Araliadiol Stabilization via Cyclodextrin Inclusion Complex

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Solution Overview

Problem

The storage stability of araliadiol preparations is not well established, posing a challenge for their use as pharmaceuticals or functional foods.

Innovation Solution

A powdery preparation is created by mixing araliadiol with dextrin and cyclodextrin, optionally including macromolecular polysaccharides like gum arabic or gum ghatti, where cyclodextrin constitutes 20% or more of the mixture, to stabilize araliadiol, and a process involving extraction and column adsorption is used to produce this preparation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If araliadiol is stored as a pure compound or conventional preparation, then it maintains its active properties, but it deteriorates rapidly and loses stability during storage

Engineering Contradiction:
Improvestorage stabilityVSAvoidshelf life
Core Design Contradiction:
ReliabilityVSDuration of action of stationary object

Solution Approach 1:

The patent uses cyclodextrin as an intermediary substance to encapsulate araliadiol. The cyclodextrin forms an inclusion complex with araliadiol, where the hydrophobic araliadiol molecule is trapped within the hydrophobic cavity of the cyclodextrin ring structure. This mediator protects araliadiol from environmental factors such as oxidation and hydrolysis, significantly improving storage stability and extending shelf life without compromising the active compound's efficacy.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent creates a composite material system consisting of araliadiol combined with cyclodextrin and other excipients (dextrin, macromolecular polysaccharides). This composite preparation combines the therapeutic properties of araliadiol with the stabilizing properties of cyclodextrin and the protective properties of other excipients, achieving both efficacy and long-term storage stability that neither component could provide alone.

Inventive Principle:
Principle #40Composite materials

2Manufacturing precision

If araliadiol is purified to high concentration through HPLC, then it achieves therapeutic efficacy, but it becomes unstable during storage

Engineering Contradiction:
Improvepurification levelVSAvoidstorage stability
Core Design Contradiction:
Manufacturing precisionVSReliability

Solution Approach 1:

The patent applies cyclodextrin as a protective intermediary immediately after HPLC purification. The cyclodextrin encapsulation occurs in the final formulation stage, protecting the highly purified araliadiol from degradation during storage and transport, thus maintaining both the high purification level achieved through HPLC and the required storage stability.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent performs HPLC purification as a preliminary action to ensure high purity of araliadiol before formulation. The purification is completed first, then the purified araliadiol is immediately combined with cyclodextrin and other excipients to create a stable formulation, ensuring that the high purification level is maintained throughout storage.

Inventive Principle:
Principle #10Preliminary action

3Reliability

If conventional encapsulation methods are used for araliadiol, then some stability is achieved, but the stability is insufficient for long-term storage at room temperature

Engineering Contradiction:
Improvestorage stabilityVSAvoidstorage duration
Core Design Contradiction:
ReliabilityVSDuration of action of stationary object

Solution Approach 1:

The patent uses cyclodextrin as a superior intermediary compared to conventional encapsulation materials. The unique toroidal structure of cyclodextrin with its hydrophobic interior cavity provides exceptional protection for the hydrophobic araliadiol molecule, enabling long-term stability at room temperature that conventional encapsulation methods cannot achieve.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the physical-chemical parameters of the araliadiol preparation by forming an inclusion complex with cyclodextrin. This complexation alters the solubility, stability, and protective characteristics of araliadiol, transforming it from an unstable pure compound into a stable formulated preparation suitable for long-term storage at room temperature.

Inventive Principle:
Principle #35Parameter changes

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 resulting preparation achieves stable storage of araliadiol, enabling its use in pharmaceuticals and functional foods with improved cognitive function benefits and extended shelf life.

Implementation Method 1

mixing araliadiol with a specific excipient to make a powdery preparation... comprising araliadiol, dextrin and cyclodextrin

Methodology Applied
Scientific EffectInclusion complex formation: Absorption (physical)

Implementation Method 2

passing the extract obtained in the extraction step through a column packed with a hydrophobic synthetic adsorbent to adsorb araliadiol on the hydrophobic synthetic adsorbent

Methodology Applied
Scientific EffectAdsorption: Adsorption

Implementation Method 3

extracting a Gotu kola plant body with a mixture of organic solvent and water

Methodology Applied
Scientific EffectSolvent extraction: Liquid-Liquid Extraction

Implementation Method 4

further comprising a macromolecular polysaccharide... wherein the macromolecular polysaccharide is gum arabic or gum ghatti

Methodology Applied
Scientific EffectPhysical encapsulation: Physical Containment

Data Source

PatentUS20240189233A1Powdery preparation and method for manufacturing same
Publication Date: 2024.06.13 ICHIMARU PHARCOS CO LTD
  • US20240189233A1 patent drawing
  • US20240189233A1 patent drawing
  • US20240189233A1 patent drawing

AI summary

To provide a stabilized preparation for using Araliadiol as a medicine or a functional food, and a method for manufacturing the same. A powdery preparation that contains Araliadiol, dextrin and cyclodextrin. Preferably, the powdery preparation further contains a macromolecular polysaccharide.