Dialkyl Ether Delivery Agents for Peptide Permeability

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Solution Overview

Problem

Conventional methods for delivering biologically and chemically active agents, such as peptides and polysaccharides, face significant barriers like skin and organ membranes, acid hydrolysis, and enzymatic degradation, limiting their oral administration and absorption.

Innovation Solution

Development of dialkyl ether delivery agent compounds and their pharmaceutically acceptable salts, which form compositions with active agents to enhance permeability and stability, allowing for effective oral and other routes of administration.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional delivery methods are used for biologically active agents, then the agents can be administered, but they are rapidly degraded by acid hydrolysis and enzymes in the gastrointestinal tract

Engineering Contradiction:
Improvestability of active agentVSAvoidenzymatic degradation
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent introduces delivery agent compounds as intermediary substances that bind to biologically active agents (peptides, polysaccharides, etc.) and facilitate their transport across biological membranes. These delivery agents act as protectors during gastrointestinal transit, preventing enzymatic degradation while enabling absorption into the circulatory system.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Ease of operation

If oral delivery is attempted for macromolecular drugs, then administration is simplified, but absorption is prohibited due to size and structure

Engineering Contradiction:
Improveease of administrationVSAvoidabsorption efficiency
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The delivery agent compounds serve as intermediaries that bind to macromolecular drugs and facilitate their absorption across biological membranes. The delivery agents have appropriate size and structure that allows them to transport larger molecules through membrane barriers, overcoming the absorption prohibition while maintaining oral administration simplicity.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent modifies the physical and chemical parameters of the delivery system by introducing compounds with specific molecular weights, charges, and structural features. These parameter changes enable the delivery system to accommodate macromolecular drugs while maintaining compatibility with biological membranes for effective absorption.

Inventive Principle:
Principle #35Parameter changes

3Reliability

If adjuvants are co-administered to increase permeability, then absorption is improved, but toxic amounts of adjuvants are required

Engineering Contradiction:
ImprovepermeabilityVSAvoidtoxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The delivery agent compounds are designed as specific intermediaries that provide membrane permeabilization functionality without requiring toxic adjuvants. These compounds bind to the active agents and facilitate their passage through membranes through controlled mechanisms, achieving improved absorption while avoiding the toxicity associated with conventional adjuvant approaches.

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 dialkyl ether delivery agent compounds facilitate the absorption and bioavailability of previously challenging active agents, including peptides and polysaccharides, by overcoming biological, chemical, and physical barriers, enabling effective therapeutic delivery.

Implementation Method 1

the dialkyl ether delivery agent compounds facilitate the absorption and bioavailability of previously challenging active agents, including peptides and polysaccharides, by overcoming biological, chemical, and physical barriers

Methodology Applied
Scientific EffectPermeation: Permeation

Data Source

PatentEP2007372B1Dialkyl ether delivery agents
Publication Date: 2015.03.04 EMISPHERE TECHNOLOGIES INC
  • EP2007372B1 patent drawing
  • EP2007372B1 patent drawing
  • EP2007372B1 patent drawing

AI summary

The present invention provides dialkyl ether compounds and pharmaceutically acceptable salts thereof, compositions containing the same and one or more active agents, and methods of administering active agents with the same.