Tamper-Resistant Dosage Form Using Adsorbent Segmentation
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Solution Overview
Problem
There is a need for improved tamper-resistant dosage forms and techniques for their preparation, as existing methods do not effectively prevent or discourage tampering, abuse, misuse, or diversion of opioid-containing pharmaceuticals.
Innovation Solution
Pharmaceutical compositions and dosage forms comprising an adsorbent and an adverse agent, such as an opioid antagonist, are developed, where the adverse agent is adsorbed onto the adsorbent to prevent release unless the dosage form is tampered with, allowing for controlled release of the active agent while deterring misuse by inducing unpleasant effects if tampered with.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If an opioid agonist is combined with an opioid antagonist in a dosage form, then tamper resistance is improved, but the complexity of the dosage form increases
Solution Approach 1:
The dosage form is divided into separate compartments or layers: one containing the opioid agonist and another containing the opioid antagonist adsorbed on an adsorbent material. This segmentation allows each component to be isolated and controlled independently, reducing unnecessary complexity while maintaining tamper resistance through the physical separation mechanism
Solution Approach 2:
An adsorbent material (such as activated charcoal or silica gel) is introduced as an intermediary substance to hold the opioid antagonist. This intermediary enables the antagonist to be released only under specific conditions (when the dosage form is tampered with), simplifying the overall design by using a passive release mechanism rather than complex active control systems
2Reliability
If an adsorbent is used to hold the adverse agent, then controlled release is improved, but the manufacturing precision requirements increase
Solution Approach 1:
The adsorption characteristics are controlled by selecting adsorbent materials with specific properties (surface area, pore size, chemical composition) and by adjusting adsorption parameters such as temperature, pH, and contact time during manufacturing. This allows for consistent and predictable release behavior without requiring extremely tight manufacturing tolerances
Solution Approach 2:
Composite materials are used where the adsorbent is combined with other excipients or matrix materials to create a formulation that provides both the desired adsorption characteristics and ease of manufacturing. The composite structure allows for more forgiving manufacturing processes while maintaining controlled release performance
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 dosage forms effectively prevent the adverse agent from being released in vivo when administered intact, while ensuring its release if the dosage form is tampered with, thereby reducing abuse and misuse by inducing undesirable effects, and providing controlled release of the active agent.
Implementation Method 1
Pharmaceutical compositions and dosage forms comprising an adsorbent and an adverse agent, such as an opioid antagonist, are developed, where the adverse agent is adsorbed onto the adsorbent to prevent release unless the dosage form is tampered with
Data Source
AI summary
Pharmaceutical compositions and dosage forms comprising an adsorbent, and an adverse agent, such as an opioid antagonist. In one embodiment, at least a portion of the adverse agent is on the surface or within the micropore structure of an adsorbent material. The pharmaceutical compositions and dosage forms comprising the adsorbent and the adverse agent are useful for preventing or discouraging tampering, abuse, misuse or diversion of a dosage form containing an active pharmaceutical agent, such as an opioid. The present invention also relates to methods for treating a patient with such a dosage form, as well as kits containing such a dosage form with instructions for using the dosage form to treat a patient. The present invention further relates to process for preparing such pharmaceutical compositions and dosage forms.