Lacosamide Extended Release Dosage Form for Seizure Control

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Solution Overview

Problem

Current pharmaceutical formulations of lacosamide for treating partial onset seizures require twice-daily administration, leading to high peak-trough fluctuations and increased adverse reactions due to high maximum steady-state plasma concentrations.

Innovation Solution

Development of an extended release dosage form of lacosamide that includes a combination of an extended release portion and an optional immediate release portion, designed to maintain therapeutic blood levels for 24 hours with reduced peak-trough fluctuations.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If immediate release dosage form is administered twice daily to achieve therapeutic effect, then seizure control is improved, but peak-trough fluctuations increase and adverse reactions occur more frequently

Engineering Contradiction:

Improveseizure control efficacyVSAvoidadverse reactions and peak-trough fluctuations

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The dosage form is divided into multiple particles or granules with different release characteristics (immediate release portion and extended release portion), allowing the drug to be released in a controlled manner over time. This segmentation enables maintaining therapeutic efficacy while reducing peak-trough fluctuations and adverse reactions.

Inventive Principle:

Principle #1Segmentation

2Reliability

If high daily dose is administered as immediate release to treat partial onset seizures, then therapeutic effect is improved, but incidence of adverse reactions increases

Engineering Contradiction:

Improvetreatment efficacyVSAvoidadverse reactions

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the release rate parameter of the drug by developing an extended release dosage form. This transforms the immediate release characteristic into a controlled, sustained release profile, thereby maintaining the same daily dose while reducing peak concentrations that cause adverse reactions.

Inventive Principle:

Principle #35Parameter changes

3Reliability

If twice-daily administration is used to maintain therapeutic blood levels, then seizure protection is improved, but patient compliance deteriorates due to frequent dosing

Engineering Contradiction:

Improvetherapeutic blood level maintenanceVSAvoidpatient compliance

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The extended release dosage form provides continuous release of lacosamide over 24 hours, maintaining therapeutic blood levels throughout the dosing interval. This continuous action eliminates the need for twice-daily administration, thereby improving patient compliance while maintaining seizure protection.

Inventive Principle:

Principle #20Continuity of useful action

4Ease of operation

If extended release dosage form is developed for once-daily administration, then patient compliance and reduction of adverse reactions are improved, but manufacturing complexity increases

Engineering Contradiction:

Improvepatient complianceVSAvoiddosage form structure

Core Design Contradiction:

Ease of operationVSDevice complexity

Solution Approach 1:

The patent uses composite materials comprising different types of particles or granules (immediate release and extended release portions) to achieve the desired release profile. This composite approach allows once-daily administration with reduced adverse reactions while managing manufacturing complexity through the use of established pharmaceutical excipients and formulations.

Inventive Principle:

Principle #40Composite materials

Data Source

PatentUS20250025433A1Lacosamide pharmaceutical composition and dosage form thereof

Publication Date: 2025.01.23 SHANGHAI AUCTA PHARMA CO LTD

AI summary

A dosage form of lacosamide and a pharmaceutical dosage form thereof is disclosed. The dosage form includes an extended release portion and optionally an immediate release portion. Also provided are methods of providing extended release of lacosamide and treatment of: neurological or psychiatric disease or condition.