Inotodiol Ester Prodrug for Solubility and Intestinal Delivery

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Solution Overview

Problem

Inotodiol, a compound isolated from Inonotus obliquus, has low solubility and stability, leading to poor absorption and biological activity when administered orally, with precipitated fractions being excreted without reaching the intended intestinal regions.

Innovation Solution

Development of an ester derivative prodrug of inotodiol through ester condensation reactions with fatty acids or glucuronic acid, enhancing solubility and stability, allowing for absorption in the small intestine and release of active inotodiol in the large intestine.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If inotodiol is administered orally, then it is absorbed in the small intestine, but it precipitates and is excreted before reaching the large intestine where it would exhibit biological activity

Engineering Contradiction:

Improvebiological activityVSAvoidprecipitated inotodiol

Core Design Contradiction:

ReliabilityVSLoss of substance

Solution Approach 1:

The patent uses a prodrug formulation as an intermediary substance that carries inotodiol through the gastrointestinal tract. The prodrug is designed to be absorbed in the small intestine and then transported to the large intestine where it releases active inotodiol, preventing premature precipitation and excretion while ensuring delivery to the target region where biological activity occurs

Inventive Principle:

Principle #24Intermediary (Mediator)

2Productivity

If inotodiol is administered orally, then it reaches the intestine, but it has low solubility and stability leading to poor absorption

Engineering Contradiction:

Improveabsorption rateVSAvoidinotodiol stability

Core Design Contradiction:

ProductivityVSStability of the object's composition

Solution Approach 1:

The patent modifies the chemical parameters of inotodiol by creating a prodrug formulation with altered solubility and stability characteristics. The prodrug structure changes the physical-chemical properties to enhance dissolution and absorption in the gastrointestinal tract, while maintaining the ability to release active inotodiol at the target site

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The prodrug formulation performs preliminary solubilization and stabilization of inotodiol before it reaches the absorption site. By pre-modifying the compound's properties, the formulation ensures proper dissolution and absorption in the small intestine, preventing premature precipitation and ensuring efficient delivery to the large intestine

Inventive Principle:

Principle #10Preliminary action

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 prodrug exhibits improved solubility and stability, facilitating absorption and biological activity, enabling effective treatment of inflammatory and allergic diseases.

Implementation Method 1

the ester bond is easily decomposed into inotodiol and a fatty acid in the small intestine

Methodology Applied

Scientific EffectHydrolysis: Hydrolysis

Data Source

PatentUS12454546B2Inotodiol ester derivative precursor drug

Publication Date: 2025.10.28 CARBOEXPERT INC

AI summary

The present disclosure relates to an ester derivative prodrug of inotodiol and use thereof. The prodrug not only has increased solubility with respect to an inorganic solvent and an organic solvent, but also has improved stability, and thus can be used in the treatment of various inflammatory diseases, including inflammatory diseases or allergic diseases.