Roluperidone Solid-State Forms for Stability and Bioavailability

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Solution Overview

Problem

Existing formulations of roluperidone lack desirable properties for improved processing, handling, stability, and bioavailability, limiting their effectiveness in treating schizophrenia.

Innovation Solution

Development of various solid state forms and salts of roluperidone, including crystalline forms and co-crystals, which offer enhanced properties such as chemical stability, solubility, and bioavailability, facilitating better pharmaceutical compositions and formulations.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing formulations of roluperidone are used, then the basic therapeutic function is provided, but processing characteristics, handling, stability, and bioavailability are insufficient

Engineering Contradiction:

ImprovestabilityVSAvoidprocessing characteristics

Core Design Contradiction:

ReliabilityVSEase of manufacture

Solution Approach 1:

The patent applies parameter changes by discovering and utilizing different solid state forms (polymorphs, solvates, hydrates) of roluperidone, each with distinct physical and chemical parameters. These different crystal structures provide improved stability, solubility, and processing characteristics while maintaining the core therapeutic function of the drug

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent employs composite materials by creating co-crystals of roluperidone with various co-formers. These co-crystal structures combine roluperidone with other molecular components to achieve enhanced stability, improved bioavailability, and better processing characteristics that neither component achieves alone

Inventive Principle:

Principle #40Composite materials

2Reliability

If existing formulations of roluperidone are used, then the basic therapeutic function is provided, but solubility and bioavailability are limited

Engineering Contradiction:

ImprovebioavailabilityVSAvoidsolubility

Core Design Contradiction:

ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent utilizes parameter changes by identifying solid state forms with different solubility characteristics. By selecting appropriate polymorphs, solvates, or hydrates, the formulation achieves improved solubility and bioavailability while maintaining adequate stability for pharmaceutical use

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent applies the intermediary principle by using solvates and hydrates where solvent molecules are incorporated into the crystal structure. These intermediary solvent molecules facilitate improved solubility and bioavailability while the overall crystal structure maintains stability

Inventive Principle:

Principle #24Intermediary (Mediator)

Data Source

PatentUS12441701B2Solid state forms of roluperidone and salts thereof

Publication Date: 2025.10.14 TAPI CZECH INDUSTRIES SRO

AI summary

The present disclosure relates to solid state forms of roluperidone and salts thereof, processes for preparation thereof, and pharmaceutical compositions thereof.