Phospholipid Foaming Agent Liquid Composition for Topical Application

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Solution Overview

Problem

The development of liquid pharmaceutical compositions that form a foam for topical application is time-consuming and often results in inhomogeneous foams due to variations in mechanical foaming techniques, making it difficult to achieve consistent foam volumes and stabilities.

Innovation Solution

A method involving a liquid composition with a phospholipid foaming agent and a pharmaceutically acceptable active agent, mechanically foamed without propellants, where the concentration of ingredients is varied to achieve specific foam volumes and stabilities using the SITA measurement method, ensuring reproducible and consistent foam production.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Manufacturing precision

If mechanical foaming techniques are varied to achieve desired foam properties, then foam volume and stability can be adjusted, but the development time increases and foam homogeneity decreases

Engineering Contradiction:
Improvefoam homogeneityVSAvoiddevelopment time
Core Design Contradiction:
Manufacturing precisionVSLoss of time

Solution Approach 1:

The invention changes the chemical composition parameters of the liquid composition, specifically incorporating phospholipids and surfactants with optimized concentrations (0.1-10% w/w phospholipids, 0.05-5% w/w surfactants) to achieve consistent foam properties without extensive mechanical parameter adjustments

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention uses composite foaming systems combining phospholipids with surfactants (ionic, nonionic, or amphoteric) to create a synergistic effect that produces homogeneous and stable foams more reliably than single-component systems, reducing development time and improving consistency

Inventive Principle:
Principle #40Composite materials

2Volume of stationary object

If mechanical foaming parameters are adjusted to achieve specific foam volumes, then foam volume can be controlled, but foam stability becomes inconsistent

Engineering Contradiction:
Improvefoam volumeVSAvoidfoam stability
Core Design Contradiction:
Volume of stationary objectVSStability of the object's composition

Solution Approach 1:

The invention optimizes chemical composition parameters including phospholipid concentration (0.1-10% w/w), surfactant concentration (0.05-5% w/w), and pH (5-8) to achieve simultaneous control of foam volume and stability, making the foam less sensitive to mechanical parameter variations

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The composite system of phospholipids combined with surfactants creates a more stable foam structure where the phospholipid head groups and surfactant molecules work synergistically to stabilize air-liquid interfaces, maintaining consistent foam stability across different foam volumes

Inventive Principle:
Principle #40Composite materials

3Ease of operation

If propellants are used to generate foam, then foam generation is easier, but the composition becomes less suitable for topical pharmaceutical application

Engineering Contradiction:
Improvefoam generationVSAvoidtopical application suitability
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The invention removes propellants from the composition entirely, relying instead on mechanical activation through pumping and mixing mechanisms to generate foam, thereby ensuring suitability for topical pharmaceutical application while maintaining ease of operation

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The invention replaces chemical propellant-driven foam generation with a mechanical foam generation system using pumps, mixers, and aerators, substituting chemical propulsion with mechanical energy input to achieve propellant-free foamable compositions

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

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

This method significantly simplifies the development process, allowing for the creation of foams with controlled volumes and stabilities, enhancing the uniform distribution and penetration of active ingredients, thereby improving the efficacy and application of pharmaceuticals.

Implementation Method 1

the liquid composition is capable of mechanically foaming without an additional propellant

Methodology Applied
Scientific EffectMechanical foaming: Foam

Implementation Method 2

a phospholipid foaming agent

Methodology Applied
Scientific EffectPhospholipid foaming: Surfactant

Data Source

PatentUS9693956B2Liquid compositions capable of foaming and including active agents, and methods for making or developing same
Publication Date: 2017.07.04 MIKA PHARMA GES FUR DIE ENTWICKLUNG & VERMARKTUNG PHARMA PROD
  • US9693956B2 patent drawing
  • US9693956B2 patent drawing
  • US9693956B2 patent drawing

AI summary

A liquid composition suitable for topical use comprising is provided that includes a phospholipid foaming agent and at least one solvent; and a pharmaceutically acceptable active agent; wherein the liquid composition is capable of mechanically foaming without an additional propellant; and wherein upon mechanical foaming of 250 ml of the liquid composition results in a foam with a foam volume of at least about 400 ml and a foam stability wherein at least about 50% of the foam volume is still present after about 5 minutes at 25° C., as determined using a SITA foam measurement. Also provided herein are methods of making disclosed compositions and methods of use.