Glucomannan Matrix Abuse Deterrent Formulation
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Solution Overview
Problem
Current pharmaceutical compositions that provide extended release of active ingredients face challenges in deterring abuse, particularly due to the limitations of polyethylene oxide-based formulations which can be sensitive to oxidation and unsuitable for thermolabile APIs, and may cause adverse effects with bitter agents.
Innovation Solution
The development of pharmaceutical compositions incorporating glucomannan, a polyalkylene oxide with a molecular weight of up to 300,000, and a high molecular weight polyethylene oxide, which forms a solid dosage form that is resistant to crushing and forms a viscous gel when contacted with an aqueous solution, thereby deterring abuse.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If polyethylene oxide is used to provide extended release and abuse deterrence, then mechanical integrity and abuse resistance are improved, but the formulation becomes sensitive to oxidation and unsuitable for thermolabile APIs
Solution Approach 1:
The patent introduces glucomannan as an intermediary substance that forms a protective matrix around the API, physically isolating it from oxidative environments while maintaining the extended release properties. This intermediary layer prevents direct contact between the API and oxidizing agents without compromising the abuse deterrent characteristics of the polyethylene oxide matrix.
Solution Approach 2:
The patent creates a composite material system combining glucomannan and polyethylene oxide with different molecular weights. This composite structure leverages the oxidation resistance of glucomannan to protect thermolabile APIs while maintaining the abuse deterrent and extended release properties provided by the polyethylene oxide matrix.
2Strength
If polyethylene oxide is used to form a solid dosage form resistant to crushing, then abuse deterrence is improved, but the formulation becomes unsuitable for thermolabile APIs due to curing temperature requirements
Solution Approach 1:
Glucomannan serves as a thermal intermediary that allows the formulation to achieve mechanical integrity at lower temperatures. The glucomannan matrix can be formed and cured at temperatures suitable for thermolabile APIs, while still providing the crushing resistance needed for abuse deterrence through its interaction with the polyethylene oxide.
Solution Approach 2:
The patent changes the thermal parameters of the formulation by incorporating glucomannan, which alters the curing temperature requirements. This parameter change enables the use of lower temperatures during formulation and storage, making the dosage form suitable for thermolabile APIs while maintaining the mechanical strength required for abuse resistance.
3Reliability
If bitter agents are added to deter abuse, then abuse resistance is improved, but adverse effects occur in the patient population
Solution Approach 1:
The patent extracts and removes the need for bitter agents by using physical and chemical properties of the dosage form itself (matrix structure, gel formation, crushing resistance) to provide abuse deterrence. This eliminates the harmful adverse effects associated with bitter agents while maintaining effective abuse resistance through the formulation's inherent properties.
Solution Approach 2:
The patent converts the potential harm of using harsh abuse deterrent substances into a benefit by using naturally derived glucomannan and food-grade polyethylene oxide. These materials provide abuse resistance through their physical properties (matrix structure, gel formation) rather than through harmful chemical effects, turning a potentially harmful approach into a safe and effective one.
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 compositions achieve extended release and abuse deterrence by maintaining mechanical integrity and forming a viscous gel, preventing easy manipulation or injection, while being less prone to oxidative degradation and suitable for a wider range of APIs.
Implementation Method 1
forming a viscous gel when contacted with an aqueous solution
Implementation Method 2
The polymeric matrix tablet has increased hardness and retains a plastic-like nature after curing
Implementation Method 3
after curing at a temperature above the softening temperature of the polyethylene oxide
Data Source
AI summary
A pharmaceutical composition comprising at least one active pharmaceutical ingredient (API) or a pharmaceutically acceptable salt thereof, a glucomannan, a first polyalkylene oxide having an average molecular weight of no more than 300,000, and a second polyalkylene oxide having an average molecular weight of at least 1,000,000 and methods of making. The pharmaceutical composition provides extended release of the API and has abuse deterrent features.