Controlled-Release Opioid Antagonist Composition for Urinary Retention

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Solution Overview

Problem

There is a lack of specific treatment options for opioid-induced urinary retention, particularly in oral dosage forms, which poses a challenge in managing this condition effectively.

Innovation Solution

A pharmaceutical composition comprising an opioid antagonist, such as naloxone, and an opioid agonist, such as oxycodone, in a controlled release formulation to treat urinary retention, including opioid-induced cases, providing both immediate and sustained release properties to address the condition effectively.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If intravenous opioid antagonists (methylnaltrexone, naloxone) are used to reverse opioid-induced bladder dysfunction, then urinary retention is treated, but the treatment is limited to intravenous administration and lacks oral dosage forms

Engineering Contradiction:
Improveadministration routeVSAvoiddosage form availability
Core Design Contradiction:
Ease of operationVSAdaptability or versatility

Solution Approach 1:

The invention changes the administration route parameter from intravenous to oral, and introduces controlled-release formulation parameters to extend duration of action. This allows the same therapeutic agent (opioid antagonist) to be delivered through different routes and formulations, making the treatment more versatile and easier to administer while maintaining therapeutic efficacy

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention segments the treatment approach by combining immediate-release and controlled-release formulations of opioid antagonists. This segmentation allows for both rapid onset (immediate-release) and sustained effect (controlled-release), providing flexibility in treating different stages and severities of opioid-induced urinary retention

Inventive Principle:
Principle #1Segmentation

2Object-affected harmful factors

If opioid agonists are administered for pain management, then pain is relieved, but urinary retention occurs as a side effect

Engineering Contradiction:
Improvepain reliefVSAvoidurinary retention
Core Design Contradiction:
Object-affected harmful factorsVSObject-generated harmful factors

Solution Approach 1:

The invention introduces an intermediary substance (opioid antagonist) that specifically counteracts the harmful effect (urinary retention) caused by the opioid agonist, while allowing the beneficial effect (pain relief) to continue. The antagonist acts as a mediator that selectively blocks the antagonist receptors responsible for urinary retention without completely blocking the agonist's pain-relieving effects

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention converts the harmful side effect (urinary retention caused by opioid agonists) into a treatable condition with a specific counter-agent. By developing controlled-release formulations of opioid antagonists, the harm is transformed into a manageable situation where the antagonist's blocking effect is sustained over time, preventing urinary retention while preserving pain relief

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

3Reliability

If frequent administration of opioid antagonists is performed, then urinary retention is effectively treated, but patient compliance decreases and treatment complexity increases

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidadministration frequency
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The invention implements controlled-release formulations that provide continuous release of the opioid antagonist over extended periods (12-48 hours or longer). This continuity of useful action maintains therapeutic levels of the antagonist in the body, effectively treating urinary retention without requiring frequent dosing, thereby improving patient compliance while maintaining treatment reliability

Inventive Principle:
Principle #20Continuity of useful action

Data Source

PatentEP2317991B1Use of opioid antagonists for treating urinary retention
Publication Date: 2017.05.03 EURO CELTIQUE SA

AI summary

The invention pertains to the use of opioid antagonists for the treatment of urinary retention.