Intravesical Oxybutynin Composition for Bladder Dysfunction

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current treatments for neurogenic bladder dysfunction, particularly those involving detrusor hyperactivity and detrusor-sphincter dyssynergia, face challenges in optimizing drug dosage and delivery, leading to suboptimal therapeutic outcomes due to systemic side effects and inadequate adjustment of drug amounts at the bladder site.

Innovation Solution

An oxybutynin-containing composition is developed for topical administration via instillation into the urinary bladder, with a treatment dose determined by objective urodynamic parameters such as detrusor pressure, detrusor coefficient, and intravesical pressure, ensuring optimal bladder function improvement and reduced side effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If oxybutynin is administered systemically for neurogenic bladder dysfunction, then detrusor overactivity is suppressed, but systemic side effects occur and drug dosage optimization is difficult

Engineering Contradiction:
Improvetherapeutic effectivenessVSAvoidsystemic side effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by delivering oxybutynin directly to the bladder through intravesical instillation, creating a high local concentration at the target site while maintaining low systemic levels. This resolves the contradiction by concentrating the therapeutic effect locally in the bladder to suppress detrusor overactivity, while minimizing systemic absorption that causes side effects like dry mouth, constipation, and cognitive impairment.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent uses an intermediary approach by formulating oxybutynin in a specific composition with controlled release properties and optimal pH for intravesical administration. This intermediary formulation ensures sustained local delivery to the bladder wall, maintaining effective concentrations at the target site while preventing excessive systemic absorption, thus resolving the contradiction between therapeutic effectiveness and systemic side effects.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Reliability

If high dose oxybutynin is administered to ensure therapeutic effect, then detrusor overactivity is controlled, but side effects increase

Engineering Contradiction:
Improvedetrusor overactivity controlVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent implements local quality by achieving high local concentration of oxybutynin directly at the bladder site through intravesical instillation, rather than relying on high systemic doses. This allows effective control of detrusor overactivity through localized action, while the low systemic circulation levels prevent the occurrence of side effects that would result from high systemic dosing.

Inventive Principle:
Principle #3Local quality

3Manufacturing precision

If oxybutynin composition is optimized for local delivery, then therapeutic outcome improves, but dosage determination becomes more complex

Engineering Contradiction:
Improvedrug dosage optimizationVSAvoiddosage determination process
Core Design Contradiction:
Manufacturing precisionVSDevice complexity

Solution Approach 1:

The patent applies parameter changes by optimizing the oxybutynin composition for intravesical delivery with specific pH ranges (4.5-6.5), controlled release characteristics, and standardized concentration formulations. These parameter optimizations improve therapeutic outcomes through enhanced local delivery and stability, while the standardized formulations actually simplify dosage determination by providing pre-optimized, ready-to-use compositions with predictable local effects.

Inventive Principle:
Principle #35Parameter changes

4Object-affected harmful factors

If topical administration is used to reduce systemic side effects, then side effects are minimized, but drug delivery optimization becomes challenging

Engineering Contradiction:
Improvesystemic side effectsVSAvoiddrug delivery optimization
Core Design Contradiction:
Object-affected harmful factorsVSEase of manufacture

Solution Approach 1:

The patent uses an intermediary formulation approach by developing a specifically designed oxybutynin composition for intravesical administration, incorporating optimal pH buffers, viscosity modifiers, and release-controlling excipients. This intermediary formulation resolves the contradiction by enabling effective local drug delivery to the bladder wall while minimizing systemic absorption, thus achieving both reduced side effects and optimized drug delivery through careful compositional design.

Inventive Principle:
Principle #24Intermediary (Mediator)

Data Source

PatentEP3909570A1Oxybutynin for intravesical application
Publication Date: 2021.11.17 FARCO PHARMA GMBH
  • EP3909570A1 patent drawingFigure 1A~1C
  • EP3909570A1 patent drawingFigure 2A~2C
  • EP3909570A1 patent drawingFigure 3A~3C

AI summary

The present invention relates to an oxybutynin-containing composition for use in the prophylactic or therapeutic treatment of, in particular, neurogenic bladder dysfunction and its uses, a storage or application device for this purpose, a packaging unit and a kit, which is designed in particular as an instillation system.