Waterless Foam Composition with Modulating Agent for Active Stability

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Solution Overview

Problem

Existing waterless pharmaceutical and cosmetic compositions face challenges in stabilizing active agents due to factors like acid residues, metal ions, and oxidation, leading to instability and reduced efficacy, and there is a need for a versatile, stable, and non-irritating foam formulation that can accommodate various active ingredients.

Innovation Solution

A waterless foam composition incorporating a modulating agent, a hydrophobic or hydrophilic solvent, a stabilizing surfactant, and a polymeric agent, which adjusts the pH and stabilizes active agents, preventing reactions and breakdown, and is adaptable for different active pharmaceutical or cosmetic agents.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If ointment is used as a hydrophobic carrier for topical drug administration, then drug delivery is improved, but the composition forms an impermeable barrier that prevents removal of metabolic products and reduces drug efficacy

Engineering Contradiction:
Improvedrug delivery efficiencyVSAvoidimpermeable barrier formation
Core Design Contradiction:
ProductivityVSObject-generated harmful factors

Solution Approach 1:

The patent uses a composite system combining hydrophobic ointment base with hydrophilic microemulsion droplets. This composite structure allows the hydrophobic carrier to provide sustained drug release while the hydrophilic microemulsion domains create channels for metabolic waste removal and improve permeability, resolving the contradiction between drug delivery efficiency and barrier impermeability

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The invention introduces localized hydrophilic regions within the hydrophobic ointment matrix through microemulsion technology. These localized hydrophilic domains provide specific functions (waste removal, improved permeability) without compromising the overall hydrophobic drug delivery capability of the ointment base

Inventive Principle:
Principle #3Local quality

2Stability of the object's composition

If stabilizers, antioxidants, antimicrobials and buffers are added to protect active agents in waterless compositions, then agent stability is improved, but the formulation complexity increases

Engineering Contradiction:
Improveactive agent stabilityVSAvoidformulation complexity
Core Design Contradiction:
Stability of the object's compositionVSDevice complexity

Solution Approach 1:

The patent employs an inert microemulsion environment where the specific combination of surfactants and co-surfactants creates a protective microenvironment that inherently stabilizes active agents. This inert-like protective environment reduces the need for additional stabilizers and antioxidants, maintaining agent stability while minimizing formulation complexity

Inventive Principle:
Principle #39Inert atmosphere (Inert environment)

Solution Approach 2:

The microemulsion system provides self-stabilization through its inherent structural properties. The organized surfactant assemblies and microemulsion thermodynamic stability automatically protect active agents without requiring external stabilizing agents, achieving both stability and simplicity

Inventive Principle:
Principle #25Self-service

3Adaptability or versatility

If foam emulsion composition is changed to accommodate active ingredients, then adaptability is improved, but foam stability is reduced

Engineering Contradiction:
Improveaccommodation of active ingredientsVSAvoidfoam stability
Core Design Contradiction:
Adaptability or versatilityVSStability of the object's composition

Solution Approach 1:

The patent develops a universal microemulsion-based foam formulation platform that can accommodate various active ingredients while maintaining foam stability. The multi-functional surfactant system provides both foam stabilization and active ingredient compatibility, allowing the same base formulation to work with different APIs without compromising stability

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

Solution Approach 2:

The microemulsion acts as an intermediary system between the foam structure and active ingredients. It mediates the interaction by providing a compatible microenvironment for diverse active ingredients while the outer foam structure maintains stability, allowing adaptability without sacrificing foam integrity

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 composition ensures the chemical stability of active agents, maintains therapeutic effectiveness, and forms a stable, non-irritating foam that overcomes the limitations of traditional waterless formulations by stabilizing agents and providing a stable environmental window.

Implementation Method 1

a modulating agent, which adjusts the pH and stabilizes active agents, preventing reactions and breakdown

Methodology Applied
Scientific EffectpH adjustment:

Implementation Method 2

Some active agents are known to be generally unstable or susceptible to isomerisation or to breakdown, resulting in loss of activity and the use of stabilizers, anti oxidants antimicrobials and buffers

Methodology Applied
Scientific EffectOxidation prevention: Oxidation

Data Source

PatentUS8795693B2Compositions with modulating agents
Publication Date: 2014.08.05 VYNE THERAPEUTICS INC
  • US8795693B2 patent drawing
  • US8795693B2 patent drawing

AI summary

The present invention relates to a waterless composition and foam as a vehicle in which an active pharmaceutical or cosmetic agent, when added is stable or stabilized by or its destabilization is impeded by the presence of a modulating agent. The pharmaceutical or cosmetic composition and foam, includes: a waterless solvent, a modulating agent and one or more active pharmaceutical or cosmetic agents. The present invention also relates to a method of treatment administering the waterless composition and foam.