GLP-1 Peptide Granule Composition for Oral Bioavailability

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Solution Overview

Problem

The challenge in oral delivery of proteins and peptides, such as GLP-1, lies in their inability to readily cross the gastrointestinal tract membranes, leading to low bioavailability.

Innovation Solution

The use of specific granule compositions comprising a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid and GLP-1 peptide, with controlled granule design and dry granulation processes, enhances the bioavailability by ensuring simultaneous or faster release of the salt and peptide, as determined by dissolution testing.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If oral administration of GLP-1 peptide is used, then convenience of administration is improved, but bioavailability deteriorates due to inability to cross gastrointestinal tract membranes

Engineering Contradiction:

Improveconvenience of administrationVSAvoidbioavailability

Core Design Contradiction:

Ease of operationVSReliability

Solution Approach 1:

The patent uses SNAC (N-(8-(2-hydroxybenzoyl)amino)caprylic acid) as an intermediary delivery agent that facilitates the transport of GLP-1 peptide across the gastrointestinal tract membrane. SNAC acts as a carrier that enables the peptide to cross the membrane while maintaining its bioactivity, thus resolving the contradiction between oral administration convenience and bioavailability.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent creates a composite granule system combining SNAC and GLP-1 peptide in specific ratios (1:0.1 to 1:10 w/w). This composite formulation allows the peptide to be delivered orally while the SNAC component enables membrane penetration, simultaneously achieving convenience and improved bioavailability.

Inventive Principle:

Principle #40Composite materials

2Reliability

If granule design is optimized for simultaneous release, then bioavailability is improved, but manufacturing complexity increases

Engineering Contradiction:

ImprovebioavailabilityVSAvoidmanufacturing complexity

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The patent divides the formulation into separate granule types: first granules containing SNAC and second granules containing GLP-1 peptide. This segmentation allows independent optimization of each component's release characteristics while achieving simultaneous release in the gastrointestinal tract, reducing the complexity of achieving controlled release.

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The patent applies different properties to different parts of the formulation: the SNAC-containing granules are designed to dissolve rapidly to provide local concentration gradients that facilitate peptide transport. This localized optimization of release characteristics achieves improved bioavailability without requiring complex system-wide control mechanisms.

Inventive Principle:

Principle #3Local quality

Data Source

PatentUS12594326B2Compositions of GLP-1 peptides and preparation thereof

Publication Date: 2026.04.07 NOVO NORDISK AS

AI summary

The invention relates to pharmaceutical compositions comprising a first type of granules and a second type of granules, wherein said first type of granules comprises a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid and no GLP-1 peptide, and wherein said second type of granules comprises a GLP-1 peptide and no salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid, as well as the intermediate granules, processes for the preparation of the granules and compositions, and use thereof in medicine.