Abuse-Resistant Oxymorphone Tablet with Barrier Layer
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current pharmaceutical formulations of opioid agonists, such as oxycodone, are vulnerable to abuse due to their ability to be crushed or dissolved, leading to rapid bioavailability and increased risk of overdose, as they do not effectively deter methods like snorting, swallowing, or injection, despite being designed for oral administration.
Innovation Solution
An abuse-resistant oral pharmaceutical composition featuring a barrier layer and a diffusion layer, optionally with an expansion layer, that slows down drug release when the formulation is physically compromised, making it difficult to achieve rapid euphoria or overdose, by maintaining a controlled release profile even when the dosage form is altered.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If sustained release formulations are designed to release drug over extended time, then therapeutic efficacy is improved, but the formulations become vulnerable to abuse by crushing or grinding
Solution Approach 1:
The tablet is divided into multiple functional layers: an outer barrier layer that resists dissolution and crushing, and an inner core layer containing the sustained-release drug formulation. This segmentation allows the barrier layer to prevent abuse while the core layer maintains extended drug release, resolving the contradiction between durability and abuse resistance.
Solution Approach 2:
The invention uses composite material structures combining different polymers and materials with complementary properties. The barrier layer uses dissolution-resistant materials while the core layer uses sustained-release matrices, creating a composite tablet that simultaneously achieves extended duration and abuse deterrence through the synergistic properties of its components.
2Object-affected harmful factors
If the formulation is made resistant to crushing and dissolution, then abuse potential is reduced, but drug release may be compromised
Solution Approach 1:
By segmenting the tablet into barrier and core layers, the barrier layer can be optimized for resistance to crushing and dissolution without affecting the core layer's drug release kinetics. The barrier layer acts as a protective shell that does not interfere with the sustained-release mechanism of the core, maintaining both abuse resistance and proper drug release rate.
Solution Approach 2:
The barrier layer serves as an intermediary between the external environment and the drug-containing core. It mediates by resisting abusive actions (crushing, dissolution) while allowing the core to function normally, thus protecting the drug release system without compromising productivity.
3Quantity of substance
If multiple tablets are taken to achieve high serum concentration, then therapeutic effect is improved, but risk of overdose increases
Solution Approach 1:
The invention changes the physical and chemical parameters of the tablet formulation to create a dissolution-resistant barrier layer that prevents rapid drug release. This parameter change ensures that even if multiple tablets are compromised, the drug releases slowly and controllably, reducing the risk of overdose while maintaining the ability to achieve therapeutic doses through proper administration.
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 significantly reduces the intensity and rate of euphoria when administered improperly, making it harder for abusers to achieve a 'high' and decreases the risk of overdose by maintaining a controlled drug release, even when the formulation is compromised, thus providing a safer therapeutic delivery.
Implementation Method 1
a diffusion layer, comprising a second polymer, substantially covering the barrier layer, wherein the diffusion layer is bonded to the barrier layer and comprises a drug that is substantially homogeneously distributed within the second polymer and diffuses from the diffusion layer within the gastrointestinal (GI) tract
Data Source
AI summary
An abuse resistant oral pharmaceutical composition, comprising: a barrier layer, comprising a first polymer; a diffusion layer, comprising a second polymer, substantially covering the barrier layer, wherein the diffusion layer is bonded to the barrier layer and comprises a drug that is substantially homogeneously distributed within the second polymer and diffuses from the diffusion layer within the gastrointestinal (GI) tract; and optionally an expansion layer comprising an expandable polymer, wherein the expansion layer is substantially covered by the barrier layer. Methods of making the same and methods of using the same are also provided.