pH-Responsive Abuse Deterrent Pharmaceutical Compositions

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Solution Overview

Problem

There is a need for pharmaceutical compositions that minimize the potential for improper administration and abuse of medications, particularly pain medications, stimulants, and anxiety-reducing drugs, while ensuring effective oral administration and reducing the euphoric effect associated with improper use.

Innovation Solution

The development of oral pharmaceutical compositions incorporating a drug, a pH-dependent agent, and a pH-independent agent, which are designed to release the drug effectively in acidic environments but retard release in neutral or alkaline conditions, thereby discouraging injection or insufflation abuse and ensuring therapeutic efficacy through controlled release mechanisms.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If the drug is formulated for immediate release, then the therapeutic efficacy is improved, but the abuse potential increases

Engineering Contradiction:

Improvetherapeutic efficacyVSAvoidabuse potential

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies dynamics by making the drug release rate variable based on environmental conditions. The composition releases drug rapidly in acidic environments (simulating oral stomach conditions) but slowly in neutral/alkaline environments (simulating injection or insufflation conditions), thus adapting the release profile to the administration route to prevent abuse while maintaining efficacy

Inventive Principle:

Principle #15Dynamics

Solution Approach 2:

The patent changes the pH parameter as the controlling factor for drug release. By formulating with pH-dependent release characteristics, the composition automatically adjusts its drug release behavior based on the pH of the surrounding environment, enabling differentiated release profiles for different administration routes

Inventive Principle:

Principle #35Parameter changes

2Object-affected harmful factors

If the drug release is retarded in neutral/alkaline conditions, then the abuse deterrent effect is improved, but the oral bioavailability may be reduced

Engineering Contradiction:

Improveabuse deterrent effectVSAvoidoral bioavailability

Core Design Contradiction:

Object-affected harmful factorsVSReliability

Solution Approach 1:

The dynamic release mechanism ensures rapid drug release in acidic conditions (pH < 5) that simulate the oral gastric environment, thereby maintaining oral bioavailability. The same dynamic mechanism retards release in neutral/alkaline conditions (pH ≥ 5) that simulate abuse routes, thus achieving both goals simultaneously through environment-responsive behavior

Inventive Principle:

Principle #15Dynamics

Solution Approach 2:

The formulation incorporates preliminary anti-action by pre-designing the pH-dependent release characteristics to counteract potential abuse before it occurs. The composition is engineered to inherently resist release under abuse conditions (neutral/alkaline pH) while facilitating release under legitimate use conditions (acidic pH), creating a built-in protective mechanism

Inventive Principle:

Principle #9Preliminary anti-action

3Object-affected harmful factors

If the composition is designed for controlled release, then the abuse potential is reduced, but the device complexity increases

Engineering Contradiction:

Improveabuse potentialVSAvoidcomposition complexity

Core Design Contradiction:

Object-affected harmful factorsVSDevice complexity

Solution Approach 1:

The patent utilizes parameter changes (pH) as the controlling mechanism for drug release, which is a natural environmental parameter rather than a mechanical or electronic control system. This approach achieves controlled release with minimal compositional complexity by leveraging the inherent pH differences between legitimate oral administration and abuse routes

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The composition performs self-service by automatically adjusting its drug release profile in response to the pH environment without requiring external control mechanisms. The formulation itself contains the intelligence to differentiate between appropriate and inappropriate administration routes through its pH-responsive properties, eliminating the need for complex control systems

Inventive Principle:

Principle #25Self-service

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The compositions effectively deliver a therapeutically relevant amount of the drug orally while significantly reducing the potential for abuse by limiting drug release in non-oral administration methods, maintaining therapeutic efficacy while minimizing euphoric effects and abuse potential.

Implementation Method 1

Methodology Applied

Scientific EffectpH-dependent dissolution:

Implementation Method 2

ensuring therapeutic efficacy through controlled release mechanisms

Methodology Applied

Scientific EffectControlled release:

Data Source

PatentUS11571390B2Abuse deterrent compositions and methods of use

Publication Date: 2023.02.07 OHEMO LIFE SCI INC

AI summary

Orally administrable pharmaceutical compositions, methods of administration, and methods of making the same are provided. The pharmaceutical compositions provide abuse deterrent properties.