Abuse-Deterrent Opioid Formulation with pH-Modulating Coats
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current abuse-deterrent formulations for opioid analgesics are ineffective in preventing overdose from swallowing multiple intact pills or tablets, as they primarily focus on preventing crushing, snorting, or injection, and do not adequately address the common practice of ingesting multiple units to achieve euphoria, leading to serious adverse effects and deaths.
Innovation Solution
A unit dose formulation with a core containing an active substance, surrounded by an acid labile coat and an alkalinizing coat, which inhibits the release of the active substance when multiple units are ingested, using pH-modulating agents like magnesium hydroxide and citric acid to control gastric pH and delay or prevent the release of the active ingredient.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Strength
If abuse-deterrent formulations are designed to prevent crushing, snorting, or injection, then resistance to manipulation is improved, but effectiveness against swallowing multiple intact pills is worsened
Solution Approach 1:
The patent changes the chemical parameter (pH) of the gastric environment by incorporating pH-modulating agents that react to alter stomach acidity. When multiple pills are swallowed, the cumulative pH change triggers a response that prevents drug release, thereby addressing overdose protection without compromising the integrity of intact pill swallowing.
Solution Approach 2:
The patent introduces pH-modulating agents as intermediary substances that mediate between the swallowed pills and the drug release mechanism. These agents detect the pH changes resulting from multiple pill ingestion and trigger the prevention mechanism, serving as a bridge between the abuse behavior and the protective response.
2Reliability
If pH-modulating agents are used to control gastric pH, then release control is improved, but formulation complexity is worsened
Solution Approach 1:
The patent merges the pH-modulating agents with the drug substance or excipients into a single integrated formulation. Rather than adding separate complex delivery systems, the pH-responsive components are combined with the existing tablet structure, achieving release control while minimizing additional complexity.
Solution Approach 2:
The formulation uses the body's own gastric pH changes as the trigger mechanism, eliminating the need for external sensors, power sources, or complex control systems. The pH-modulating agents automatically respond to the chemical environment changes caused by multiple pill ingestion, providing self-regulating release control.
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 delays or prevents the release of the active substance when multiple units are ingested, reducing the risk of overdose and abuse by maintaining a pH threshold that inhibits dissolution and release, thereby minimizing the risk of adverse effects and deaths.
Implementation Method 1
using pH-modulating agents like magnesium hydroxide and citric acid to control gastric pH
Implementation Method 2
inhibits the release of the active substance when multiple units are ingested, using pH-modulating agents like magnesium hydroxide and citric acid to control gastric pH and delay or prevent the release of the active ingredient
Data Source
AI summary
Drug delivery formulations, uses thereof and methods of making same are provided in order to reduce the potential for abuse, misuse or improper administration of an addictive substance or any active substance and to prevent, reduce, inhibit, or delay purposeful or accidental overdose of an active substance by ingesting too many dosage forms at once, for example.