Cyclodextrin-Tributyrin Inclusion Complex for Taste Masking

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Solution Overview

Problem

Tributyrin, a prodrug of butyric acid, is challenging to administer due to its unpleasant sensory qualities, such as bitterness and odor, and existing delivery methods like coated tablets and enemas are inefficient in reaching therapeutic concentrations in the gastrointestinal tract, while fermentation approaches are unpredictable and unsuitable for uniform butyrate production.

Innovation Solution

A stable inclusion complex of tributyrin with γ-cyclodextrin is formed through microencapsulation and oven drying, which masks the unpleasant taste and odor, allowing for effective oral administration and targeted delivery to the intestines.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If tributyrin is administered directly, then butyrate delivery to the intestines is achieved, but unpleasant bitterness and odor occur

Engineering Contradiction:

Improvebutyrate delivery efficacyVSAvoidsensory qualities (bitterness and odor)

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

Cyclodextrin serves as an intermediary substance that forms an inclusion complex with tributyrin. The cyclodextrin cavity encapsulates the tributyrin molecule, masking its unpleasant sensory properties while allowing controlled release in the gastrointestinal tract. This mediator approach resolves the contradiction by separating the therapeutic function from the harmful sensory effects.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The tributyrin molecule is nested within the cyclodextrin cavity structure. This host-guest inclusion complex effectively hides the tributyrin inside the cyclodextrin shell, preventing direct interaction with taste and smell receptors while maintaining the ability to release butyrate in the target location.

Inventive Principle:

Principle #7Nested doll (Nesting)

2Ease of operation

If coated tablets or enemas are used for delivery, then tributyrin administration is achieved, but therapeutic concentrations are not reached efficiently

Engineering Contradiction:

Improveadministration methodVSAvoidtherapeutic concentration achievement

Core Design Contradiction:

Ease of operationVSReliability

Solution Approach 1:

The invention changes the physical and chemical parameters of tributyrin by forming an inclusion complex with cyclodextrin. This modification alters the solubility, stability, and release characteristics of tributyrin, enabling it to achieve therapeutic concentrations in the intestines through oral administration without requiring invasive methods like enemas.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The invention replaces the mechanical delivery systems (coated tablets requiring dissolution, enemas requiring rectal administration) with a molecular-level delivery system based on host-guest inclusion complexes. The cyclodextrin-tributyrin complex provides controlled release through molecular encapsulation rather than macroscopic coating dissolution or direct rectal delivery.

Inventive Principle:

Principle #28Mechanics substitution (Replace mechanical system)

3Productivity

If fermentation approaches are used for butyrate production, then butyrate is produced, but production is unpredictable and non-uniform

Engineering Contradiction:

Improvebutyrate productionVSAvoidproduction uniformity

Core Design Contradiction:

ProductivityVSManufacturing precision

Solution Approach 1:

Instead of relying on microbial fermentation processes that vary unpredictably, the invention uses a chemically stable inclusion complex that self-regulates its release. The cyclodextrin-tributyrin complex provides consistent, predictable butyrate delivery without requiring biological systems, thereby achieving uniform production and delivery.

Inventive Principle:

Principle #25Self-service

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The cyclodextrin-tributyrin complex is gustatorily and olfactorily neutral, enabling effective butyrate release in the small and large intestines, improving intestinal health and reducing the sensory impact, thus overcoming the limitations of existing delivery methods.

Implementation Method 1

A stable inclusion complex of tributyrin with γ-cyclodextrin is formed through microencapsulation

Methodology Applied

Scientific EffectInclusion complex formation: Absorption (physical)

Implementation Method 2

oven drying, which masks the unpleasant taste and odor

Methodology Applied

Scientific EffectEvaporation: Evaporation

Data Source

PatentUS10864281B2Inclusion complexes and methods for making the same

Publication Date: 2020.12.15 THE BOARD OF TRUSTEES OF THE UNIV OF ILLINOIS

AI summary

The invention provides novel formulations comprising a stable inclusion complex of tributyrin and a cyclodextrin. In one particular embodiment, the formulation comprises an oven dried inclusion complex of tributyrin and γ-cyclodextrin that is effective in minimizing or preventing the unpleasant taste and odor of tributyrin, thus making it suitable for oral administration and delivery to the digestive tract and intestines. The invention provides compositions of these inclusion complexes and methods of using them that are advantageous as food, medicinal and other products, where the negative sensory properties of tributyrin can be a liability.