Nicotinic Acid Composition for Targeted Colon Microbiota Release

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Solution Overview

Problem

Existing treatments fail to effectively influence the intestinal microbiota to positively impact diseases associated with changes in the microbiota and impaired interactions between the intestinal microbiota and the intestines, such as inflammatory bowel diseases and metabolic disorders.

Innovation Solution

A pharmaceutical composition containing nicotinic acid, nicotinamide, and/or tryptophan, designed for selective release in the terminal ileum or colon, locally influences the intestinal microbiota, altering the secretion pattern of antimicrobial peptides to reduce inflammation and modify the microbiota.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If nicotinic acid and/or nicotinamide and/or tryptophan are administered systemically, then diseases associated with changes in intestinal microbiota can be treated, but the substances are absorbed in the small intestine and do not reach the colon in sufficient amounts to effectively influence the microbiota

Engineering Contradiction:
Improveeffectiveness of microbiota modificationVSAvoidamount of active substance reaching colon
Core Design Contradiction:
ReliabilityVSLoss of substance

Solution Approach 1:

The invention divides the intestinal tract into segments (small intestine and colon) and uses different release mechanisms for different segments. The composition is designed to resist absorption in the small intestine and release specifically in the colon, ensuring the active substance reaches the target location effectively.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention uses an intermediary release mechanism (controlled release system) to transport the active substance from the small intestine to the colon without premature absorption. This intermediary system allows the substance to bypass the absorbing small intestine and release in the colon where it is needed.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Reliability

If nicotinic acid is administered to treat intestinal inflammation, then vitamin deficiency is eliminated, but systemic side effects occur and the substance does not specifically target the intestinal microbiota

Engineering Contradiction:
Improvespecificity of action on intestinal microbiotaVSAvoidsystemic side effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The invention applies local quality by designing a composition that releases the active substance specifically in the colon rather than systemically. This localized release ensures high concentration at the target site (intestinal microbiota) while minimizing systemic exposure and associated side effects.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The invention extracts the therapeutic action from the systemic circulation and concentrates it specifically in the colon. By removing the substance from general systemic distribution and delivering it directly to the intestinal microbiota, the treatment achieves specificity while reducing off-target effects.

Inventive Principle:
Principle #2Taking out (Extraction)

3Reliability

If conventional formulations are used to deliver nicotinic acid to the colon, then the substance must be administered in high doses, but this increases systemic absorption and side effects

Engineering Contradiction:
Improvedelivery efficiency to colonVSAvoidsystemic side effects from high dosing
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The invention ensures continuous and sustained release of the active substance in the colon, maintaining therapeutic levels at the target site without requiring high initial doses. This continuous local action improves delivery efficiency while avoiding the peak systemic concentrations that cause side effects.

Inventive Principle:
Principle #20Continuity of useful action

Solution Approach 2:

The invention changes the release parameters of the active substance by using a controlled release system that modifies the dissolution and absorption characteristics. This allows the substance to remain stable in the small intestine and release gradually in the colon, improving delivery efficiency without increasing systemic exposure.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentEP3831379B1A composition containing nicotinic acid and/or nicotinamide and/or tryptophan for positively influencing the intestinal microbiota
Publication Date: 2025.09.10 CONARIS RES INST
  • EP3831379B1 patent drawingFigure 1a~1e
  • EP3831379B1 patent drawingFigure 2
  • EP3831379B1 patent drawingFigure 3

AI summary

The present invention relates to a new composition containing nicotinic acid, nicotinamide, tryptophan or related compounds for positively influencing the intestinal microbiota. In certain embodiments, the pharmaceutical composition is partially or entirely released into the small intestine or large intestine.