Oclacitinib Maleate Form B Stability Against Humidity

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Solution Overview

Problem

Existing solid state forms of oclacitinib maleate, such as form A, are hygroscopic and unstable at high relative humidity, limiting their shelf-life and stability in pharmaceutical compositions.

Innovation Solution

Identification and characterization of new solid state forms of oclacitinib maleate, including crystalline form B, crystalline monohydrate, crystalline tetramethyl urea solvate, and amorphous forms, which offer improved stability and non-hygroscopic properties.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If crystalline form A of oclacitinib maleate is used, then it can be manufactured and processed, but it is hygroscopic and unstable at high relative humidity, limiting shelf-life

Engineering Contradiction:

Improvestability at high relative humidityVSAvoidhygroscopicity

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by discovering and utilizing different polymorphic forms (form B, monohydrate, tetramethyl urea solvate) and amorphous forms of oclacitinib maleate, each with distinct physical and chemical properties. These different solid state forms exhibit varying degrees of hygroscopicity and stability, allowing selection of forms optimized for high humidity stability while maintaining manufacturability

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent employs composite material strategies by creating pharmaceutical compositions that combine oclacitinib maleate in specific solid state forms with pharmaceutically acceptable excipients and carriers. These composite formulations enhance the stability and shelf-life of the active ingredient while maintaining its therapeutic efficacy

Inventive Principle:

Principle #40Composite materials

2Duration of action of stationary object

If existing solid state forms are used, then pharmaceutical compositions can be prepared, but shelf-life is limited due to instability in humid conditions

Engineering Contradiction:

Improveshelf-lifeVSAvoidstability in humid conditions

Core Design Contradiction:

Duration of action of stationary objectVSReliability

Solution Approach 1:

The patent utilizes parameter changes by identifying and characterizing multiple solid state forms with different stability profiles. The amorphous form and certain crystalline forms (form B, monohydrate) demonstrate enhanced stability under humid storage conditions compared to form A, thereby extending shelf-life while maintaining reliability

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent applies beforehand cushioning by selecting solid state forms that inherently resist hygroscopic degradation and instability under humid conditions. This preventive approach cushions against the harmful effects of humidity before they can compromise the pharmaceutical composition, ensuring extended shelf-life and maintained stability

Inventive Principle:

Principle #11Beforehand cushioning (Prior cushioning)

Data Source

PatentUS12202834B2Solid state forms of oclacitinib maleate

Publication Date: 2025.01.21 VATIONPHARMA BV

AI summary

The present invention relates to solid state forms of oclacitinib maleate and methods for the preparation of the solid state forms of oclacitinib maleate. The solid state forms of oclacitinib maleate of the present invention include amorphous oclacitinib maleate, crystalline tetramethyl urea solvate form of oclacitinib maleate, crystalline monohydrate form of oclacitinib maleate and crystalline form of oclacitinib maleate (form B).