Buffered Oral Protein Formulations Against Digestive Enzyme Degradation

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Solution Overview

Problem

Existing methods for orally administering protein-based active ingredients, such as insulin, are ineffective due to degradation by digestive enzymes in the stomach and intestine, necessitating parenteral administration despite efforts to develop alternative routes.

Innovation Solution

Formulating protein active ingredients in a free form with a buffer system that maintains a pH between 4 and 8, providing protection against gastric and intestinal enzymes by inhibiting pancreatic secretion and maintaining stability during gastrointestinal transit.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If protein active ingredients are administered orally in free form, then ease of operation is improved, but reliability deteriorates due to degradation by digestive enzymes

Engineering Contradiction:

Improveease of administrationVSAvoidstability against digestive enzymes

Core Design Contradiction:

Ease of operationVSReliability

Solution Approach 1:

A buffer system acts as an intermediary substance between the protein active ingredient and the digestive enzymes. The buffer maintains a specific pH range (6.5-8.5) that creates a protective environment, preventing pepsin and other gastric enzymes from degrading the protein while allowing oral administration convenience.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention changes the pH parameter of the gastrointestinal environment by introducing a buffer system. By maintaining pH between 6.5-8.5 (physiological or slightly alkaline range), the solution alters the conditions that would otherwise activate digestive enzymes, thereby protecting the protein active ingredient during oral transit.

Inventive Principle:

Principle #35Parameter changes

2Reliability

If a buffer system is added to protect protein active ingredients, then stability against digestive enzymes is improved, but device complexity increases

Engineering Contradiction:

Improvestability against digestive enzymesVSAvoidformulation complexity

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The buffer system uses common, inexpensive buffering agents that can be easily incorporated into the formulation. These are simple chemical substances (not complex devices) that perform their protective function temporarily during gastrointestinal transit, then are naturally metabolized or excreted, keeping the overall system simple and cost-effective.

Inventive Principle:

Principle #27Cheap short-living objects (Disposable)

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 buffer system effectively protects protein active ingredients from digestive enzymes, allowing for stable oral administration and maintaining bioactivity, as demonstrated by in vitro and in vivo tests.

Implementation Method 1

Methodology Applied

Scientific EffectBuffer system:

Data Source

PatentEP2234598B1Pharmaceutical compositions containing at least one proteinaceous active ingredient protected against digestive enzymes

Publication Date: 2025.11.19 BENNIS FARID

Figure 1

AI summary

The present invention relates to pharmaceutical compositions containing at least one proteinaceous active ingredient protected against digestive enzymes. Said pharmaceutical compositions contain said at least one active ingredient, in free form, and also, when they are liquid, a system capable of buffering them at a pH above 4 and below or equal to 8, or, when they are solid, a system capable of exerting, when they are placed in a liquid medium, a buffer effect between a pH above 4 and a pH below or equal to 8.