Sustained Release Beta-Alanine Formulations for Athletic Performance
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Solution Overview
Problem
Current beta-alanine supplements cause adverse side effects like paraesthesia due to rapid absorption, leading to compliance issues and discomfort during anaerobic activities, as they are typically administered in high doses multiple times a day.
Innovation Solution
Development of sustained release formulations of free beta-alanine or its biological sources, such as carnosine, in pharmaceutical and dietary supplements, including tablets, capsules, and topical applications, to gradually increase carnosine biosynthesis in muscles, reducing side effects and enhancing anaerobic working capacity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If high doses of beta-alanine are administered multiple times a day to increase carnosine levels, then athletic performance is improved, but paraesthesia and compliance issues occur
Solution Approach 1:
The patent divides the total beta-alanine dose into multiple smaller units encapsulated in gastro-resistant capsules, releasing the amino acid gradually in the intestine rather than all at once in the stomach. This segmentation of release timing and location maintains effective carnosine synthesis while keeping plasma beta-alanine concentrations low enough to avoid paraesthesia
Solution Approach 2:
The patent uses gastro-resistant capsules as an intermediary delivery system that mediates between the need for high beta-alanine doses and the need to avoid paraesthesia. The capsule acts as a controlled-release vehicle, regulating the timing and location of beta-alanine release to achieve therapeutic effects without adverse sensations
2Reliability
If multiple daily doses are administered to maintain carnosine levels, then muscle buffering capacity is improved, but compliance and convenience deteriorate
Solution Approach 1:
The patent employs periodic action through gastro-resistant capsules that are designed to release beta-alanine at specific intervals after ingestion (typically 2-4 hours in the intestine). This periodic release pattern maintains steady carnosine synthesis over time while requiring only once-or twice-daily dosing, significantly improving compliance
Solution Approach 2:
The gastro-resistant capsule is prepared in advance with embedded beta-alanine in a controlled-release matrix. This preliminary preparation ensures that the exact dosage and release timing are predetermined, eliminating the need for complex dosing schedules and improving ease of use
3Ease of operation
If sustained release formulations are used to reduce paraesthesia, then compliance is improved, but the rate of carnosine synthesis may be reduced
Solution Approach 1:
The patent shifts the release dimension from gastric (stomach) to intestinal by using gastro-resistant capsules. This dimensional change in release location allows for sustained release over several hours while the intestine's absorptive surface area and blood flow maintain efficient uptake, preserving carnosine synthesis rate despite the slower release profile
Data Source
AI summary
Methods and compositions are provided for increasing the anaerobic working capacity of muscle and other tissues. Also provided are compositions formulated for the sustained release of free beta-alanine. Also provided is a dietary supplement formulated, for example, as a solid food product, an edible suspension, liquid or semi-liquid as described herein.