Amphetamine Extended Release Chewable Tablet
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Solution Overview
Problem
There is a need for a quick-acting, stable, extended release amphetamine product that can be conveniently delivered, especially for patients who have difficulty swallowing whole tablets and capsules.
Innovation Solution
The development of amphetamine extended release compositions that provide both immediate and extended release therapeutic effects, with a formulation that includes a higher percentage of immediate release components compared to extended release components, and are designed as chewable tablets that can also be orally disintegrating, dissolvable, or dispersible.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If extended release amphetamine products are designed to provide long-lasting therapeutic effects, then the duration of action is improved, but rebound effects and plasma concentration fluctuations worsen
Solution Approach 1:
The tablet is segmented into multiple functional components: immediate release amphetamine salts for rapid onset, extended release amphetamine salts for sustained effect, and an orally disintegrating matrix for controlled dissolution. This segmentation allows each component to contribute differently to the overall release profile, achieving both long duration and stable plasma concentrations.
Solution Approach 2:
The invention changes the physical and chemical parameters of the amphetamine delivery system by using different salt forms (immediate release vs. extended release salts), different particle sizes, and different matrix materials. These parameter changes enable tailored release kinetics that maintain stable plasma concentrations over an extended period.
2Duration of action of moving object
If amphetamine tablets are designed as whole tablets for extended release, then the duration of action is improved, but ease of operation worsens for patients with swallowing difficulties
Solution Approach 1:
The tablet exhibits local quality differences through its orally disintegrating matrix design, which allows different portions of the tablet to serve different functions. The matrix is designed to disintegrate rapidly in the oral cavity, releasing fine particles that can be swallowed easily or held in the mouth, providing flexibility for patients with swallowing difficulties while maintaining extended release properties.
Solution Approach 2:
The tablet transitions from a solid whole form to a disintegrated particulate form dynamically upon contact with oral fluids. This dynamic transformation allows the tablet to adapt to patient needs - patients can swallow the disintegrated particles easily or retain them in the mouth for buccal absorption, maintaining ease of operation while preserving the extended release mechanism.
3Speed
If immediate release components are increased in the formulation, then the onset of therapeutic effect is improved, but the duration of extended release effect worsens
Solution Approach 1:
The formulation employs periodic action through sequential release phases: immediate release components provide rapid initial therapeutic effect, followed by extended release components that maintain therapy over time. The orally disintegrating matrix facilitates this periodic release by controlling the dissolution and release kinetics of different amphetamine salt components at different time points.
Solution Approach 2:
The tablet uses composite materials combining immediate release amphetamine salts, extended release amphetamine salts, and an orally disintegrating matrix material. This composite structure allows simultaneous presence of fast-acting and slow-acting components, where the matrix holds both types of salts and releases them in a controlled sequence, achieving both rapid onset and prolonged duration.
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 compositions achieve a therapeutic effect lasting about 13 hours, with a single plasma concentration peak for both d-amphetamine and l-amphetamine, and are suitable for patients with swallowing difficulties, including pediatric and geriatric patients.
Implementation Method 1
amphetamine-cation exchange resin complex
Implementation Method 2
water-permeable, non-ionic modified release barrier coating
Data Source
AI summary
An oral amphetamine extended release solid dose is described. The compositions contain a combination of an uncoated amphetamine-cation exchange resin complex, a barrier coated amphetamine-cation exchange resin complex-matrix, and an uncomplexed amphetamine, wherein one or more of these components contains blends of different forms of amphetamines. Either the modified release coated and/or the uncoated amphetamine-cation exchange resin complex may have two forms of amphetamine in a complex with a single cation exchange resin. Following administration of a single dose of the composition, a therapeutically effective amount of amphetamine is reached by about one hour and the composition provides at least a thirteen hour effect post-dose.