Dispersible Benzamide Formulation for Swallowability and Bioavailability

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Solution Overview

Problem

There is a need for an age-appropriate and swallowable formulation of N-((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide to treat tumors, cancers, or Rasopathy disorders, particularly in pediatric patients or those with dysphagia, as existing formulations are difficult to administer and can lead to polymorphic interconversion affecting solubility and bioavailability.

Innovation Solution

Development of dispersible formulations, including crystalline Form IV of N-((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide, which are dispersible in liquids or orodispersible in saliva, ensuring accurate dosing and enhanced adherence, while maintaining stability and purity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If conventional formulations (capsules or tablets) are used, then the drug can be administered to adults, but pediatric patients or those with dysphagia cannot swallow them properly

Engineering Contradiction:

ImproveswallowabilityVSAvoidage-appropriateness

Core Design Contradiction:

Ease of operationVSAdaptability or versatility

Solution Approach 1:

The patent transforms the physical state and size parameters of the drug formulation by creating dispersible tablets that can be broken into smaller pieces or dissolved in liquid, making them suitable for pediatric patients and those with swallowing difficulties while maintaining the same active ingredient and therapeutic effect

Inventive Principle:

Principle #35Parameter changes

2Ease of manufacture

If the drug is administered in non-dispersible form, then manufacturing is simpler, but polymorphic interconversion occurs affecting solubility and bioavailability

Engineering Contradiction:

Improveformulation simplicityVSAvoidbioavailability consistency

Core Design Contradiction:

Ease of manufactureVSReliability

Solution Approach 1:

The patent applies preliminary action by pre-converting the drug into a specific polymorphic form (Form IV) with controlled crystal structure and stability properties before administration, preventing subsequent polymorphic interconversion that would otherwise occur in the body and affect bioavailability consistency

Inventive Principle:

Principle #10Preliminary action

Solution Approach 2:

The patent uses composite material principles by formulating the drug with specific excipients and using co-crystallization techniques to create a stable composite structure that maintains consistent polymorphic form and prevents interconversion, ensuring reliable solubility and bioavailability

Inventive Principle:

Principle #40Composite materials

Data Source

PatentUS20260083690A1Dispersible formulations of n-((r)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2- fluoro-4-iodo-phenylamino)-benazmide and uses thereof

Publication Date: 2026.03.26 SPRINGWORKS THERAPEUTICS INC

AI summary

The present disclosure relates to dispersible pharmaceutical compositions comprising N-((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide, and, optionally, a pharmaceutically acceptable carrier.