Neramexane Titration Package for Tinnitus Dose Escalation

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Solution Overview

Problem

Current medical treatments for tinnitus lack effective and replicable reduction of tinnitus severity, with existing therapies often resulting in placebo effects and drug-related adverse events, necessitating a safer and more efficient dosing regimen.

Innovation Solution

A titration scheme for neramexane, involving gradual up-titration of dosages from 12.5 mg to 75 mg over four to five weeks, minimizing side effects and utilizing a titration package with distinct dosages and administration schedules to achieve an effective dose for treating inner ear disorders like tinnitus.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If a high dosage of neramexane is administered to achieve effective treatment of tinnitus, then therapeutic efficacy is improved, but drug-related adverse events increase

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidadverse events
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies preliminary action by implementing a titration scheme that gradually increases the dosage of neramexane over several weeks before reaching the maintenance dosage. This gradual up-titration allows the patient's body to adapt to the drug, minimizing adverse events while eventually achieving the therapeutic efficacy associated with higher dosages. The package provides dosages ranging from 6.25 mg to 62.5 mg to facilitate this progressive approach.

Inventive Principle:
Principle #10Preliminary action

2Object-affected harmful factors

If a gradual titration scheme is implemented to minimize side effects, then adverse events are reduced, but treatment duration is extended

Engineering Contradiction:
Improveside effectsVSAvoidtreatment duration
Core Design Contradiction:
Object-affected harmful factorsVSLoss of time

Solution Approach 1:

The patent applies dynamics by providing a flexible titration scheme where the dosage can be adjusted based on individual patient response. The package includes multiple dosages (6.25 mg, 12.5 mg, 25 mg, 37.5 mg, 50 mg, 62.5 mg) that allow clinicians to optimize the balance between minimizing side effects and achieving therapeutic effect within a reasonable time frame. This dynamic adjustment capability enables adaptation to each patient's unique response pattern.

Inventive Principle:
Principle #15Dynamics

3Ease of operation

If multiple dosages are provided in a titration package to enable flexible dosing, then patient compliance is improved, but package complexity increases

Engineering Contradiction:
Improvepatient complianceVSAvoidpackage structure
Core Design Contradiction:
Ease of operationVSDevice complexity

Solution Approach 1:

The patent applies segmentation by dividing the treatment regimen into distinct dosage levels (6.25 mg, 12.5 mg, 25 mg, 37.5 mg, 50 mg, 62.5 mg), each contained in separate blister cards or packaging sections. This segmentation allows for clear organization and easy identification of different dosages, simplifying the titration process for patients while providing the flexibility needed for individualized dosing. Each segment corresponds to a specific week or phase of treatment.

Inventive Principle:
Principle #1Segmentation

Data Source

PatentEP2203163B1Titration package for neramexane and its use in the treatment of an inner ear disorder
Publication Date: 2014.08.27 MERZ PHARMA GMBH & CO KGAA
  • EP2203163B1 patent drawingFigure 1
  • EP2203163B1 patent drawingFigure 2
  • EP2203163B1 patent drawingFigure 3~4

AI summary

The present invention relates to a titration scheme for the administration of a 1-amino-alkylcyclohexane derivative which allows for quick attainment of an effective dose of a 1-amino-alkylcyclohexane derivative while minimizing side effects. The present invention further relates to a titration package for providing a 1-amino-alkylcyclohexane derivative (e.g., neramexane or a pharmaceutically acceptable salt thereof) in at least two different dosages. The present titration scheme/titration package may be useful in the treatment of various diseases, including tinnitus.