Memantine Premixture Coating for Dysphagia Suspension
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Solution Overview
Problem
Current pharmaceutical compositions of memantine for Alzheimer's disease often have a bitter taste and large particle sizes, making them difficult for patients with dysphagia to swallow, and existing solutions like grinding tablets or oral disintegrating tablets are either ineffective or uncomfortable for patients with neurological problems.
Innovation Solution
A pharmaceutical composition with a premixture that forms a suspension in the buccal cavity, characterized by small particle sizes (90% < 170 microns) and a pleasant taste, which can be administered as an oral suspension, powder, or quickly disintegrating tablets, ensuring easy swallowing and flexible dosing without uncomfortable aggregates.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If memantine is administered as traditional oral tablets, then the medication can be delivered in a stable solid form, but the large particle size and bitter taste make it difficult for patients with dysphagia to swallow
Solution Approach 1:
The patent divides the memantine medication into extremely fine particles through a specific granulation process, reducing particle size to less than 170 microns (with 50% under 60 microns). This segmentation transforms the original large tablet structure into microscopic particles that can be easily suspended in liquid and swallowed without difficulty, directly resolving the swallowing ease contradiction.
Solution Approach 2:
The patent changes the physical parameter of particle size from traditional tablet dimensions to sub-170 micron fine particles through controlled granulation. This parameter transformation enables the medication to transition from an unswallowable solid form to a swallowable suspension form, solving the contradiction between maintaining solid dosage stability and achieving easy swallowing.
2Ease of operation
If memantine tablets are ground to reduce particle size, then swallowing may be improved, but the bitter taste of memantine remains and aggregates form in the buccal cavity
Solution Approach 1:
The patent introduces a coating composition as an intermediary substance that envelops the memantine particles. This coating layer acts as a mediator between the bitter memantine and the patient's buccal cavity, preventing direct contact and taste perception while also preventing particle aggregation. The coating resolves both the bitter taste and aggregate formation problems simultaneously.
Solution Approach 2:
The patent applies a preliminary protective coating to the memantine particles before administration. This pre-action prevents the harmful effects (bitter taste and aggregation) from occurring in the first place by creating a barrier layer that interferes with the interaction between memantine and the buccal environment, eliminating the need for post-processing interventions.
3Ease of operation
If oral disintegrating tablets are used, then disintegration occurs in the buccal cavity, but the process takes 20-45 seconds which is uncomfortable for patients with neurological problems
Solution Approach 1:
The patent changes the disintegration time parameter from 20-45 seconds to less than 10 seconds through optimized granulation and coating techniques. This dramatic parameter reduction transforms the disintegration process from an uncomfortable prolonged event to an immediate, imperceptible transformation, resolving the contradiction between disintegration effectiveness and patient comfort.
Solution Approach 2:
The patent performs preliminary preparation of the particles through controlled granulation and coating processes that pre-structure the material for ultra-rapid disintegration. This preliminary action ensures that when the medication contacts the buccal cavity, the disintegration occurs instantaneously without requiring prolonged time, eliminating the discomfort associated with extended disintegration periods.
4Ease of manufacture
If memantine suspension is prepared by simple grinding and water addition, then administration is simplified, but large aggregates form that are uncomfortable in the buccal cavity
Solution Approach 1:
The patent performs preliminary granulation and coating of the memantine particles before suspension preparation. This pre-processing action creates uniformly coated fine particles that resist aggregation even when simple water addition is used for suspension preparation. The preliminary structuring maintains preparation simplicity while eliminating aggregate formation.
Solution Approach 2:
The coating composition serves as an intermediary substance that prevents direct interaction between memantine particles and water during suspension preparation. This intermediary layer maintains particle separation and prevents aggregate formation while allowing the suspension to be prepared through simple mixing, resolving the contradiction between preparation simplicity and aggregate prevention.
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 masks the bitter taste of memantine and facilitates easy swallowing by forming a suspension within seconds, suitable for patients with dysphagia, and can be administered through enteral feeding tubes without obstruction, providing a practical and comfortable treatment option.
Implementation Method 1
A pharmaceutical composition with a premixture that forms a suspension in the buccal cavity, characterized by small particle sizes (90% < 170 microns)
Data Source
AI summary
Pharmaceutical composition of memantine for administering orally which comprises a premixture comprising:i) between 74 and 85% w/w total of the premixture of a granulate of pellets comprising memantine between 10 and 15% w/w total of the premixture; coated by first coating of polyvinylpyrrolidone and a second coating comprising between 80 and 95% w/w total of the coating of cationic copolymer of dimethylaminoethyl methacrylate, butyl methacrylate and methyl methacrylate and between 5 and 20% w/w total of the coating of magnesium stearate;ii) between 4 and 7% w/w total of the premixture of sucralose;iii) between 11 and 19% w/w total of the premixture of essences.All the components have a particle size smaller than 710 microns. The composition can be a suspension, a powder for preparing a suspension or an oral disintegrating tablet. It can also be used to be administered through a nasogastric tube.