Ozanimod Hydrochloride Form A Crystallization for Improved Flow
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Solution Overview
Problem
Existing crystalline forms of Ozanimod hydrochloride exhibit electrostatic charging, leading to flow problems during industrial production, resulting in inferior products and increased costs.
Innovation Solution
Development of a stable crystalline form, Form A, with improved flow properties, prepared by dissolving Ozanimod hydrochloride in a mixture of water and propanol alcohol, followed by controlled cooling and filtration, yielding a substantially pure form with enhanced stability and non-adherent properties.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Productivity
If known crystalline forms of Ozanimod hydrochloride are used, then the compound can be obtained, but electrostatic charging occurs leading to flow problems during industrial production
Solution Approach 1:
The patent applies parameter changes by modifying the crystallization conditions, specifically using a controlled cooling process from 80°C to 25°C at a rate of 0.5-2°C per minute. This controlled parameter change results in the formation of Crystal Form A with improved flow properties and reduced electrostatic charging, directly resolving the contradiction between productivity and ease of operation
Solution Approach 2:
The patent employs composite materials by combining water and propanol alcohol in a specific volume ratio (3:1 to 7:1, preferably 4:1) as the crystallization solvent system. This composite solvent system enables the formation of Crystal Form A with superior flow characteristics, eliminating the flow problems associated with known crystalline forms while maintaining industrial production efficiency
2Reliability
If known crystalline forms of Ozanimod hydrochloride are used, then the compound can be produced, but surface adhesion increases causing quality issues and higher costs
Solution Approach 1:
The patent applies parameter changes by implementing a specific controlled cooling rate (0.5-2°C per minute) during crystallization. This parameter modification produces Crystal Form A with reduced surface adhesion properties, eliminating the harmful adhesion effects while ensuring consistent product quality and reducing production costs
Solution Approach 2:
The patent converts the potentially harmful electrostatic charging and adhesion properties into beneficial flow characteristics by optimizing the crystallization process. The controlled cooling in the water-propanol alcohol system transforms the crystal structure to reduce surface energy and adhesion, turning what was previously a harmful property into a beneficial flow characteristic
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
Form A exhibits improved flowability and stability, facilitating efficient industrial production and pharmaceutical compositions with reduced costs and improved product quality.
Implementation Method 1
dissolving Ozanimod hydrochloride in a mixture of water and propanol alcohol
Implementation Method 2
followed by controlled cooling and filtration
Implementation Method 3
followed by controlled cooling and filtration, yielding a substantially pure form
Data Source
AI summary
The presented invention relates to crystalline form, Form A of Ozanimod hydrochloride, processes for preparation thereof and pharmaceutical compositions comprising the Ozanimod hydrochloride Form A.