Multilayered Oral Dosage Form with Superabsorbent Gel
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Solution Overview
Problem
Current controlled release formulations for pharmaceutical agents are vulnerable to misuse and accidental abuse, particularly when compromised, leading to potentially fatal consequences due to rapid release of the active ingredient.
Innovation Solution
A multilayered oral dosage form comprising controlled release microparticles and a superabsorbent material that maintains controlled release properties even when bisected or crushed, forming a hard gel to prevent immediate release and dose dumping.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If controlled release formulations incorporate larger amounts of pharmaceutically active agent to facilitate reduced dosing frequency, then convenience and adverse event profile are improved, but vulnerability to misuse and accidental abuse increases
Solution Approach 1:
The formulation is divided into multiple independent microparticles, each containing controlled release mechanisms. This segmentation ensures that even if the tablet is crushed or damaged, individual microparticles maintain their controlled release properties and cannot be rapidly extracted or administered in dangerous ways
Solution Approach 2:
A polymer matrix acts as an intermediary between the pharmaceutically active agent and the external environment. This matrix controls the release rate of the drug and prevents rapid extraction, making it difficult to abuse the formulation even when the tablet structure is compromised
2Ease of operation
If controlled release formulations are damaged by accidental chewing or grinding, then immediate release of pharmaceutically active agent occurs, but convenience is improved
Solution Approach 1:
The microparticles are pre-coated with controlled release polymers and encapsulated in a protective matrix before being incorporated into the tablet. This beforehand protection ensures that even if the tablet is crushed or chewed, the microparticles maintain their controlled release properties and cannot cause immediate drug release
Solution Approach 2:
The formulation converts the potential harm of physical damage into a benefit by designing microparticles that become even more effective at controlling drug release when the tablet is damaged. The polymer matrix and coating layers are specifically designed to maintain integrity and control release rates even under physical stress
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 formulation effectively prevents rapid release of the pharmaceutical agent, reducing the risk of misuse and accidental abuse by maintaining controlled release characteristics, even when exposed to aqueous environments or alcohol, and making extraction difficult through nasal administration or syringe injection.
Implementation Method 1
the superabsorbent material swells to form a hard gel that prevents immediate release of the pharmaceutical agent
Implementation Method 2
controlled release microparticles having at least one pharmaceutically active agent disposed therein
Implementation Method 3
maintains its controlled release properties for at least one pharmaceutically active agent even when bisected or crushed
Data Source
AI summary
Disclosed is a misuse preventative, controlled release composition in the form of a multilayered oral dosage form. A first layer contains a plurality of controlled release microparticles having a pharmaceutically active agent (for example, an opioid analgesic) disposed therein. A second layer comprises a superabsorbent material. When crushed, either intentionally or accidentally, and exposed to an aqueous medium, the superabsorbent material creates a hard gel that traps the microparticles. The hard gel and microparticles provide controlled release of the pharmaceutically active agent.