Tamper-Resistant Tablet with Matrix and Particulates
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Solution Overview
Problem
Current tamper-resistant pharmaceutical dosage forms fail to provide rapid release of pharmacologically active compounds while maintaining adequate tamper-resistance, and they often have drawbacks such as difficulty in manufacturing, patient compliance, and risk of bovine spongiform encephalopathy due to gelatin content.
Innovation Solution
A tamper-resistant tablet comprising a matrix material making up at least 40 wt.% of the total weight and particulates making up at most 60 wt.%, where the particulates contain a pharmacologically active compound and a polyalkylene oxide with a molecular weight over 20,000 g/mol, providing immediate in vitro release and enhanced mechanical properties.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Strength
If tamper-resistant dosage forms with increased breaking strength are used, then resistance to crushing is improved, but rapid release of the active substance cannot be achieved
Solution Approach 1:
The dosage form is divided into multiple individual particles or pellets embedded in a matrix material. Each particle contains the active substance and is designed to disintegrate rapidly upon contact with gastric fluid, while the collective structure provides tamper resistance. This segmentation allows rapid drug release from individual particles while maintaining overall structural integrity against crushing.
Solution Approach 2:
The dosage form uses a composite structure combining a matrix material (such as gelatin, gelatinoid, or starch-based material) with embedded particles containing the active substance. The matrix provides mechanical strength and tamper resistance, while the embedded particles are designed to disintegrate rapidly in gastric fluid, enabling fast drug release without compromising structural integrity.
2Ease of manufacture
If gelatin is used in the dosage form, then manufacturing ease is improved, but risk of bovine spongiform encephalopathy increases
Solution Approach 1:
The patent replaces permanent gelatin with alternative materials that can be safely disposed of after serving their function. The matrix material is designed to dissolve completely in gastric fluid, leaving no persistent risk. This substitution eliminates the TSE risk associated with gelatin while maintaining the desired manufacturing properties and rapid disintegration characteristics.
Solution Approach 2:
The invention changes the material parameter from gelatin to alternative matrix materials such as gelatinoid materials or starch-based materials. These alternatives maintain the necessary functional properties (solubility, disintegration rate, manufacturing ease) while eliminating the harmful TSE risk associated with gelatin, thus modifying the material composition without sacrificing performance.
3Reliability
If controlled release is implemented, then abuse prevention is improved, but rapid therapeutic effect cannot be achieved
Solution Approach 1:
The dosage form exhibits dynamic behavior: it maintains structural integrity and resists tampering in the dry state, but undergoes rapid transformation when contacted with gastric fluid. The matrix material quickly dissolves or disintegrates in the aqueous environment, enabling immediate drug release for rapid therapeutic effect, while the dry structure provides abuse prevention through tamper resistance.
Solution Approach 2:
The dosage form exploits phase transition behavior of the matrix material. In the dry state, the matrix maintains structural integrity providing tamper resistance. Upon contact with gastric fluid, the matrix undergoes rapid dissolution or disintegration, transitioning from a solid structured state to a dissolved state, thereby enabling rapid drug release without requiring controlled release mechanisms.
Data Source
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AI summary
The invention relates to a tamper-resistant tablet comprising a matrix material in an amount of more than one third of the total weight of the tablet; and a plurality of particulates in an amount of less than two thirds of the total weight of the tablet; wherein said particulates comprise a pharmacologically active compound and a polyalkylene oxide; and form a discontinuous phase within the matrix material.