Multilayer Orally Disintegrating Tablet with Oxycodone Coating
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Solution Overview
Problem
Formulating orally disintegrating tablets that include both oxycodone and acetaminophen is challenging due to acetaminophen's ability to promote the degradation of oxycodone, especially in moist conditions, and the difficulty in preventing premature release or bitter taste.
Innovation Solution
A multilayer orally disintegrating tablet design with separate layers for acetaminophen and oxycodone, where oxycodone is coated with a binder and a subcoat soluble in gastric fluids, and then coated with a taste-masking polymer, including a pore-forming agent to prevent degradation and ensure stable, non-bitter delivery.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Adaptability or versatility
If acetaminophen and oxycodone are formulated in the same orally disintegrating tablet, then the patient compliance and convenience are improved, but the stability of oxycodone deteriorates due to degradation promoted by acetaminophen
Solution Approach 1:
The tablet is divided into multiple layers with acetaminophen and oxycodone separated in different layers. This physical segmentation prevents direct contact between the two active ingredients, eliminating the degradation reaction while maintaining the convenience of combined administration.
Solution Approach 2:
A polymer coating is applied to the oxycodone-containing layer to act as a barrier between acetaminophen and oxycodone. This intermediary layer prevents direct interaction while allowing both ingredients to be present in the same dosage form.
2Object-affected harmful factors
If oxycodone is coated with a taste-masking polymer, then the bitter taste is prevented, but the stability of oxycodone deteriorates due to degradation over time
Solution Approach 1:
The coating system is segmented into multiple functional layers: an inner protective layer that maintains stability and an outer taste-masking layer that provides palatability. This segmentation allows both taste masking and stability to be achieved simultaneously.
Solution Approach 2:
A composite coating system is used combining different polymer materials with complementary properties. The inner layer uses a stability-preserving polymer while the outer layer uses a taste-masking polymer, creating a composite structure that provides both functions.
3Speed
If oxycodone is released quickly in the mouth, then the disintegration speed is improved, but the premature release and bitter taste worsen
Solution Approach 1:
The tablet structure is segmented into rapidly disintegrating outer layers and a protected inner layer containing oxycodone. This allows the tablet to disintegrate quickly for ease of swallowing while the coated oxycodone layer prevents premature release.
Solution Approach 2:
A thin polymer coating is applied to the oxycodone-containing granules or layer. This flexible film is permeable enough to allow rapid disintegration of the tablet structure but provides sufficient barrier to prevent premature release of oxycodone in the mouth.
Data Source
AI summary
This invention pertains to an orally disintegrating multilayer tablet characterized in that it comprises at least two discrete layers, one of which comprises at least one active agent that promotes the oxidation of opioids, preferably acetaminophen, and the other of which contains granules including an inert core which is coated with at least one opioid and at least one binder, wherein said opioid coating is coated with a subcoat comprising a compound soluble in gastric fluids, said subcoat being coated with a taste-masking coating comprising a polymer or copolymer comprising dialkylaminoalkyl (meth) acrylate units and optionally a pore-forming agent.