Morphine Sulfate Abuse Deterrent Matrix via Polyethylene Oxide

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Solution Overview

Problem

Current extended release formulations of morphine sulfate are prone to abuse due to their potential for physical manipulation, such as crushing or dissolving, which can lead to higher exposure to the active pharmaceutical ingredient.

Innovation Solution

A solid oral extended release pharmaceutical dosage form comprising a cured extended release matrix formulation of morphine sulfate and polyethylene oxide, which provides improved abuse-deterrent properties by increasing the breaking strength, cracking force, and crush resistance, while maintaining similar bioavailability to existing commercial products like MS Contin®.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If extended release formulations of morphine sulfate are used to provide slow, continuous release for prolonged pain relief, then the duration of action and patient convenience are improved, but the formulations become more prone to abuse through physical manipulation such as crushing, grinding, and solvent extraction

Engineering Contradiction:

Improveduration of pain reliefVSAvoidabuse potential

Core Design Contradiction:

Duration of action of moving objectVSObject-affected harmful factors

Solution Approach 1:

The patent employs a composite matrix formulation combining polyethylene oxide (PEO) with morphine sulfate. The PEO matrix provides both the extended release mechanism and abuse-deterrent properties. This composite structure prevents easy extraction of the active ingredient while maintaining controlled release, thereby resolving the contradiction between prolonged therapeutic effect and reduced abuse potential

Inventive Principle:

Principle #40Composite materials

Solution Approach 2:

The patent utilizes specific molecular weight ranges of polyethylene oxide (1,000,000 to 10,000,000) to achieve both extended release and abuse deterrence. By carefully selecting and controlling the molecular weight parameter of the polymer matrix, the formulation maintains slow drug release for prolonged pain relief while simultaneously preventing manipulation techniques such as crushing and solvent extraction that characterize abuse scenarios

Inventive Principle:

Principle #35Parameter changes

2Strength

If the extended release matrix is made more resistant to manipulation to reduce abuse, then the mechanical strength and crush resistance are improved, but the complexity of the formulation increases

Engineering Contradiction:

Improvecrush resistanceVSAvoidformulation complexity

Core Design Contradiction:

StrengthVSDevice complexity

Solution Approach 1:

The polyethylene oxide matrix serves multiple functions simultaneously: it acts as the extended release mechanism, provides mechanical strength and crush resistance, and prevents solvent extraction. This multi-functionality reduces formulation complexity compared to using separate components for each function, as the PEO matrix inherently provides all three critical properties through its polymer structure and physical characteristics

Inventive Principle:

Principle #6Universality (Multi-functionality)

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 dosage form effectively reduces the potential for physical manipulation and abuse by enhancing its mechanical resistance, while ensuring consistent and prolonged drug release, thus maintaining therapeutic efficacy and patient safety.

Implementation Method 1

Extended release formulations of opioids have been developed to provide slow, continuous release of the opioid for prolonged pain relief

Methodology Applied

Scientific EffectDiffusion: Diffusion

Implementation Method 2

The tablets or multi-particulates are disclosed therein to be resistant to alcohol extraction and to dose dumping when concomitantly used with or in contact with alcohol

Methodology Applied

Scientific EffectMatrix erosion:

Implementation Method 3

a use of polyethylene oxide for increasing the breaking strength and/or the cracking force and/or the crush resistance of a solid oral extended release pharmaceutical dosage form

Methodology Applied

Scientific EffectMechanical reinforcement:

Implementation Method 4

The dosage forms of the present invention offer improved characteristics, such as a reduced potential for physical manipulation (including crushing, grinding, solvent extraction, injection, inhaling)

Methodology Applied

Scientific EffectMechanical resistance:

Data Source

PatentUS20250127715A1Abuse deterrent morphine sulfate dosage forms

Publication Date: 2025.04.24 PURDUE PHARMA LP

AI summary

The present invention relates to a solid oral extended release pharmaceutical dosage form comprising a cured extended release matrix formulation, the extended release matrix formulation comprising:a therapeutically effective amount of morphine sulfate, andpolyethylene oxide.The invention further relates to a process of preparing the dosage form as well as to a method of treating pain by administering the dosage form