Matrix Tablet Reducing Opioid Blood Fluctuations

Resolve Bottlenecks,
Find Innovative SolutionsGenerate Solutions

Solution Overview

Problem

Current opioid formulations experience significant fluctuations in plasma concentrations, leading to peak and trough effects that result in inadequate pain control and increased adverse side effects, as they require frequent administration and high doses to maintain therapeutic levels.

Innovation Solution

Development of a matrix-type tablet with a sustained-release mechanism using pH-independent, water-insoluble polymers and mineral excipients, which maintains steady-state opioid plasma concentrations for extended periods with reduced fluctuations, allowing for twice-a-day administration with minimal peak and trough variations.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If opioids are administered orally at sufficient frequency and high doses to maintain therapeutic levels, then pain control efficiency is improved, but plasma concentration fluctuations increase and adverse side effects worsen

Engineering Contradiction:

Improvepain control efficiencyVSAvoidadverse side effects

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent employs a dynamic matrix system composed of water-insoluble polymers and mineral excipients that continuously adjusts opioid release rates based on dissolution conditions, maintaining stable plasma concentrations without requiring frequent high-dose administration, thereby reducing adverse side effects while preserving pain control efficiency

Inventive Principle:

Principle #15Dynamics

Solution Approach 2:

The invention changes the physical and chemical parameters of the formulation by using specific water-insoluble polymers and mineral excipients with controlled surface areas and pore structures, transforming the release profile from fluctuating peaks and troughs to a sustained steady-state concentration that minimizes side effects while maintaining therapeutic efficacy

Inventive Principle:

Principle #35Parameter changes

2Speed

If opioids are released quickly to achieve rapid pain relief, then onset of action is improved, but plasma concentration fluctuations increase and duration of action decreases

Engineering Contradiction:

Improveonset of actionVSAvoidduration of sustained release

Core Design Contradiction:

SpeedVSDuration of action of moving object

Solution Approach 1:

The patent incorporates preliminary action by pre-forming a matrix structure with controlled porosity and surface area using water-insoluble polymers and mineral excipients, which is designed to dissolve at a controlled rate upon contact with gastrointestinal fluids, providing both rapid initial release for quick onset and sustained release for extended duration without significant concentration fluctuations

Inventive Principle:

Principle #10Preliminary action

3Reliability

If opioid formulations use frequent administration to maintain therapeutic levels, then pain control is improved, but patient compliance and convenience worsen

Engineering Contradiction:

Improvetherapeutic level maintenanceVSAvoidadministration frequency

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The patent achieves continuous useful action through a matrix formulation that provides sustained opioid release over extended periods (12-24 hours or longer), maintaining therapeutic levels without requiring frequent administration, thereby improving patient compliance and convenience while ensuring reliable pain control through continuous therapeutic coverage

Inventive Principle:

Principle #20Continuity of useful action

4Reliability

If high doses of opioids are administered to ensure sufficient analgesia, then pain relief efficacy is improved, but plasma concentration peaks increase and adverse effects worsen

Engineering Contradiction:

Improveanalgesia efficacyVSAvoidplasma concentration stability

Core Design Contradiction:

ReliabilityVSStability of the object's composition

Solution Approach 1:

The invention changes formulation parameters by using water-insoluble polymers and mineral excipients with specific surface area and pore structure characteristics, transforming the release profile to maintain stable plasma concentrations at therapeutic levels without excessive peaks, thereby ensuring adequate analgesia efficacy while minimizing concentration stability issues and associated adverse effects

Inventive Principle:

Principle #35Parameter changes

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 matrix-type tablet achieves a steady-state plasma concentration above 60% of the peak value for at least 10 hours, reducing fluctuations and side effects like nausea and drowsiness, while maintaining efficient pain control and minimizing breakthrough pain.

Implementation Method 1

the compression matrix of said matrix-type tablet consisting of at least one excipient chosen from the group comprising sustained-release, pH-independent and water-insoluble polymers, mineral excipients and their mixtures

Methodology Applied

Scientific EffectDissolution:

Implementation Method 2

matrix-type tablet for the sustained release of at least one opioid

Methodology Applied

Scientific EffectSustained release:

Data Source

PatentUS10111869B2Reduction of opioid blood fluctuations

Publication Date: 2018.10.30 ETHYPHARM SA

AI summary

The present invention relates to the use of a sustained release matrix containing at least one opioid for producing a solid oral formulation in table form suitable for reducing blood concentration fluctuations of said opioid.