Centanafadine Bead Formulations for Pediatric Once-Daily Release

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Solution Overview

Problem

There is a need for novel pharmaceutical compositions of centanafadine, particularly in a form suitable for pediatric use and with controlled release profiles, to address the challenges of administering this drug effectively and efficiently.

Innovation Solution

The development of pharmaceutical formulations comprising centanafadine or its pharmaceutically acceptable salts, including beads with core particles containing centanafadine and excipients, which provide a multiphasic release profile and delayed-sustained release characteristics, suitable for pediatric use and stable under elevated temperatures and humidity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If centanafadine is administered in conventional formulations, then the drug can be delivered to patients, but it requires frequent dosing and lacks controlled release profiles

Engineering Contradiction:

Improveduration of drug actionVSAvoiddosing frequency

Core Design Contradiction:

Duration of action of moving objectVSProductivity

Solution Approach 1:

The formulation segments the drug delivery system into multiple bead types with different release characteristics (immediate-release beads, sustained-release beads, delayed-release beads). Each bead type contains centanafadine with distinct release profiles, allowing the combination to provide prolonged therapeutic coverage and enable once-daily dosing while maintaining effective drug levels throughout the dosing interval.

Inventive Principle:

Principle #1Segmentation

2Adaptability or versatility

If pediatric formulations are developed, then the drug becomes suitable for children, but formulation complexity increases

Engineering Contradiction:

Improvesuitability for pediatric useVSAvoidformulation complexity

Core Design Contradiction:

Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The patent combines multiple functional bead types (immediate-release, sustained-release, delayed-release) into a single composite formulation. This merging approach integrates various release mechanisms and excipient systems into one unified pediatric-friendly dosage form, providing both simplicity for administration and the complex controlled-release functionality needed for once-daily dosing in children.

Inventive Principle:

Principle #5Merging (Combining)

3Reliability

If stable formulations are created for harsh conditions, then the drug remains stable under elevated temperatures and humidity, but manufacturing constraints increase

Engineering Contradiction:

Improvestability under elevated temperatures and humidityVSAvoidmanufacturing constraints

Core Design Contradiction:

ReliabilityVSEase of manufacture

Solution Approach 1:

The formulation employs parameter changes by selecting excipients and coating materials with specific properties that provide stability across a range of environmental conditions. The bead coating system and excipient selection are optimized to maintain drug stability under elevated temperatures and humidity while remaining compatible with standard manufacturing processes, thus achieving robust stability without excessive manufacturing complexity.

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentUS12370144B2Centanafadine pharmaceutical formulations, and methods of making and using same

Publication Date: 2025.07.29 OTSUKA PHARM CO LTD

AI summary

Pharmaceutical formulation comprising centanafadine or a pharmaceutically acceptable salt thereof and an excipient, and related methods of manufacture and use, are disclosed.