Sustained-Release Tablet Combating Injection Misuse
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Solution Overview
Problem
Current pharmaceutical compositions fail to prevent the extraction of active ingredients from liquid media, including aqueous and hydro-alcoholic solutions, making them susceptible to misuse via injection, and existing solutions do not address extraction in acidic or ethanol-based mediums effectively.
Innovation Solution
A sustained-release oral pharmaceutical composition comprising a mixture of polyvinyl acetate, polyvinylpyrrolidone, xanthan gum, and carbomer or gum arabic, which forms a gel in aqueous or hydro-alcoholic solutions, trapping the active ingredient and making it difficult to extract, with a crush resistance that deters misuse via injection, oral, and nasal routes.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If an excipient that gels in water is used to prevent parenteral misuse, then active ingredient extraction in aqueous media is limited, but extraction in acid or hydro-alcoholic media is not prevented
Solution Approach 1:
The patent uses a composite matrix comprising multiple excipients including gel-forming substances and pH-independent sustained-release polymers. This composite structure prevents active ingredient extraction in diverse liquid media (aqueous, acidic, and hydro-alcoholic) by combining the gel-forming property with pH-independent release characteristics, thereby resolving the limitation of single-excipient formulations that only work in specific media conditions.
Solution Approach 2:
The patent modifies the chemical and physical parameters of the matrix by selecting polymers with pH-independent sustained-release properties. This ensures that the matrix maintains its structural integrity and release control across varying pH conditions (acidic, neutral, basic) and solvent compositions (aqueous, hydro-alcoholic), preventing extraction in all tested media types.
2Reliability
If water-insoluble ultra-hard matrix tablets are used, then oral and nasal misuse is prevented, but injection misuse is still possible
Solution Approach 1:
The patent combines water-insoluble pH-independent sustained-release polymers with gel-forming excipients to create a composite matrix. This composite structure maintains the ultra-hard, water-insoluble properties that prevent oral and nasal misuse, while the gel-forming component ensures that the matrix dissolves or gels in injection volumes, preventing parenteral abuse by making the active ingredient unavailable for injection.
Solution Approach 2:
The gel-forming excipient acts as an intermediary that bridges the contradiction between maintaining structural hardness (to prevent oral/nasal misuse) and enabling gel formation in liquid media (to prevent injection misuse). When exposed to injection volumes, the gel-forming excipient creates a gel structure that traps the active ingredient, preventing its extraction and injection, while the overall matrix remains ultra-hard in its solid state.
3Ease of manufacture
If a single excipient formulation is used, then manufacturing is simple, but extraction can occur in specific liquid media (acidic or ethanol-based)
Solution Approach 1:
The patent employs a composite excipient system rather than a single excipient, combining gel-forming substances with pH-independent sustained-release polymers. This composite approach maintains relative manufacturing simplicity while providing comprehensive protection against extraction in diverse media including aqueous, acidic, and hydro-alcoholic solutions, thereby resolving the limitation of single-excipient formulations.
Solution Approach 2:
The patent designs the matrix with multi-functional excipients that perform multiple roles: gel formation to prevent parenteral misuse, pH-independent sustained-release to maintain structural integrity across pH ranges, and water-insolubility to prevent oral/nasal abuse. This universal design ensures effectiveness across all tested liquid media while keeping the formulation relatively simple.
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 effectively limits active ingredient extraction to less than 40% in hydro-alcoholic media and less than 25% in aqueous media, compared to Oxycontin, and its high crush resistance and gel formation in solutions prevent injection and nasal misuse, while maintaining pH-independent release.
Implementation Method 1
A sustained-release oral pharmaceutical composition comprising a mixture of polyvinyl acetate, polyvinylpyrrolidone, xanthan gum, and carbomer or gum arabic, which forms a gel in aqueous or hydro-alcoholic solutions, trapping the active ingredient
Data Source
AI summary
The invention relates to an oral pharmaceutical composition in the form of a sustained-release tablet comprising an active ingredient capable of being misused, which composition makes it possible to combat misuse by injection.