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
Engineering 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
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.
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.
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
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.
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.
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
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.
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.
Data Source
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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.