Segmented Opioid Dosage Form with Enteric Gelling Agent
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
There is a need for an immediate release solid oral dosage form of opioid analgesics that is resistant to tampering and abuse, particularly parenteral and nasal abuse, while maintaining its immediate release characteristics for proper administration.
Innovation Solution
The development of an immediate release solid oral dosage form comprising an opioid analgesic composition and a delayed release gelling agent composition, where the gelling agent is enteric-coated and designed to increase viscosity upon tampering, making the dosage form unsuitable for parenteral administration, and incorporating aversive agents to deter abuse.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If a gelling agent is incorporated into an immediate release dosage form to inhibit tampering, then abuse deterrence is improved, but extended release characteristics are introduced which compromise the immediate release nature of the active agent
Solution Approach 1:
The dosage form is segmented into two distinct functional components: an immediate release active agent composition and a delayed release gelling agent composition. This segmentation allows each component to perform its specific function independently - the active agent provides immediate therapeutic effect while the gelling agent remains dormant during proper administration but activates upon tampering to provide abuse deterrence through gel formation and viscosity increase.
Solution Approach 2:
The gelling agent is pre-positioned within the dosage form in a dormant state, prepared in advance to activate only upon tampering. The enteric coating is applied beforehand to protect the gelling agent from dissolving during normal gastrointestinal passage, ensuring it remains inactive during proper administration and only activates when the dosage form is crushed or tampered with, at which point the coating is compromised and the gelling agent releases to form a viscous gel.
2Reliability
If sufficient gelling agent is used to inhibit tampering through viscosity increase, then parenteral abuse is deterred, but the dosage form complexity and manufacturing difficulty increase
Solution Approach 1:
An enteric coating material serves as an intermediary between the gelling agent and the gastrointestinal environment. This coating layer protects the gelling agent from premature activation during normal oral administration, allowing the dosage form to pass through the stomach and intestines without triggering gel formation. Only when the dosage form is crushed or tampered with does the coating become compromised, allowing the gelling agent to release and activate, thus providing parenteral abuse deterrence without complicating the basic formulation structure.
3Reliability
If a gelling agent is added to the formulation, then abuse deterrence is improved, but the manufacturing process becomes more complex
Solution Approach 1:
The manufacturing process merges two relatively simple sub-processes: (1) preparation of immediate release active agent particles, and (2) coating of these particles with enteric material and incorporation of gelling agent. This merging approach allows the complex functionality to be achieved through sequential, straightforward operations rather than requiring sophisticated manufacturing equipment or multi-step processes, maintaining ease of manufacture while achieving the desired abuse deterrence through the combined functionality of the coated particles.
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 reduces the abuse potential of opioid analgesics by making them unsuitable for injection or nasal absorption when tampered with, while ensuring rapid drug release upon proper administration, thereby addressing the challenges of abuse deterrence and maintaining therapeutic efficacy.
Implementation Method 1
the crushed dosage form is mixed with a solution, a viscosity is obtained which inhibits the drug from being drawn into a needle
Implementation Method 2
a viscosity is obtained which inhibits the drug from being drawn into a needle, thereby hindering parenteral abuse
Implementation Method 3
when the crushed dosage form is applied to a mucosal surface (e.g., the nasal cavity), the composition forms a gel upon contact with mucosal moisture, thereby inhibiting absorption
Data Source
AI summary
Disclosed herein are immediate release solid oral dosage forms, their methods of preparation and use. The immediate release solid oral dosage form may comprise an active agent composition in an immediate release form, such as an opioid analgesic composition and a gelling agent composition in a delayed release form.