Subcutaneous Opioid Antagonist Pellets for Extended Release

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Solution Overview

Problem

Current opioid antagonists like naltrexone and PDE5 inhibitors face challenges in maintaining consistent drug levels and patient compliance due to their oral administration, leading to spikes in blood concentration and increased risk of relapse or adverse events, while existing implantable forms are large, painful, and visible, limiting their effectiveness and acceptance.

Innovation Solution

Development of subcutaneously implantable pellet formulations containing opioid antagonists or PDE5 inhibitors, which are smaller, less painful, and less visible, using a combination of pharmaceutically acceptable lubricants, vehicles, and ascorbic acid to ensure extended release over days to months, reducing the need for daily dosing and minimizing side effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If oral administration of naltrexone is used, then ease of administration is improved, but reliability deteriorates due to ineffective blood concentration levels and low retention in treatment

Engineering Contradiction:

Improveease of administrationVSAvoideffectiveness of treatment

Core Design Contradiction:

Ease of operationVSReliability

Solution Approach 1:

The patent replaces the oral mechanical administration system with a subcutaneous implant system. The implant is inserted under the skin and releases naltrexone continuously over time, eliminating the need for daily oral dosing while maintaining reliable therapeutic blood concentration levels.

Inventive Principle:

Principle #28Mechanics substitution (Replace mechanical system)

Solution Approach 2:

The patent introduces a subcutaneous implant as an intermediary delivery mechanism between the naltrexone and the bloodstream. The implant acts as a reservoir that slowly releases the drug into the tissue, ensuring consistent bioavailability without requiring patient compliance with daily oral intake.

Inventive Principle:

Principle #24Intermediary (Mediator)

2Reliability

If intramuscular injection of naltrexone is used, then reliability of treatment is improved, but ease of operation deteriorates due to large deposit size and pain

Engineering Contradiction:

Improveeffectiveness of treatmentVSAvoidpatient comfort

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The patent applies local quality by placing the implant in the subcutaneous tissue layer rather than the intramuscular layer. This location provides a smaller, less painful deposit that is less visible and less likely to cause discomfort, while still maintaining reliable drug release through the subcutaneous tissue and capillary network.

Inventive Principle:

Principle #3Local quality

3Reliability

If daily oral dosing is required, then reliability of maintaining therapeutic levels is improved, but loss of time increases due to need for daily patient compliance

Engineering Contradiction:

Improveconsistency of drug levelsVSAvoidtime for daily dosing

Core Design Contradiction:

ReliabilityVSLoss of time

Solution Approach 1:

The patent achieves continuity of useful action through the implant's sustained release mechanism. The naltrexone is released continuously from the implant over several months, maintaining stable therapeutic blood concentration levels without requiring intermittent daily dosing actions from the patient.

Inventive Principle:

Principle #20Continuity of useful action

Solution Approach 2:

The patent applies preliminary action by loading a large quantity of naltrexone into the implant during the initial insertion procedure. This pre-loaded reservoir then provides continuous drug release over time, eliminating the need for repeated dosing actions and freeing the patient from daily compliance requirements.

Inventive Principle:

Principle #10Preliminary action

4Reliability

If large diameter implants are used, then reliability of drug delivery is improved, but object-affected harmful factors worsen due to visibility and pain

Engineering Contradiction:

Improvedrug delivery effectivenessVSAvoidvisibility and pain

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by reducing the diameter of the implant from the conventional large size to a smaller subcutaneous dimension. This parameter reduction maintains adequate drug delivery effectiveness through optimized release kinetics while significantly reducing visibility, pain, and cosmetic concerns for the patient.

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 subcutaneously implantable pellet formulations provide a consistent and prolonged release of opioid antagonists or PDE5 inhibitors, improving patient compliance, reducing pain and visibility issues, and maintaining therapeutic levels, thereby enhancing treatment efficacy and reducing adverse events.

Implementation Method 1

pharmaceutical compositions suitable for use as extended, sustained and/or controlled release formulations

Methodology Applied

Scientific EffectControlled release:

Implementation Method 2

provide a consistent and prolonged release of opioid antagonists or PDE5 inhibitors

Methodology Applied

Scientific EffectDegradation: Decomposition (biological)

Data Source

PatentUS11185540B2Extended release compositions of opioid antagonists and phosphodiesterase 5 inhibitors

Publication Date: 2021.11.30 PARDON MY SCOTCH LLC

AI summary

Pharmaceutical compositions of one or more opioid antagonists or phosphodiesterase 5 (PDE5) inhibitors are disclosed.