SAM-e Gallic Acid Ester Compositions for Improved Uptake

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Solution Overview

Problem

The low uptake and efficacy of exogenous S-adenosyl-L-methionine (SAMe) supplementation necessitates the development of compositions to enhance its delivery and plasma levels.

Innovation Solution

Compositions comprising exogenous SAMe and gallic acid esters, particularly ethyl gallate, isoamyl gallate, or propyl gallate, with optimized weight ratios, are formulated to improve SAMe levels in vivo.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If exogenous SAMe is administered alone, then it is simple to use, but the uptake and plasma levels are very low

Engineering Contradiction:

Improveuptake and plasma levelsVSAvoidcomposition complexity

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

Gallic acid esters are used as intermediary substances that facilitate the absorption and uptake of exogenous SAMe. The gallic acid ester component acts as a mediator that enhances the bioavailability of SAMe, allowing it to achieve therapeutic plasma levels that cannot be obtained with SAMe alone.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention creates a composite composition combining SAMe with gallic acid esters. This composite formulation leverages the synergistic effects of both components, where the gallic acid ester enhances SAMe absorption while SAMe provides the therapeutic benefit, resolving the contradiction between simplicity and effectiveness.

Inventive Principle:

Principle #40Composite materials

2Reliability

If conventional dosage forms of SAMe are used, then the formulation is simple, but SAMe levels in vivo are insufficient

Engineering Contradiction:

ImproveSAMe levels in vivoVSAvoidformulation complexity

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The invention changes the formulation parameters by introducing gallic acid esters at specific ratios (from 5:1 to 1:400 weight ratios). This parameter modification transforms the formulation from a simple SAMe dosage form to an optimized composite that achieves sufficient in vivo SAMe levels while maintaining reasonable formulation complexity.

Inventive Principle:

Principle #35Parameter changes

3Reliability

If high doses of SAMe are administered to achieve therapeutic levels, then efficacy may be improved, but the dosage frequency and complexity increase

Engineering Contradiction:

Improvetherapeutic efficacyVSAvoiddosage frequency

Core Design Contradiction:

ReliabilityVSProductivity

Solution Approach 1:

The gallic acid ester acts as an absorption-enhancing intermediary that allows lower doses of SAMe to achieve the same therapeutic effect. This mediator effect improves the efficiency of SAMe utilization, reducing the need for frequent high-dose administration and thereby improving productivity without sacrificing efficacy.

Inventive Principle:

Principle #24Intermediary (Mediator)

Data Source

PatentUS20250275997A1Compositions Comprising S-Adenosylmethionine and a Gallic Acid Ester

Publication Date: 2025.09.04 BONAFIDE HEALTH LLC

AI summary

Provided herein are compositions and formulations comprising S-adenosyl-L-methionine (“SAM-e” or “SAMe”) and one or more gallic acid esters. Also provided herein are methods for improving the delivery of SAMe. Compositions and formulations provided herein increase SAMe plasma concentrations and area under the curve (AUC) values. Also provided herein are methods of treating a disease or disorder in a subject by administering compositions or formulations comprising exogenous SAMe and one or more gallic acid esters.