Stable Amphetamine Transdermal Matrix Without Reactive Moieties
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Solution Overview
Problem
Existing transdermal drug delivery compositions for amphetamine are prone to the formation of reaction products and degradation compounds, such as N-acetyl amphetamine, which reduces the efficacy and stability of the drug.
Innovation Solution
Formulating a polymer matrix for transdermal delivery of amphetamine that is free of vinyl acetate moieties, acetyl moieties, acyl halide moieties, carbonate ester moieties, carboxyl moieties, and ester moieties, using solvents like cyclohexane and incorporating antioxidants like butylated hydroxytoluene (BHT) to minimize reaction and degradation, and incorporating components like silicone dioxide and hydrogenated hydrocarbon resins.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional polymer matrices containing vinyl acetate moieties are used for transdermal amphetamine delivery, then the composition can be manufactured with common materials, but the amphetamine reacts to form N-acetyl amphetamine and other degradation products, reducing therapeutic effectiveness
Solution Approach 1:
The patent removes vinyl acetate moieties and other reactive functional groups (acetyl, acyl halide, carbonate ester, carboxyl, and ester moieties) from the polymer matrix composition. This extraction of harmful reactive components prevents amphetamine from reacting to form N-acetyl amphetamine and other degradation products, thereby maintaining therapeutic effectiveness while enabling long-term stability.
2Ease of manufacture
If reactive solvents and polymers are used to achieve desired delivery profile, then the composition can be formulated with available materials, but amphetamine degradation occurs during manufacturing and storage
Solution Approach 1:
The patent changes the chemical parameters of the polymer matrix by selecting materials free of reactive functional groups (vinyl acetate, acetyl, acyl halide, carbonate ester, carboxyl, and ester moieties). This parameter change in material composition allows the formulation to proceed with available non-reactive materials while preventing amphetamine degradation during manufacturing and storage.
3Reliability
If antioxidants with reactive moieties are added to prevent degradation, then oxidation protection is provided, but new reaction pathways are introduced that may affect amphetamine stability
Solution Approach 1:
The patent applies local quality by carefully selecting antioxidants that lack reactive moieties (acetyl, vinyl acetate, acyl halide, carbonate ester, carboxyl, and ester groups). This localized chemical property of the antioxidant ensures it provides oxidation protection without introducing new reaction pathways that could affect amphetamine stability.
Data Source
AI summary
Described are transdermal drug delivery compositions comprising amphetamine, methods of making transdermal drug delivery compositions comprising amphetamine, and therapeutic methods of using them. In specific embodiments, the compositions are free of components with moieties that are reactive with amphetamine. In specific embodiments, the compositions are manufactured using solvents free of components with moieties that are reactive with amphetamine. Therapeutic methods using the compositions also are described.