Polyglycerol Esters for Sustained BHB Release
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Solution Overview
Problem
Current methods lack efficient and physiologically compatible precursors or metabolites for 3-hydroxybutyric acid (BHB) or its salts, which are essential for therapeutic applications but face issues with toxicity, nausea, and short plasma half-life, limiting their effectiveness in treating metabolic and neurodegenerative diseases.
Innovation Solution
The development of polyglycerol esters of polycarboxylic acids esterified with oxobutanol, which serve as efficient and physiologically compatible precursors or metabolites for 3-hydroxybutyric acid, allowing for direct and effective access to BHB, reducing toxicity and extending its therapeutic duration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If 3-hydroxybutyric acid or its salts are administered orally, then therapeutic effect is achieved, but toxicity and nausea occur
Solution Approach 1:
The patent introduces polyglycerol esters of polycarboxylic acids esterified with oxobutanol as intermediary compounds that serve as precursors to 3-hydroxybutyric acid. These esters act as carriers that deliver the active substance in a physiologically compatible form, avoiding direct administration of the toxic free acid while still achieving the desired therapeutic effect through metabolic conversion.
Solution Approach 2:
The patent changes the chemical form of 3-hydroxybutyric acid from free acid to esterified form (polyglycerol esters of polycarboxylic acids esterified with oxobutanol). This parameter change in molecular structure improves physiological compatibility and eliminates toxicity and nausea side effects while maintaining therapeutic efficacy through metabolic breakdown.
2Reliability
If 3-hydroxybutyric acid is administered, then therapeutic effect is achieved, but plasma half-life is short
Solution Approach 1:
The patent uses polyglycerol esters of polycarboxylic acids esterified with oxobutanol as preliminary compounds that are metabolically converted to 3-hydroxybutyric acid. This preliminary action allows for sustained release and prolonged plasma half-life compared to direct administration of the free acid, which is rapidly cleared from the system.
3Reliability
If larger quantities of 3-hydroxybutyric acid are administered, then therapeutic benefit is enhanced, but side effects increase
Solution Approach 1:
The patent employs polyglycerol esters of polycarboxylic acids esterified with oxobutanol as intermediary carriers that can deliver larger total quantities of 3-hydroxybutyric acid equivalent while maintaining physiological compatibility. The ester form allows for higher administration doses without proportionally increasing side effects, as the body processes the ester form more tolerably.
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 polyglycerol esters provide a continuous and prolonged release of 3-hydroxybutyric acid, minimizing side effects and enabling larger quantities to be administered safely, thus enhancing therapeutic benefits for metabolic and neurodegenerative disease treatments.
Implementation Method 1
polyglycerol esters of polycarboxylic acids esterified with oxobutanol... provide a continuous and prolonged release of 3-hydroxybutyric acid
Data Source
AI summary
The invention relates to a method for producing polyglycerol esters of polycarboxylic acids esterified with oxobutanol, in particular mono- or polyvalent polyglycerol esters of polycarboxylic acids esterified with 4-oxo-4-(C1-C5-alkoxy)-2-butanol or with 4-oxo-4-(hydroxy-C3-C5-alkoxy)-2-butanol. The invention also relates to products obtainable in this manner and to the use thereof.