Sodium Alginate Gel Barrier Stabilizes Oral Peptide Drugs

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current pharmaceutical preparations for oral treatment of inflammatory gastrointestinal diseases often fail to effectively address the underlying pathogenesis and regeneration processes in the gastrointestinal tract, leading to inadequate healing and increased risk of polymorbidity, especially in seniors, due to instability of short peptides in gastric enzymes and secondary acid formation from carbonate-based medications.

Innovation Solution

A pharmaceutical preparation comprising sodium alginate, dipeptide α-glutamyl-tryptophan (Glu-Trp) monosodium salt, and water, formulated to provide gastroprotective and hepatoprotective effects by stabilizing the gastric environment and enhancing mucosal regeneration, with a specific ratio of ingredients that prevent ulcer formation and improve immune response.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Object-affected harmful factors

If potassium hydrogen carbonate is added to regulate gastric acidity, then the acidity of gastric juice is reduced, but secondary acid formation occurs which is even stronger and can lead to heartburn and esophagitis

Engineering Contradiction:
Improvegastric acidityVSAvoidsecondary acid formation
Core Design Contradiction:
Object-affected harmful factorsVSObject-generated harmful factors

Solution Approach 1:

The patent removes potassium hydrogen carbonate from the formulation entirely, replacing it with sodium alginate and dipeptide α-glutamyl-tryptophan monosodium salt. This extraction of the problematic carbonate component eliminates the secondary acid formation mechanism while maintaining gastroprotective effects through alternative mechanisms.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

Sodium alginate acts as an intermediary substance that forms a protective gel barrier in the stomach, mediating between the gastric environment and the mucosal tissue. This gel barrier provides buffering capacity without triggering the carbonate-bicarbonate cycle that leads to rebound hyperacidity.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Ease of operation

If short peptides such as alpha-glutamyl-tryptophan dipeptide are administered orally, then enteral administration is convenient, but the peptides are unstable in gastric and small intestinal enzymes and break down into individual amino acids

Engineering Contradiction:
Improveenteral administrationVSAvoidpeptide stability
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent changes the chemical parameters of the peptide by converting it to its monosodium salt form (α-glutamyl-tryptophan monosodium salt). This parameter change increases the peptide's stability in the gastrointestinal environment while maintaining its biological activity and immunomodulatory effects.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The formulation creates a composite system combining sodium alginate with the dipeptide monosodium salt. The sodium alginate matrix provides a protective environment that enhances the stability of the peptide against enzymatic degradation while allowing controlled release and absorption.

Inventive Principle:
Principle #40Composite materials

3Device complexity

If conventional pharmaceutical preparations are used for oral treatment, then the treatment approach is simple, but they fail to effectively address the underlying pathogenesis and regeneration processes in the gastrointestinal tract

Engineering Contradiction:
Improvetreatment formulationVSAvoidhealing effectiveness
Core Design Contradiction:
Device complexityVSReliability

Solution Approach 1:

The patent creates a multi-functional formulation where sodium alginate provides mucosal protection and buffering, while the dipeptide α-glutamyl-tryptophan monosodium salt provides immunomodulatory and regenerative effects. This combination addresses multiple aspects of gastrointestinal pathology simultaneously, including inflammation, regeneration, and acid regulation.

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

Solution Approach 2:

The formulation merges two previously separate therapeutic approaches: the gastroprotective properties of sodium alginate and the immunomodulatory effects of the dipeptide. By combining these substances in a single oral preparation, the patent achieves synergistic effects that enhance overall healing effectiveness.

Inventive Principle:
Principle #5Merging (Combining)

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 preparation demonstrates significant gastroprotective and hepatoprotective activities by reducing ulcer formation, improving body weight, and normalizing liver and pancreatic functions, with a safe and effective reduction in the severity of gastrointestinal and pancreatic damage, as evidenced by experimental and clinical studies.

Implementation Method 1

sodium alginate, a functional additive and water for the oral treatment of inflammatory gastrointestinal diseases

Methodology Applied
Scientific EffectGel formation: Gel

Implementation Method 2

regulate the acidity of the gastric juice

Methodology Applied
Scientific EffectBuffering:

Implementation Method 3

thymogen (alpha-glutamyl tryptophan) has the ability to regulate the acidity of gastric juice

Methodology Applied
Scientific EffectAcidity regulation:

Implementation Method 4

the modulating influence of synthetic glycamyl-tryptophan dipeptide (thymogen) on the non-specific immune defense

Methodology Applied
Scientific EffectImmunomodulation:

Implementation Method 5

formulated to provide gastroprotective and hepatoprotective effects by stabilizing the gastric environment and enhancing mucosal regeneration

Methodology Applied
Scientific EffectMucosal protection:

Implementation Method 6

with a specific ratio of ingredients that prevent ulcer formation

Methodology Applied
Scientific EffectUlcer prevention:

Data Source

PatentEP2767286B1Oral pharmaceutical composition for the treatment of inflammatory gastrointestinal diseases
Publication Date: 2018.01.17 OBSHESTVO S OGRANICHENNOJ OTVETABTVENNOSTJU CITONIR

AI summary

The invention relates to a peptide drug for oral administration. The pharmaceutical preparation in gel form contains sodium alginate, a functional additive, and water. The functional additive in the preparation is 0.07–0.13 mg of α-glutamyl-tryptophan dipeptide in the form of its monosodium salt per 10 ml dose. The sodium alginate content per dose of the preparation is 200–300 mg. This results in increased efficacy of the preparation in the treatment of inflammatory gastrointestinal diseases.