Tamper-Resistant Opioid Formulation via Segmented Matrix
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Solution Overview
Problem
Current pharmaceutical dosage forms of opioid analgesics are vulnerable to tampering and abuse, as they can be crushed or dissolved for immediate release, leading to potential overdose and illicit use, and existing solutions often rely on antagonists or viscosity to deter misuse.
Innovation Solution
A solid oral dosage form comprising particles with a core containing an opioid agonist and an internal adhesion promoter, dispersed in a controlled release matrix, which maintains the controlled release profile even when the dosage form is crushed or exposed to alcohol, using a combination of controlled release materials, adhesion promoters, and alcohol-resistant coatings to prevent immediate release.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If the dosage form is made easily crushable or dissolvable, then the drug is immediately available for rapid pain relief, but the dosage form becomes vulnerable to tampering and abuse
Solution Approach 1:
The dosage form is divided into multiple particles with cores containing the opioid agonist, dispersed in a controlled release matrix. This segmentation maintains the controlled release profile while preventing immediate liberation of the drug upon crushing, as the drug remains enclosed within the matrix structure.
Solution Approach 2:
The invention uses a composite matrix system combining controlled release materials with the opioid agonist. This composite structure provides both the controlled release functionality and resistance to tampering, eliminating the need for separate antagonist components while maintaining safety and efficacy.
2Duration of action of moving object
If the dosage form uses a controlled release matrix, then the drug is released over an extended period, but the dosage form may be dangerous upon crushing due to immediate availability of the drug
Solution Approach 1:
The controlled release matrix is segmented into multiple particles with drug-containing cores. When crushed, the matrix structure remains intact enough to continue controlling drug release, preventing the sudden liberation that would occur with traditional controlled release forms. The segmentation ensures that even when the dosage form is tampered with, the drug release kinetics are maintained.
Solution Approach 2:
The invention creates local differentiation between the core containing the opioid agonist and the surrounding controlled release matrix. This local quality ensures that the drug is only released through the controlled mechanism of the matrix, even when the overall dosage form structure is compromised by crushing or other tampering attempts.
3Reliability
If the dosage form relies on inclusion of an antagonist to deter abuse, then parenteral misuse is reduced, but the formulation complexity increases and may interfere with the pharmacologic action of the active agent
Solution Approach 1:
The invention uses a composite controlled release matrix that inherently provides resistance to both oral and parenteral misuse without requiring separate antagonist components. The matrix structure itself acts as the abuse-deterrent mechanism, simplifying the formulation while maintaining or improving reliability against misuse compared to antagonist-based approaches.
Data Source
AI summary
Disclosed in certain embodiments is a solid oral dosage form comprising a plurality of particles, each particle comprising (i) a core comprising an active agent susceptible to abuse and an internal adhesion promoter, wherein the cores are (i) dispersed in a matrix comprising a controlled release material or (ii) coated with a controlled release material. The dosage form can also include an alcohol resistant material.