Neramexane Titration Package for Faster Dosing With Fewer Side Effects

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Solution Overview

Problem

Current medical treatments for tinnitus lack replicable reduction of tinnitus severity and are associated with significant side effects, and there is a need for a titration scheme that allows for quick and safe attainment of effective doses of 1-amino-alkylcyclohexane derivatives like neramexane while minimizing adverse events.

Innovation Solution

A titration scheme and package for administering neramexane or its pharmaceutically acceptable salts, which involves gradual up-titration over four to five weeks to achieve effective doses of 5 to 150 mg per day, minimizing side effects by adjusting dosages in 12.5 mg or 25 mg steps, and providing a titration package with multiple dosages to ensure compliance and safety.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If a high effective dose of neramexane is administered quickly, then the therapeutic effect for tinnitus is achieved faster, but side effects increase significantly

Engineering Contradiction:
Improvespeed of achieving effective doseVSAvoidside effects
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent applies preliminary action by implementing a pre-planned titration schedule that gradually increases the dose of neramexane over 4-5 weeks before reaching the effective maintenance dose. This preliminary dose escalation phase allows the patient's body to adapt to the medication, minimizing side effects while ensuring eventual achievement of the therapeutic effective dose for tinnitus treatment.

Inventive Principle:
Principle #10Preliminary action

2Reliability

If a gradual titration scheme is implemented to minimize side effects, then patient safety and compliance improve, but the time to reach effective dose increases

Engineering Contradiction:
Improvepatient safety and complianceVSAvoidtime to reach effective dose
Core Design Contradiction:
ReliabilityVSLoss of time

Solution Approach 1:

The patent applies dynamics by implementing a flexible titration scheme that can be adjusted based on individual patient response and tolerance. The dose escalation is dynamic, allowing acceleration or deceleration of the titration process while maintaining patient safety and compliance, thereby optimizing the balance between treatment speed and patient well-being.

Inventive Principle:
Principle #15Dynamics

3Ease of operation

If a fixed single dosage is provided, then the package is simple and easy to use, but it cannot accommodate individualized treatment requirements for different patients

Engineering Contradiction:
Improvesimplicity of package designVSAvoidindividualized dosage flexibility
Core Design Contradiction:
Ease of operationVSAdaptability or versatility

Solution Approach 1:

The patent applies segmentation by dividing the medication package into multiple segments with different dosages (e.g., 6.25 mg, 12.5 mg, 25 mg, 50 mg tablets). This segmented approach allows patients to start at a low dose and progressively increase to their individualized effective dose, providing both ease of use through structured packaging and adaptability for personalized treatment requirements.

Inventive Principle:
Principle #1Segmentation

Data Source

PatentEP2548552B1Titration package for 1-amino-alkylcyclohexanes
Publication Date: 2015.11.18 MERZ PHARMA GMBH & CO KGAA
  • EP2548552B1 patent drawingFigure 1
  • EP2548552B1 patent drawingFigure 2
  • EP2548552B1 patent drawingFigure 3~4

AI summary

The present invention relates to a titration scheme for the administration ofa 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.