D-Amphetamine Covalent Bonding for Sustained Release

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Solution Overview

Problem

Current d-amphetamine treatments suffer from rapid drug concentration spikes leading to undesirable side effects, cardiovascular risks, and high abuse potential due to their immediate release formulations, which result in rebound symptoms and increased risk of addiction.

Innovation Solution

Development of novel compounds and compositions of d-amphetamine covalently bonded with organic compounds, such as heterocyclic nitrogen compounds or amino acids, designed for controlled and sustained release, reducing rapid blood concentration spikes and enhancing therapeutic efficacy while minimizing abuse potential.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Speed

If immediate release formulations of d-amphetamine are used, then rapid therapeutic effect is achieved, but rapid blood concentration spikes occur leading to side effects and abuse potential

Engineering Contradiction:

Improveonset of therapeutic effectVSAvoidcardiovascular stress and abuse potential

Core Design Contradiction:

SpeedVSObject-affected harmful factors

Solution Approach 1:

The patent applies preliminary action by covalently bonding d-amphetamine to organic compounds (such as amino acids or heterocyclic nitrogen compounds) to create prodrug derivatives. These derivatives are metabolized in the body to release d-amphetamine in a controlled manner, preventing rapid blood concentration spikes while maintaining therapeutic efficacy. The bonding act is performed in advance to modify the release profile of the active ingredient.

Inventive Principle:

Principle #10Preliminary action

2Object-affected harmful factors

If sustained release formulations are developed to reduce blood concentration spikes, then cardiovascular risks are reduced, but the complexity of the drug formulation increases

Engineering Contradiction:

Improvecardiovascular stressVSAvoidformulation complexity

Core Design Contradiction:

Object-affected harmful factorsVSDevice complexity

Solution Approach 1:

The patent applies parameter changes by modifying the chemical structure of d-amphetamine through covalent bonding with organic compounds. This chemical modification changes the pharmacokinetic parameters of the drug, specifically the release rate and blood concentration profile, thereby reducing cardiovascular stress without requiring complex physical formulation systems.

Inventive Principle:

Principle #35Parameter changes

3Object-affected harmful factors

If d-amphetamine is covalently bonded with organic compounds for controlled release, then abuse potential is reduced, but the manufacturing process becomes more complex

Engineering Contradiction:

Improveabuse liabilityVSAvoidsynthesis process simplicity

Core Design Contradiction:

Object-affected harmful factorsVSEase of manufacture

Solution Approach 1:

The patent uses organic compounds (amino acids or heterocyclic nitrogen compounds) as intermediaries to covalently bond with d-amphetamine. These intermediary molecules facilitate controlled release of the active ingredient while reducing abuse potential. The intermediaries are metabolized or cleaved in the body to release d-amphetamine, providing a bridge between the need for controlled release and therapeutic efficacy.

Inventive Principle:

Principle #24Intermediary (Mediator)

Data Source

PatentUS12091386B2D-amphetamine compounds, compositions, and processes for making and using the same

Publication Date: 2024.09.17 ZEVRA THERAPEUTICS INC

AI summary

Disclosed are d-amphetamine compounds and compositions comprising at least one organic acid covalently bound to d-amphetamine, having the structure ofa salt thereof, a derivative thereof, or a combination thereof. Methods of making and using the same are also disclosed.