Beta-Hydroxybutyric Acid Compositions for Oral Delivery
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Solution Overview
Problem
Current methods for delivering exogenous ketone bodies, such as beta-hydroxybutyric acid, face challenges including excessive electrolyte introduction, unpleasant taste, and gastrointestinal distress, particularly when administered in salt forms or as esters, and require dilute solutions to prevent acidosis and isotonic deficiencies.
Innovation Solution
Aqueous beta-hydroxybutyric acid compositions that are free or substantially free of beta-hydroxybutyrate salts, administered in specific concentration ranges to maintain stability and prevent self-esterification, allowing for rapid blood ketone level elevation without causing acute acidosis or gastrointestinal distress, and can be provided as concentrates for later dilution by the user.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If beta-hydroxybutyric acid is administered in salt forms (beta-hydroxybutyrate salts), then ketone body delivery is achieved, but excessive electrolyte introduction and altered electrolyte balance occur
Solution Approach 1:
The patent extracts and removes the electrolyte component (metal cations) from the beta-hydroxybutyrate salt structure, delivering only the active ketone body moiety. This is achieved by using beta-hydroxybutyric acid or its esters instead of salts, thereby eliminating excessive electrolyte introduction while maintaining ketone body delivery efficacy
Solution Approach 2:
The patent introduces esters of beta-hydroxybutyric acid as intermediary compounds that can be hydrolyzed to release the active ketone body without introducing electrolytes. These esters serve as a mediator between the desired ketone body delivery and the avoidance of electrolyte imbalance
2Productivity
If beta-hydroxybutyric acid is administered in concentrated forms, then ketone body delivery efficiency is improved, but acute acidosis and gastrointestinal distress occur
Solution Approach 1:
The patent changes the concentration parameter of beta-hydroxybutyric acid administration to optimal ranges (0.1-10% w/v) that balance delivery efficiency with safety. This parameter optimization prevents acute acidosis and gastrointestinal distress while maintaining effective ketone body delivery
Solution Approach 2:
The patent uses esters of beta-hydroxybutyric acid as intermediary compounds that provide a buffer against the acidic effects of the free acid. These esters hydrolyze to release the active ketone body more gradually, reducing the risk of acute acidosis and gastrointestinal distress
3Object-affected harmful factors
If beta-hydroxybutyric acid solutions are made dilute to prevent acidosis, then tolerability is improved, but the volume required for effective delivery increases
Solution Approach 1:
The patent optimizes the concentration parameter to a specific range (0.1-10% w/v) that achieves the dual goal of preventing acidosis while maintaining effective delivery in reasonable volumes. This parameter optimization resolves the trade-off between dilution and delivery efficiency
Solution Approach 2:
The patent uses esters as alternative forms that provide similar ketone body delivery benefits without the severe acidic effects, allowing for more concentrated formulations that reduce the volume required while maintaining tolerability
4Object-generated harmful factors
If beta-hydroxybutyric acid is administered as esters, then electrolyte balance is maintained, but unpleasant taste and hydrolysis requirements occur
Solution Approach 1:
The patent selects specific ester compounds with improved sensory properties and appropriate hydrolysis rates. By changing the chemical structure parameter to specific esters, the formulation achieves better taste acceptability while maintaining the electrolyte-free advantage and appropriate release characteristics
Data Source
AI summary
Beta-hydroxybutyric acid compositions for oral delivery are substantially free of beta-hydroxybutyrate salts and are effective in rapidly raising blood ketone levels without causing acute acidosis or gastrointestinal (GI) distress when consumed in sufficiently dilute form and/or as a gel or suspension. By excluding beta-hydroxybutyrate salts (e.g., less than 1% by weight) containing alkali or alkaline earth metal ions, beta-hydroxybutyric acid solutions, gels, or suspensions can deliver exogenous ketone bodies without significantly altering electrolyte balance. Although aqueous beta-hydroxybutyric acid solutions are moderately acidic with a pH of about 3.5 to 4, when diluted with sufficient water, the water acts as a pseudo buffering agent that offsets otherwise harsh acidic effects when consumed orally. Gels and suspensions can also ameliorate acidic effects by partially encapsulating the beta-hydroxybutyric acid. Beta-hydroxybutyric acid can be enriched with the R- or the S-enantiomer, a racemic mixture, pure R-beta-hydroxybutyric acid, or pure S-beta-hydroxybutyric acid.