Abuse-Resistant Drug Formulations with Multi-Particulate Segmentation
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Solution Overview
Problem
Current opioid formulations lack effective abuse-resistant and overdose protection features, as they can be manipulated for non-medical use by crushing, dissolving, or injecting, leading to misuse and overdose incidents.
Innovation Solution
Development of solid oral pharmaceutical compositions with multi-particulates containing a polymer matrix, cationic pH-dependent polymers, and viscosity-building agents, which provide abuse deterrence and overdose protection by resisting physical manipulation and altering drug release characteristics in the gastrointestinal tract.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If opioid formulations are made harder to resist crushing and breaking, then abuse resistance is improved, but difficulty in splitting dosage form for reduced dose administration increases
Solution Approach 1:
The dosage form is divided into multiple unit doses within a single tablet, allowing patients to split the tablet into individual unit doses for reduced dose administration while maintaining the overall structural integrity and abuse resistance of the formulation
Solution Approach 2:
Different regions of the tablet have different hardness characteristics - the outer portions are harder to resist crushing while the inner portions can be more easily separated, enabling selective splitting for dose reduction without compromising overall abuse resistance
2Reliability
If controlled-release formulations are used to prevent bursts of drug bioavailability, then abuse resistance is improved, but ability to provide immediate drug release for therapeutic effect decreases
Solution Approach 1:
The controlled-release formulation is segmented into multiple unit doses that can be released sequentially or simultaneously depending on administration, allowing the formulation to provide both controlled-release characteristics for abuse resistance and immediate release capability when needed for therapeutic effect
Solution Approach 2:
The formulation dynamically adjusts its release characteristics based on administration conditions - maintaining controlled-release properties under normal conditions while enabling immediate release when the dosage form is manipulated or administered in specific ways, thus adapting to different user needs
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 effectively prevent abuse and overdose by maintaining therapeutic drug release while deterring non-medical use routes, such as nasal inhalation and injection, and reducing euphoric effects from excessive doses.
Implementation Method 1
an outer (or functional) coating layer containing a first cationic pH-dependent polymer
Implementation Method 2
a second population of multi-particulates containing a first viscosity-building polymer and a first alkaline buffering agent
Data Source
AI summary
Disclosed are solid oral pharmaceutical compositions that that are intended to provide protection against overdose and tampering, as well as abuse deterrence. The compositions contain a plurality of granules or multi-particulates. A first population of multi particulates contains an API or drug susceptible to abuse, a polymer matrix, and an outer coating that contains a cationic pH dependent polymer. These multi particulates also contain a plasticizer and a surfactant. A second population of multi particulates contains a viscosity building polymer and an alkaline buffering agent. Compositions may further include a disintegrant, and/or additional viscosity building polymers and/or alkaline buffering agents and/or ion exchange polymers. Also disclosed are the methods of making and using the compositions.