Orosoluble SAMe–Probiotic Composition for Bioavailability

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Solution Overview

Problem

Existing formulations of S-adenosyl methionine (SAMe) and probiotics face stability, bioavailability, and unpleasant taste issues, leading to low adherence and effectiveness in treating mood disorders like anxiety and depression, especially in patients with comorbidities.

Innovation Solution

A combination of S-adenosyl methionine with microencapsulated Lactobacillus helveticus Rosell ®< -52 and Bifidobacterium longum Rosell ®< -175, formulated in an orosoluble solid oral form, ensuring stability and bioavailability, with magnesium oxide and vitamin B6 for synergistic effect.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If SAMe is formulated in traditional oral forms, then it can be administered orally, but it suffers from instability and poor bioavailability

Engineering Contradiction:
Improvestability and bioavailabilityVSAvoidoral administration convenience
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent changes the physical and chemical parameters of SAMe by converting it into an orosoluble salt form (such as SAMe disulfate p-toluensulfonate). This parameter change enables the compound to dissolve rapidly in oral fluids, dramatically improving bioavailability while maintaining oral administration convenience. The salt form achieves over 90% bioavailability compared to traditional forms.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent utilizes phase transition by designing an orosoluble formulation that transitions from solid state to dissolved state rapidly in the oral cavity. The orosoluble granulate form dissolves quickly in saliva, creating a supersaturated solution that enhances absorption. This phase transition approach resolves the contradiction between stability and bioavailability.

Inventive Principle:
Principle #36Phase transitions

2Reliability

If probiotics are administered in traditional formulations, then they can reach the intestine, but they lose viability due to stomach acid and have unpleasant taste

Engineering Contradiction:
Improveprobiotic viabilityVSAvoidstomach acid damage and taste issues
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent introduces an intermediary protective mechanism where probiotics are microencapsulated or incorporated into the orosoluble matrix that protects them from stomach acid. This intermediary protection allows probiotics to survive gastric conditions and reach the intestine alive, while also masking unpleasant tastes. The formulation acts as a mediator between the probiotics and the harsh gastric environment.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the environmental parameters experienced by probiotics by creating a protected microenvironment within the orosoluble formulation. This modifies pH exposure and physical conditions, allowing probiotics to maintain viability through the gastric tract despite the harsh external environment.

Inventive Principle:
Principle #35Parameter changes

3Adaptability or versatility

If multiple medications are administered for mood disorders, then treatment coverage is comprehensive, but patient adherence decreases due to complexity

Engineering Contradiction:
Improvetreatment coverageVSAvoidpatient adherence
Core Design Contradiction:
Adaptability or versatilityVSEase of operation

Solution Approach 1:

The patent merges multiple therapeutic agents (SAMe and probiotics) into a single orosoluble formulation. This combination product delivers both compounds simultaneously in one administration, maintaining comprehensive treatment coverage while simplifying the regimen to improve patient adherence. The merged formulation eliminates the need for multiple separate medications.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The orosoluble formulation serves multiple functions simultaneously: it provides rapid dissolution for bioavailability enhancement, protects probiotics from acid damage, masks unpleasant tastes, and delivers multiple active ingredients in one dose. This multi-functionality resolves the contradiction between comprehensive treatment and simple administration.

Inventive Principle:
Principle #6Universality (Multi-functionality)

4Reliability

If SAMe is used in high doses for better efficacy, then treatment effectiveness improves, but side effects increase

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent changes the delivery parameters of SAMe through orosoluble formulation, which achieves superior bioavailability (>90%). This allows lower doses to achieve the same therapeutic effect, thereby maintaining treatment effectiveness while reducing side effects. The parameter change in delivery efficiency decouples dose from effectiveness.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentEP4138828B1ORAL COMPOSITION CONTAINING S-ADENOSYLMETHIONINE (SAMe) AND A MIXTURE OF PROBIOTICS AND USE THEREOF
Publication Date: 2025.10.01 MONTEFARMACO OTC SPA

AI summary

The present invention refers to oral compositions containing S- adenosyl methionine (or S-adenosyl-l-methionine or SAMe) in combination with at least one probiotic, at least one physiologically acceptable excipient and optionally at least one additional ingredient and use thereof in the treatment and/or prevention of mood disorders preferably in case of anxiety or depression.