Acamprosate Sprinkle Pellets for Gastrointestinal Tolerance
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Solution Overview
Problem
Current oral formulations of acamprosate, such as enteric-coated tablets, often cause gastrointestinal issues due to their size and composition, leading to poor bioavailability and tolerability, particularly in patients with difficulty swallowing or digestive disorders like Fragile X Syndrome, where significant adverse events like nausea, vomiting, and diarrhea are common.
Innovation Solution
Development of an orally-administrable pharmaceutical formulation comprising acamprosate calcium in the form of sprinkles with a core, sustained release coating, and enteric coating, designed to minimize gastric irritation and optimize drug release, allowing for a smoother absorption and reduced gastrointestinal distress.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Object-affected harmful factors
If enteric-coated tablets are used for acamprosate administration, then gastrointestinal protection is achieved, but tablet size and composition cause swallowing difficulties and gastrointestinal issues
Solution Approach 1:
The patent divides the single tablet formulation into multiple smaller sprinkle pellets containing acamprosate. These segmented pellets can be easily sprinkled onto food, eliminating swallowing difficulties while maintaining enteric-coating protection for each individual pellet to prevent gastrointestinal irritation.
Solution Approach 2:
The invention applies enteric-coating specifically to the surface of each sprinkle pellet, creating a localized protective layer that prevents gastrointestinal irritation only where needed (in the digestive tract) while allowing the core pellet material to remain small and easily administrable.
2Quantity of substance
If larger tablet formulations are used to achieve therapeutic dosage, then drug efficacy is improved, but gastrointestinal adverse events increase
Solution Approach 1:
The total therapeutic dosage of acamprosate is divided into multiple smaller pellets, each containing a fraction of the total dose. This segmentation allows the same quantity of drug to be administered in a form that reduces gastrointestinal adverse events, as each small pellet is better tolerated than a single large tablet.
Solution Approach 2:
The formulation combines acamprosate with excipients and applies enteric-coating material to create composite sprinkle pellets. This composite structure maintains the required drug dosage while the enteric-coating component specifically addresses gastrointestinal tolerance issues.
3Ease of manufacture
If conventional tablet formulations are used, then manufacturing simplicity is maintained, but bioavailability is reduced due to poor tolerability
Solution Approach 1:
The invention changes the physical parameters of the formulation from a single large tablet to multiple small pellets with specific size distributions. It also changes the coating parameters by applying enteric-coating to each pellet. These parameter changes improve bioavailability through better tolerability and absorption while maintaining manufacturing feasibility through established pelletization and coating techniques.
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 sprinkles formulation achieves controlled and sustained release of acamprosate, enhancing bioavailability and tolerability, reducing gastrointestinal adverse events, and providing a more patient-friendly administration option for patients with swallowing difficulties.
Implementation Method 1
sprinkles comprise a core, a sustained release coating, and an enteric coating
Implementation Method 2
designed to minimize gastric irritation and optimize drug release
Data Source
AI summary
The present invention provides an orally-administrable, pharmaceutical formulation comprising: a plurality of pellets, wherein: the pellets comprise a core, a sustained release coating, and an enteric coating; and the core comprises an active ingredient and a diluent.