Gastroretentive Acamprosate Formulation for Controlled Release

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Solution Overview

Problem

Acamprosate, a compound used to treat alcoholism and neuropsychiatric disorders, has low bioavailability due to its high solubility and low permeability, leading to inefficient absorption and frequent dosing requirements, along with dose-dependent side effects and high doses needed for efficacy.

Innovation Solution

The development of gastroretentive (GR) formulations of acamprosate that provide controlled release, allowing for less frequent dosing and reduced side effects by maintaining therapeutic levels for extended periods, combined with other medications like neuroleptics, SSRIs, and SNRIs in fixed-dose combinations.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Speed

If immediate-release formulations of acamprosate are used, then the drug can be absorbed quickly, but the bioavailability is low and frequent dosing is required

Engineering Contradiction:

Improveabsorption speedVSAvoidbioavailability

Core Design Contradiction:

SpeedVSReliability

Solution Approach 1:

The patent divides the single dose into multiple smaller doses that are released sequentially over time through the gastroretentive system, maintaining steady drug levels in the bloodstream without requiring frequent re-dosing

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The formulation dynamically adjusts drug release based on gastric retention time, providing sustained release of acamprosate over several hours to improve bioavailability while reducing dosing frequency

Inventive Principle:

Principle #15Dynamics

2Reliability

If higher doses of acamprosate are administered to achieve efficacy, then therapeutic benefits improve, but dose-dependent side effects increase

Engineering Contradiction:

Improvetherapeutic efficacyVSAvoidside effects

Core Design Contradiction:

ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The gastroretentive formulation provides continuous release of acamprosate at optimized concentrations over an extended period, maintaining therapeutic efficacy while avoiding the peaks associated with high single doses that cause side effects

Inventive Principle:

Principle #20Continuity of useful action

3Reliability

If frequent dosing is required to maintain therapeutic levels, then therapeutic coverage is improved, but treatment adherence becomes more difficult

Engineering Contradiction:

Improvetherapeutic coverageVSAvoidtreatment adherence

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The formulation segments the dosing schedule by providing extended-release capabilities that allow less frequent administration (e.g., once or twice daily instead of multiple times daily), improving patient compliance while maintaining continuous therapeutic coverage

Inventive Principle:

Principle #1Segmentation

Data Source

PatentEP2785337B1Acamprosate formulations, methods of using the same, and combinations comprising the same

Publication Date: 2021.01.20 SYNCHRONEURON INC

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AI summary

Embodiments disclosed herein generally relate to acamprosate formulations, methods of use of the formulations, to methods of using the formulations in combination with at least one other medication, and to combination products and compositions comprising the formulations and at least one other medication, such as neuroleptic (antipsychotic) and/or antidepressant drugs.