Elastomeric Polymer Matrix for Abuse-Resistant Opioid Delivery
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Solution Overview
Problem
Current opioid formulations are vulnerable to misuse, as they can be crushed or dissolved for immediate release, leading to abuse and overdose, despite efforts to create non-crushable and non-dissolvable pills, as abusers find ways to circumvent these deterrents through heating, freezing, or solvents.
Innovation Solution
A non-crushable and non-dissolvable elastomeric polymer formulation is developed, where oxycodone is physically trapped or covalently bound within elastomeric polymer micro particles with low glass transition temperatures, and enzyme-sensitive peptides are used to ensure release only in the stomach or intestine, combining physical barriers with enzymatic degradation for a two-step safety system.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If traditional opioid formulations are used, then the drug is easily accessible for immediate release, but the formulations are vulnerable to misuse through crushing or dissolving
Solution Approach 1:
The patent uses an elastomeric polymer matrix that forms a flexible, rubbery structure at room temperature and physiological conditions. This elastomeric network physically entraps the opioid drug, preventing traditional crushing or dissolving methods from releasing the drug immediately. The flexible polymer shell maintains its integrity under abuse conditions while allowing controlled drug release through enzymatic degradation in the gastrointestinal tract.
Solution Approach 2:
The patent exploits changes in the physical state of the polymer by selecting elastomeric polymers with glass transition temperatures below room temperature. This parameter change ensures the polymer remains in a rubbery, flexible state under abuse conditions (room temperature, heat, freezing), maintaining its abuse-deterrent properties while allowing the drug to be released under physiological conditions through enzymatic action.
2Reliability
If non-crushable and non-dissolvable formulations are developed, then abuse is deterred, but abusers find ways to circumvent these deterrents through heating, freezing, or solvents
Solution Approach 1:
The patent replaces mechanical abuse-deterrent mechanisms (crushing, dissolving barriers) with a biochemical mechanism. Instead of relying on physical barriers that can be overcome by mechanical force or solvents, the formulation uses an elastomeric polymer matrix that requires specific enzymatic degradation for drug release. This substitution makes the formulation resistant to heating, freezing, and solvent exposure, as these conditions do not degrade the polymer matrix.
Solution Approach 2:
The patent converts the potential harm of abuse attempts into a benefit by designing the elastomeric polymer to be stable under abuse conditions (heat, freezing, solvents) but specifically degradable by gastrointestinal enzymes. Attempts to circumvent the formulation through heating or freezing actually reinforce the polymer's stability, while the drug is released safely through the intended physiological pathway of enzymatic degradation in the digestive tract.
3Strength
If elastomeric polymer formulations with low glass transition temperatures are used, then the polymer maintains a rubbery state resisting abuse, but the drug release mechanism becomes more complex
Solution Approach 1:
The patent employs self-service by utilizing the body's natural gastrointestinal enzymes to degrade the elastomeric polymer matrix and release the drug. The formulation does not require complex mechanical release mechanisms or external triggers; instead, it relies on the physiological environment's inherent enzymatic activity to automatically degrade the polymer and release the opioid in a controlled manner after successful swallowing and passage through the digestive tract.
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 formulation effectively prevents misuse by maintaining a rubbery state at room temperature, resisting heat and freezing, and requiring specific enzymes for drug release, thus preventing unintended use and overdose.
Implementation Method 1
The polymer has a glass transition temperature (Tg) lower than 23° C.
Implementation Method 2
the drug is trapped either covalently or non-covalently in the at least one inner cavity within the complex, wherein the drug is protected from releasing outside of the complex
Data Source
AI summary
Non-crushable pill formulations and methods of using the formulations are disclosed. A non-crushable pill formulation for preventing unintended use of a drug, comprising a polymer, the polymer forming a polymer backbone of the complex; cross-linkers, the cross-linkers connecting the polymer backbone through covalently bonding to form at least one inner cavity within the complex; and the drug, the drug being trapped either covalently or non-covalently in the at least one inner cavity within the complex, wherein the drug is protected from releasing outside of the complex.