Solid Delivery Composition Using Thermo-Responsive GI Gels

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Solution Overview

Problem

Existing drug delivery systems struggle to effectively target and control the release of active ingredients, such as proteins and peptides, in the gastrointestinal tract, leading to degradation and reduced efficacy due to acidic conditions and enzymatic hydrolysis, necessitating invasive administration methods.

Innovation Solution

A solid composition comprising a thermo-responsive polymer, an ion-sensitive polymer, and a lipophilic compound, which synergistically form a gel upon contact with body temperature and specific ions, creating a controlled release system that protects and delivers active substances through the gastrointestinal tract.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional drug delivery systems are used to deliver active ingredients through the gastrointestinal tract, then the administration is simple and non-invasive, but the active ingredients undergo degradation due to acidic conditions and enzymatic hydrolysis, reducing efficacy

Engineering Contradiction:
Improveefficacy of active ingredient deliveryVSAvoiddegradation from acidic conditions and enzymatic hydrolysis
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent employs a multi-layered delivery system comprising a core containing the active ingredient, surrounded by a pH-dependent membrane and a pH-independent membrane. These membrane layers act as intermediaries that protect the active ingredient from degradation in the gastrointestinal tract while controlling its release at the target site.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The delivery system utilizes a composite structure combining multiple materials with different properties: a core material for active ingredient containment, a pH-dependent membrane for gastric protection, and a pH-independent membrane for controlled release. This composite approach enables the system to withstand acidic conditions and enzymatic hydrolysis while maintaining delivery efficacy.

Inventive Principle:
Principle #40Composite materials

2Object-affected harmful factors

If targeted delivery systems with multiple protective layers are implemented, then protection from degradation is improved, but the device complexity increases

Engineering Contradiction:
Improveprotection from degradationVSAvoidcomplexity of multi-layered delivery system
Core Design Contradiction:
Object-affected harmful factorsVSDevice complexity

Solution Approach 1:

The delivery system is segmented into distinct functional layers: an inner core containing the active ingredient, a pH-dependent membrane layer for gastric protection, and a pH-independent membrane layer for controlled release. This segmentation allows each layer to perform its specific protective function independently, simplifying the design of the overall complex system.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent describes a delivery system that performs multiple functions within a single integrated structure: protecting from acidic degradation, protecting from enzymatic hydrolysis, controlling release rate, and enabling targeted delivery. By combining these functions into one universal delivery vehicle, the system reduces the need for multiple separate components, thereby managing complexity.

Inventive Principle:
Principle #6Universality (Multi-functionality)

3Duration of action of moving object

If the release rate of active ingredient is slowed down to prolong action, then duration of action is improved, but the concentration of active ingredient at the target site may be reduced

Engineering Contradiction:
Improveduration of active ingredient releaseVSAvoidconcentration of active ingredient at target site
Core Design Contradiction:
Duration of action of moving objectVSQuantity of substance

Solution Approach 1:

The delivery system utilizes pH-dependent release characteristics to create periodic or staged action patterns. The pH-independent membrane allows initial rapid release upon reaching the target pH environment, followed by sustained release over time. This periodic action pattern ensures both high initial concentration and prolonged duration of action.

Inventive Principle:
Principle #19Periodic action

Solution Approach 2:

The patent employs membranes with different pH-dependent properties to control the release parameters of the active ingredient. By changing the pH environment as the delivery system moves through the gastrointestinal tract, the system automatically adjusts its release rate, providing rapid release when needed while maintaining prolonged action, thus balancing concentration and duration.

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 composition ensures prolonged and targeted release of active substances, enhancing efficacy by protecting them from degradation and allowing for customized release profiles based on the site of action, thereby improving therapeutic outcomes.

Implementation Method 1

a thermo-responsive polymer... which synergistically form a gel upon contact with body temperature

Methodology Applied
Scientific EffectThermo-responsive sol-gel transition: Phase Change

Implementation Method 2

an ion-sensitive polymer... which synergistically form a gel upon contact with body temperature and specific ions

Methodology Applied
Scientific EffectIon-sensitive interaction: Ion Exchange

Implementation Method 3

a lipophilic compound... which synergistically form a gel upon contact with body temperature

Methodology Applied
Scientific EffectLipophilic interaction: Hydrophobe

Data Source

PatentEP3727343B1Solid delivery composition
Publication Date: 2025.10.15 COSMO TECHNOLOGIES LTD

AI summary

The present invention provides an innovative combination of biomaterials, multifunctional polymers, able to structure themselves at the site of action.The innovative combination of biomaterials of the invention is formulated in a solid composition and can be used as a versatile delivery vehicle or carrier in many pharmaceutical fields. The solid composition comprising the combination of biomaterials of the invention is provided to target delivery for medical purposes in humans.