Oxobutanol Polymer Esters for Continuous 3-Hydroxybutyrate Release
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Solution Overview
Problem
Existing methods fail to provide physiologically suitable precursors or metabolites for 3-hydroxybutyric acid or its salts, which are effective and compatible for therapeutic use, especially in treating metabolic and neurodegenerative diseases, due to their short plasma half-life, toxicity, and poor physiological compatibility.
Innovation Solution
A method for producing oxobutanol esters of polymeric carboxylic acids, specifically 4-oxo-4-(C1-C5-alkoxy)-2-butanol esters or 4-oxo-4-(hydroxy-C3-C5-alkoxy)-2-butanol esters, through esterification with polymeric carboxylic acids, providing a physiologically compatible precursor and metabolite for 3-hydroxybutyric acid or its salts.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If 3-hydroxybutyric acid or its salts are used as therapeutic agents, then therapeutic effectiveness is improved, but plasma half-life is too short and toxicity increases
Solution Approach 1:
The patent segments the single molecule of 3-hydroxybutyric acid into multiple units by forming a polymer structure. The polymeric carboxylic acid contains multiple carboxyl groups that can be esterified with oxobutanol, creating a polymer with repeated therapeutic units that release 3-hydroxybutyric acid gradually, thereby extending plasma half-life while maintaining therapeutic effectiveness.
Solution Approach 2:
The patent creates a composite molecular structure by combining oxobutanol units with polymeric carboxylic acid chains. This composite polymeric ester structure allows the therapeutic agent to persist in the body longer through gradual degradation and release, solving the short half-life problem while avoiding the toxicity issues of conventional formulations.
2Reliability
If conventional methods are used to produce 3-hydroxybutyric acid, then therapeutic activity is achieved, but physiological compatibility is poor and toxicity occurs
Solution Approach 1:
The patent introduces oxobutanol as an intermediary compound that forms ester bonds with polymeric carboxylic acid. This intermediary structure serves as a carrier that delivers 3-hydroxybutyric acid in a controlled manner, improving physiological compatibility by reducing the abrupt presence of the active compound in the body, thereby lowering toxicity while maintaining therapeutic activity.
Solution Approach 2:
The patent changes the molecular parameters of 3-hydroxybutyric acid by polymerizing it into a macromolecular structure. This parameter change from monomeric to polymeric form alters the pharmacokinetic properties, improving physiological compatibility and reducing toxicity while preserving the core therapeutic activity of the 3-hydroxybutyric acid units.
3Quantity of substance
If polymeric carboxylic acids are esterified with oxobutanol, then drug density is increased, but manufacturing complexity increases
Solution Approach 1:
The patent performs preliminary action by pre-synthesizing the polymeric carboxylic acid with multiple carboxyl groups before the esterification step. This preliminary preparation of the polymer backbone with reactive groups allows for efficient one-pot esterification with oxobutanol, achieving high drug density without requiring complex multi-step synthesis procedures, thus managing manufacturing complexity.
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 method allows for the production of oxobutanol esters of polymeric carboxylic acids that are physiologically compatible, enabling continuous release of 3-hydroxybutyric acid or its salts, reducing toxicity, and offering a high drug density with minimal by-products, suitable for therapeutic and food applications.
Implementation Method 1
at least one oxobutanol... is reacted with at least one polymeric carboxylic acid... so that, as a reaction product, one or more oxobutanol esters of the polymeric carboxylic acid is/are obtained
Data Source
AI summary
The invention relates to a method for producing oxobutanol esters of polymeric carboxylic acids, especially 4-oxo-4-(C1-C5-alkoxy)-2-butanol esters or 4-oxo-4-(hydroxy-C3-C5-alkoxy)-2-butanol esters of polymeric carboxylic acids, as well as the products thus obtained and their use.