Pharmaceutical Composition Using Deliquescent Plasticizer for Abuse Deterrent Release
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Solution Overview
Problem
Current pharmaceutical compositions with extended release and abuse deterrent properties face challenges in manufacturing, as they often result in sticky, non-flowable materials that are difficult to process using conventional equipment, and may not effectively resist tampering due to limitations with polyethylene oxide-based formulations.
Innovation Solution
The development of a pharmaceutical composition comprising hydrophilic plastomers, hydrophilic elastomers, and deliquescent plasticizers, which are humidified to plasticize the polymers, then heated to create a solid dosage form that is resistant to crushing and tampering, providing extended release and abuse deterrent properties.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If polyethylene oxide-based formulations are used to provide extended release and abuse deterrent properties, then the formulation forms a viscous gel when exposed to solvents preventing abuse, but the material becomes sticky and non-flowable making it difficult to manufacture using conventional equipment
Solution Approach 1:
The patent changes the physical and chemical parameters of the polymer matrix by using hydrophilic elastomers with specific glass transition temperatures and molecular weights, along with plasticizers in optimized ratios, to achieve a balance between manufacturability and abuse deterrent properties while maintaining extended release characteristics
Solution Approach 2:
The patent employs composite material systems combining hydrophilic elastomers, plasticizers, and APIs in specific formulations that provide both processing advantages (reduced stickiness, improved flowability) and functional advantages (extended release, abuse deterrent gel formation) that single-component systems cannot achieve
2Strength
If polymers are plasticized to impart abuse deterrent properties and extended release, then the formulation provides tamper resistance, but the plasticized polymer mass becomes sticky and non-flowable posing processing problems in milling, blending, and compressing
Solution Approach 1:
The patent optimizes the glass transition temperature of the polymer matrix through selection of specific hydrophilic elastomers and plasticizer combinations, achieving a parameter range that provides sufficient tamper resistance while maintaining adequate flowability and processability during manufacturing operations
Solution Approach 2:
The patent applies different functional properties to different aspects of the formulation: the polymer matrix provides structural integrity and tamper resistance, while the plasticizer system provides processability and flowability, creating local quality differentiation that resolves the contradiction between strength and ease of operation
3Reliability
If high molecular weight gel forming polymers are incorporated to create a physical barrier against abuse, then the tablet dosage form becomes difficult to crush or chew, but the formulation requires tight control of curing conditions limiting tamper resistant properties
Solution Approach 1:
The patent changes the curing parameters and polymer selection to achieve gel formation and tamper resistance without requiring tight control of curing conditions, using hydrophilic elastomers and plasticizers that provide flexible processing windows while maintaining functional performance
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 effectively resists tampering by maintaining mechanical integrity and forming a viscous gel when exposed to solvents, thereby preventing abuse, while being manufacturable using conventional equipment.
Implementation Method 1
at least one deliquescent plasticizer
Implementation Method 2
forming a viscous gel when the dosage form comes into contact with a suitable solvent
Implementation Method 3
The polymeric matrix tablet has increased hardness and retains a plastic-like nature after curing at a temperature above the softening temperature of the polyethylene oxide
Data Source
AI summary
Pharmaceutical compositions comprising at least one active pharmaceutical ingredient or a pharmaceutically acceptable salt thereof, at least one hydrophilic plastomer, at least one hydrophilic elastomer, and at least one deliquescent plasticizer, wherein the pharmaceutical compositions provide extended release of the API and have abuse deterrent properties. Methods for preparing the pharmaceutical compositions in which the components of the composition are humidified such that the deliquescent plasticizer deliquesces, thereby plasticizing the hydrophilic polymers.