Citric Acid Crosslinked CMC Hydrogel for Local Constipation Relief

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Solution Overview

Problem

There is a need for new agents to treat constipation that are effective for various causes and act locally in the colon with minimal side effects, as existing treatments often have systemic side effects.

Innovation Solution

Administering a therapeutically effective amount of crosslinked carboxymethylcellulose, produced by cross-linking high viscosity carboxymethylcellulose with citric acid, in a substantially dry form, preferably combined with water, to treat constipation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Strength

If crosslinked carboxymethylcellulose is produced by conventional methods, then absorption capacity is achieved, but elasticity modulus is low

Engineering Contradiction:
Improveelasticity modulusVSAvoidabsorption capacity
Core Design Contradiction:
StrengthVSReliability

Solution Approach 1:

The patent changes the chemical parameters of crosslinking by using citric acid instead of conventional crosslinking agents, and controls the degree of crosslinking to achieve optimal balance between elasticity modulus and absorption capacity. The specific crosslinking conditions (pH, temperature, time) are optimized to maintain high absorption while improving elasticity.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite hydrogel structure by crosslinking carboxymethylcellulose with citric acid, forming a network that combines the high absorption capacity of CMC with the structural integrity provided by citric acid crosslinks, achieving both improved elasticity and maintained absorption.

Inventive Principle:
Principle #40Composite materials

2Reliability

If systemic agents are used to treat constipation, then effectiveness is improved, but side effects increase

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent extracts the therapeutic action from systemic circulation and localizes it to the colon by using a polymer that remains intact through the gastrointestinal tract and only activates in the colon, thereby achieving effective constipation treatment without systemic side effects.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The crosslinked carboxnymethylcellulose acts as an intermediary that delivers therapeutic effect locally in the colon without requiring systemic absorption, mediating between the need for effective treatment and the avoidance of systemic side effects.

Inventive Principle:
Principle #24Intermediary (Mediator)

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 crosslinked carboxymethylcellulose exhibits improved elasticity and absorption capacity, maintaining significant absorption properties while increasing elasticity, and is resistant to high ionic strength of intestinal fluid, providing effective local treatment with minimal side effects.

Implementation Method 1

crosslinking high viscosity carboxymethylcellulose with citric acid

Methodology Applied
Scientific EffectCrosslinking: Chemical Bonding

Implementation Method 2

high absorption capacity

Methodology Applied
Scientific EffectAbsorption: Absorption (physical)

Implementation Method 3

resistant to high ionic strength of intestinal fluid

Methodology Applied
Scientific EffectOsmosis: Osmosis

Implementation Method 4

heating the carboxymethylcellulose/citric acid composite at a temperature of at least about 80 °C, thereby cross-linking the carboxymethylcellulose with the citric acid

Methodology Applied
Scientific EffectThermal heating: Heating

Data Source

PatentEP3448365B1Crosslinked carboxymethylcellulose for use in the treatment of constipation
Publication Date: 2026.02.25 GELESIS SRL
  • EP3448365B1 patent drawingFigure 1
  • EP3448365B1 patent drawingFigure 2
  • EP3448365B1 patent drawingFigure 3

AI summary

The present invention provides a method of treating constipation and compositions useful in said method. The method comprises administering to a subject in need thereof an effective amount of a crosslinked carboxymethylcellulose having high elastic modulus coupled with high absorbance capacity when swollen in simulated gastric fluid/water (1:8) and simulated intestinal fluids.