Oxycodone-Enzyme Composition for Abuse Deterrence
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Solution Overview
Problem
Current abuse-deterrent technologies for opioid medications, such as oxycodone, have not been effective in preventing the most common form of abuse, which involves swallowing intact capsules or tablets to achieve euphoria, and there is a need for innovative approaches to reduce the risk of abuse while ensuring the drug's therapeutic delivery.
Innovation Solution
A pharmaceutical composition comprising oxycodone combined with an oxycodone-processing enzyme, where the enzyme is in a storage-stable, reactive state that remains inactive during normal administration but becomes active when the drug is abused, transforming oxycodone into a less abusive or inactive form, thereby deterring misuse.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Object-affected harmful factors
If oxycodone is formulated with abuse-deterrent technologies to make manipulation more difficult, then the risk of abuse is reduced, but the most common form of abuse (swallowing intact capsules or tablets) cannot be deterred
Solution Approach 1:
The enzyme is incorporated into the formulation in advance, stored in a stable but reactive state, ready to convert oxycodone to inactive metabolites upon activation. This preliminary preparation allows the abuse-deterrent mechanism to activate automatically when abuse occurs, without requiring additional components or steps
Solution Approach 2:
The enzyme's activity state is changed based on environmental conditions. During normal storage and oral administration, the enzyme remains inactive or less active. Upon exposure to abusive conditions (crushing, dissolving in alcohol, heating), the enzyme becomes activated and converts oxycodone to inactive metabolites, changing the chemical state of the drug
2Object-affected harmful factors
If the enzyme is made highly reactive to effectively convert oxycodone upon abuse, then abuse deterrence is improved, but the enzyme may act on oxycodone during normal storage or administration
Solution Approach 1:
The enzyme is pre-incorporated into the formulation in a stable but reactive state, prepared in advance to activate only under abusive conditions. This allows the system to maintain stability during normal handling while being ready to convert oxycodone when needed
Solution Approach 2:
The enzyme's activity is made dynamic rather than static. The enzyme can transition between inactive and active states based on environmental conditions such as pH, temperature, or solvent exposure. This dynamic behavior allows the same enzyme to remain stable during storage but become highly reactive upon abuse
3Object-affected harmful factors
If the enzyme converts oxycodone to inactive form upon abuse, then the harmful effects are reduced, but the therapeutic efficacy may be compromised during normal administration
Solution Approach 1:
The enzyme acts as an intermediary that selectively converts oxycodone to inactive metabolites under abusive conditions. During normal oral administration, the enzyme remains inactive or is protected from contact with oxycodone, allowing therapeutic delivery. Upon abuse (crushing, dissolving in alcohol, heating), the enzyme activates and converts the drug, preventing abuse effects
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 combination effectively reduces the abuse potential of oxycodone by converting it into a less active or inactive form when abused, while ensuring its therapeutic efficacy when administered orally, thus providing a novel and efficient abuse-deterrent strategy for opioid medications.
Implementation Method 1
A pharmaceutical composition comprising oxycodone combined with an oxycodone-processing enzyme, where the enzyme is in a storage-stable, reactive state that remains inactive during normal administration but becomes active when the drug is abused, transforming oxycodone into a less abusive or inactive form
Data Source
AI summary
Disclosed are pharmaceutical compositions comprising oxycodone and an oxycodone-processing enzyme, wherein oxycodone is contained in the pharmaceutical composition in a storage stable, enzyme-reactive state and under conditions wherein no enzymatic activity acts on oxycodone.