Multibranched Polyoxyalkylene Derivative Viscosity Reduction
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Solution Overview
Problem
Current methods for modifying bio-related substances with polyoxyalkylene derivatives face challenges in producing high-molecular-weight derivatives with high purity and low viscosity, while maintaining the bioactivity of the substances, due to issues such as impurities and reactivity limitations.
Innovation Solution
A multibranched polyoxyalkylene derivative with reactive groups and oxyalkylene chains is developed, featuring a specific molecular structure that allows for increased hydration layer formation without blocking active sites, improving reactivity and reducing viscosity, and can be produced efficiently with high purity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If high-molecular-weight polyoxyalkylene is produced to increase hydration layer, then the pharmacological effect is improved, but the purity decreases and viscosity increases making production difficult
Solution Approach 1:
The invention uses a multibranched polyoxyalkylene structure where multiple polyoxyalkylene chains (typically 3-10 chains) are connected to a central core molecule. This segmentation allows each chain to contribute to the hydration layer independently, achieving the desired pharmacological effect while the branched architecture prevents excessive viscosity increase and facilitates purification by enabling selective removal of unreacted starting materials and by-products through standard purification techniques
2Reliability
If high-molecular-weight polyoxyalkylene is produced to increase hydration layer, then the pharmacological effect is improved, but the viscosity increases making handling difficult
Solution Approach 1:
The multibranched structure segments the polyoxyalkylene chains into multiple smaller units radiating from a central core, which reduces the overall viscosity compared to a linear high-molecular-weight polymer while maintaining the cumulative hydration effect. This segmentation makes the substance easier to handle, dissolve, and incorporate into pharmaceutical formulations
Solution Approach 2:
The invention transitions from a linear one-dimensional polyoxyalkylene structure to a three-dimensional multibranched architecture. This dimensional change allows the polymer to occupy more space efficiently with lower molecular weight, reducing viscosity while maintaining or enhancing the hydration layer thickness, thereby improving both pharmacological effect and ease of handling
3Reliability
If polyoxyalkylene with double-chain structure is used to increase molecular weight, then the pharmacological effect is improved, but the structure is limited and cannot provide sufficient hydration layer
Solution Approach 1:
The multibranched polyoxyalkylene structure provides multi-functionality by enabling the single molecule to serve multiple roles: each polyoxyalkylene chain contributes to hydration layer formation, the central core provides structural stability, and the overall architecture allows for adjustable molecular weight and branching degree. This universality enables sufficient hydration layer capacity that exceeds what is achievable with simple double-chain structures, while maintaining improved pharmacological effect
4Ease of manufacture
If excess single-chain polyoxyalkylene derivative is used to introduce multiple chains, then the target structure is formed, but unreacted excess remains as impurity requiring removal
Solution Approach 1:
The invention uses a core molecule with multiple reactive groups (such as cyanuric chloride, triphosgene, or polyhydric alcohols) that are pre-configured to react with polyoxyalkylene derivatives. This preliminary arrangement of reactive sites on the core allows for controlled stepwise introduction of polyoxyalkylene chains, reducing the need for large excess of starting material and minimizing unreacted impurities that would require removal
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 multibranched polyoxyalkylene derivative effectively maintains bioactivity by forming a large hydration layer, reduces viscosity for easier handling, and is produced with high purity, addressing the challenges of existing methods.
Implementation Method 1
increasing their molecular weight or formation of a hydration layer through chemical modification with an amphiphatic polymer such as a sugar chain or polyethylene glycol
Data Source
AI summary
An object of the present invention is to provide a novel multibranched polyoxyalkylene derivative, and an intermediate for the production thereof. Specifically, the object is to provide a multibranched polyoxyalkylene derivative which can keep a high activity of a bio-related substance modified with the multibranched polyoxyalkylene derivative and which can easily produce the modified substance; an intermediate thereof; and a bio-related substance to which the multibranched polyoxyalkylene derivative is bonded. The novel multibranched polyoxyalkylene derivative according to the invention is a polyoxyalkylene derivative (1) having a functional group reactive with a bio-related substance and the bio-related substance according to the invention has a structure modified with the above polyoxyalkylene derivative (1) by a reaction. Furthermore, the intermediate for the production of the novel multibranched polyoxyalkylene derivative according to the invention is a polyoxyalkylene derivative (A). wherein A1O and A2O independently represent an oxyalkylene group having 2 to 4 carbon atoms, m represents 20 to 500, n represents 15 to 700, R represents a hydrogen atom or a hydrocarbon group having 1 to 20 carbon atoms, X represents a functional group reactive with a bio-related substance, and X1 represents a hydroxyl group which may be protected.