2′-O-Fucosyllactose Crystalline Polymorphs for Purity and Stability
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Solution Overview
Problem
The commercialization of complex carbohydrates like 2′-O-fucosyllactose is hindered by challenges in synthesis and purification, with early methods producing impure amorphous forms lacking crystalline modifications, which affect stability, solubility, and other properties crucial for nutritional and therapeutic applications.
Innovation Solution
Development of crystalline polymorphs of 2′-O-fucosyllactose through specific solvent systems and crystallization processes, including the use of C1-C3 alcohols and optional water, allowing for the production of high-purity, thermally stable crystalline forms suitable for large-scale purification and pharmaceutical use.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Measurement precision
If early isolation methods using paper chromatography are used, then 2-FL can be isolated from human milk, but the purity is uncertain due to high number of isomers and lack of high performance chromatography techniques
Solution Approach 1:
The patent changes the physical state parameter of 2-FL from amorphous to crystalline form. This phase transition enables separation based on crystallization properties rather than chromatographic retention, achieving high purity through selective crystallization from specific solvent systems without requiring complex high-performance chromatography equipment
Solution Approach 2:
The patent extracts 2-FL from the complex mixture of human milk oligosaccharides by utilizing its unique crystallization behavior in specific solvent systems. The crystalline form selectively precipitates 2-FL while leaving other isomers and impurities in the mother liquor, effectively separating the target compound without sophisticated chromatographic equipment
2Stability of the object's composition
If 2-FL is produced as amorphous solid, then it is generally available, but it lacks the stability, solubility, and other properties that crystalline forms provide
Solution Approach 1:
The patent induces phase transition of 2-FL from amorphous solid to crystalline form through controlled crystallization processes using specific solvent systems. This phase change confers enhanced stability, defined solubility, and predictable physical properties while maintaining ease of manufacture through relatively simple crystallization protocols compared to complex purification methods
Solution Approach 2:
The patent modifies the physical state parameter of 2-FL by controlling crystallization conditions including solvent composition, temperature, and cooling rate. These parameter changes transform the amorphous material into well-defined crystalline polymorphs with improved stability and characterized physical properties suitable for pharmaceutical applications
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
The crystalline forms of 2′-O-fucosyllactose enhance purity, stability, and solubility, facilitating large-scale production and improving its suitability for nutritional and pharmaceutical applications, addressing the limitations of earlier methods by providing reproducible and high-quality crystalline products.
Implementation Method 1
The present invention provides crystalline 2′-O-fucosyllactose polymorphs and methodologies suitable for large scale purification of 2′-O-fucosyllactose
Implementation Method 2
crystallization or recrystallization is one of the simplest and cheapest methods to separate a product from contaminations and obtain pure substance
Data Source
AI summary
The present invention relates to novel polymorphs of the trisaccharide 2′-O-fucosyllactose (2-FL) of formula (1), methods for producing said polymorphs and their use in pharmaceutical or nutritional compositions.