle:

Principle #5Merging (Combining)

Solution Approach 2:

The invention uses a composite material system where opioid and antagonist are distributed throughout a single matrix material. This composite structure ensures that both substances are released together in fixed proportions, preventing selective extraction of the opioid component for abuse purposes.

Inventive Principle:

Principle #40Composite materials

2Reliability

If methadone is used as a substitute, then withdrawal symptoms are alleviated, but the drug produces high dependency and significant side-effects

Engineering Contradiction:

Improveeffectiveness in alleviating withdrawal symptomsVSAvoidside-effects and dependency

Core Design Contradiction:

ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent changes the pharmacological parameters by using morphine (a natural opiate) instead of methadone (a synthetic opiate), and controls the release kinetics through the matrix formulation. This provides more predictable physiological effects with fewer side-effects while maintaining withdrawal symptom relief.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The matrix formulation provides continuous, controlled release of both opioid and antagonist, ensuring steady therapeutic levels in the bloodstream. This continuous action maintains withdrawal symptom relief while preventing the peaks and troughs that contribute to dependency and side-effects.

Inventive Principle:

Principle #20Continuity of useful action

3Duration of action of moving object

If controlled-release preparations with retarded morphine and retarded antagonist are used, then the release is prolonged, but the physical separation of layers makes separation measures easy

Engineering Contradiction:

Improveduration of actionVSAvoidease of separation

Core Design Contradiction:

Duration of action of moving objectVSEase of operation

Solution Approach 1:

The patent merges the retarded release mechanism into a single matrix for both opioid and antagonist, eliminating the layered structure. This prevents mechanical separation while maintaining the prolonged controlled-release effect through the matrix's release kinetics.

Inventive Principle:

Principle #5Merging (Combining)

4Object-affected harmful factors

If commercial painkiller preparations with opioid and naloxone are used, then improper use is prevented, but the preparations are not suitable as drug substitutes

Engineering Contradiction:

Improveimproper use preventionVSAvoidsuitability as drug substitute

Core Design Contradiction:

Object-affected harmful factorsVSAdaptability or versatility

Solution Approach 1:

The patent creates a formulation that serves dual functions: it prevents improper use through the antagonist's abuse-deterrent effect while simultaneously serving as an effective substitution therapy. The matrix ensures both therapeutic efficacy and abuse prevention in a single product.

Inventive Principle:

Principle #6Universality (Multi-functionality)

Data Source

PatentUS10507205B2Methods of treating opiate dependency and preventing non-oral opiate abuse among opiate addicts

Publication Date: 2019.12.17 PURDUE PHARMACEUTICAL PRODUCTS LP

AI summary

The present invention relates to the use of an inseparable combination of morphine and at least one opiate antagonist with a bioavailability of less than 5% on oral administration for producing a medicament to be administered orally for treatment of opiate dependency in humans and to the use of an inseparable combination of an opiate and at least one opiate antagonists with a bioavailability of less than 5% on oral administration for producing a medicament to be administered orally for prevention of non-oral opiate abuse in opiate addicts.