Mazindol ADHD Treatment Plasma Half-Life

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Solution Overview

Problem

Current treatments for ADHD, particularly psychostimulants, have limitations such as short plasma half-lives leading to withdrawal effects, toxic risks, and inadequate management of symptoms like insomnia and inattention, and are not suitable for children due to administration challenges.

Innovation Solution

Mazindol, a non-amphetamine compound with a long plasma half-life and low toxic potential, is used as a monotherapy or in combination with psychostimulants, offering improved symptom management without withdrawal effects and toxic risks, and is administered once daily, suitable for children.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If psychostimulants (methylphenidate, amphetamines) are used to treat ADHD, then motor hyperactivity improvement is significant, but plasma half-life is short causing withdrawal effects and symptom rebound

Engineering Contradiction:
Improvesymptom control reliabilityVSAvoidplasma half-life
Core Design Contradiction:
ReliabilityVSDuration of action of moving object

Solution Approach 1:

The patent changes the pharmacokinetic parameter of plasma half-life by selecting mazindol (with half-life >24 hours) instead of conventional psychostimulants (with short half-lives). This parameter change eliminates the withdrawal effect and symptom rebound while maintaining reliable symptom control throughout the day.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If psychostimulants are used to treat ADHD, then arousing effect is achieved, but toxic risk increases

Engineering Contradiction:
Improvetreatment efficacyVSAvoidtoxic risk
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the safety parameter by selecting mazindol, which has demonstrated low toxic potential in clinical studies, replacing conventional psychostimulants that carry higher toxic risks including cardiovascular effects and potential for misuse.

Inventive Principle:
Principle #35Parameter changes

3Reliability

If conventional medicinal products are administered to children with ADHD, then treatment is provided, but administration difficulties arise due to tablet size and multi-day regimens

Engineering Contradiction:
Improvetreatment coverageVSAvoidadministration ease
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent changes the dosing frequency parameter from multi-day administration to once-daily administration, and selects tablet sizes appropriate for pediatric patients. This makes the treatment regimen practical for children while maintaining comprehensive symptom coverage.

Inventive Principle:
Principle #35Parameter changes

4Reliability

If psychostimulants are used to treat ADHD, then daytime alertness is improved, but nocturnal motor agitation increases causing insomnia

Engineering Contradiction:
Improvedaytime alertnessVSAvoidnocturnal motor agitation
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent changes the pharmacokinetic parameter of plasma half-life to >24 hours, which allows for sustained daytime alertness while the drug's prolonged presence in the system prevents the sharp decline that triggers nocturnal motor agitation and insomnia associated with shorter-acting psychostimulants.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentEP2004183B1Mazindol combination in the treatment of attention deficit/hyperactivity
Publication Date: 2013.06.26 ASSISTANCE PUBLIQUE HOPITAUX DE PARIS (APHP)
  • EP2004183B1 patent drawing

AI summary

The present invention relates to the field of human health, and more particularly to the treatment of attention deficit/hyperactivity disorder (ADHD) with mazindol. The latter can be administered as monotherapy or in combination with one or more compounds, including psychostimulants, for the indication of ADHD and associated or co-morbid symptoms.