Water-in-oil emulsion stability using composite surfactants

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Solution Overview

Problem

Existing water-in-oil emulsions for topical use face stability issues during storage, especially with nonsteroidal anti-inflammatory agents like NSAIDs, leading to separation and instability at varying temperatures, and often employ volatile silicone derivatives or those causing unpleasant skin sensations.

Innovation Solution

A pharmaceutical composition comprising 60-80% gelled aqueous phase with NSAIDs and 20-40% fatty phase using a combination of alkyl polyglycosides and polyglycerol esters as emulsifying surfactants, ensuring stability and homogeneity at ambient and elevated temperatures for at least three months.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Adaptability or versatility

If water-in-oil emulsions are used for topical delivery of NSAIDs, then both water-soluble and liposoluble substances can be conveyed, but the emulsions exhibit stability problems during storage and cannot maintain a stable water-in-oil form

Engineering Contradiction:
Improveability to convey both water-soluble and liposoluble substancesVSAvoidstability during storage
Core Design Contradiction:
Adaptability or versatilityVSStability of the object's composition

Solution Approach 1:

The patent uses a composite emulsifying system combining two different types of surfactants (nonionic and anionic) in specific proportions. This composite approach creates synergistic effects that enhance both the stability and versatility of the water-in-oil emulsion, allowing it to maintain its structure while delivering both water-soluble and liposoluble NSAIDs effectively

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The patent optimizes specific parameters including the HLB values of surfactants (combining surfactants with complementary HLB ranges), the ratio of aqueous to fatty phase (60-80% vs 20-40%), and storage temperature conditions. These parameter adjustments enable the emulsion to maintain stability across varying temperatures while preserving its dual solubility capability

Inventive Principle:
Principle #35Parameter changes

2Stability of the object's composition

If volatile silicone derivatives are used in water-in-oil emulsions, then emulsion stability is improved, but harmful effects on the environment and users occur

Engineering Contradiction:
Improveemulsion stabilityVSAvoidharmful effects on environment and users
Core Design Contradiction:
Stability of the object's compositionVSObject-affected harmful factors

Solution Approach 1:

The patent replaces persistent volatile silicone derivatives with biodegradable, environmentally friendly surfactants that break down harmlessly after use. These alternative surfactants provide sufficient emulsion stability during the product's shelf life and application period without creating long-term environmental contamination

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

Solution Approach 2:

The patent transforms the challenge of avoiding harmful substances into an opportunity by selecting surfactants that not only eliminate environmental harm but also provide enhanced benefits such as improved skin compatibility, reduced irritation, and maintained emulsion stability through the synergistic combination of nonionic and anionic components

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

3Object-affected harmful factors

If less volatile silicone derivatives are used in water-in-oil emulsions, then environmental harm is reduced, but unpleasant sensorial properties such as sticky sensations on the skin occur

Engineering Contradiction:
Improveenvironmental harm reductionVSAvoidsensorial properties
Core Design Contradiction:
Object-affected harmful factorsVSEase of operation

Solution Approach 1:

The patent applies different functional properties to different components of the emulsion system. The nonionic surfactant component provides the sensorial benefits (lightweight feel, non-sticky texture) while the anionic surfactant component contributes to emulsion stability and skin compatibility. This local differentiation of functions allows the formulation to achieve both environmental safety and pleasant application characteristics

Inventive Principle:
Principle #3Local quality

4Ease of manufacture

If conventional emulsifying systems are used in water-in-oil emulsions with NSAIDs, then manufacturing is simplified, but the emulsions separate and become unstable at varying temperatures

Engineering Contradiction:
Improvemanufacturing simplicityVSAvoidtemperature stability
Core Design Contradiction:
Ease of manufactureVSStability of the object's composition

Solution Approach 1:

The patent creates a dynamic emulsifying system that adapts to temperature variations. The combination of nonionic and anionic surfactants with complementary temperature profiles allows the emulsion to maintain its water-in-oil structure across a wide temperature range (4°C to 40°C). The system dynamically adjusts its interfacial properties in response to temperature changes, preventing separation while maintaining manufacturability

Inventive Principle:
Principle #15Dynamics

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 maintains a stable water-in-oil form, preventing separation and skin irritation, while ensuring effective delivery of anti-inflammatory agents, enhancing therapeutic efficacy and patient comfort.

Implementation Method 1

a pharmaceutical composition for topical use which is in the form of an emulsion of water-in-oil type

Methodology Applied
Scientific EffectEmulsion: Emulsion

Implementation Method 2

an emulsifying system comprising a combination of at least one emulsifying surfactant (S1) selected from the elements of the group consisting of compositions of alkyl polyglycosides, and compositions of alkyl polyglycosides and of fatty alcohols, and of at least one emulsifying surfactant (S2) selected from the elements of the group consisting of polyglycerol esters

Methodology Applied
Scientific EffectSurfactant: Surfactant

Data Source

PatentUS20220023208A1Pharmaceutical composition for topical use comprising at least one antiinflammatory substance
Publication Date: 2022.01.27 SOC DEXPLOITATION DE PROD POUR LES IND CHEM SEPPIC
  • US20220023208A1 patent drawing
  • US20220023208A1 patent drawing
  • US20220023208A1 patent drawing

AI summary

A pharmaceutical composition for topical use which is in the form of a water-in-oil emulsion including, for 100% of the weight thereof: —from 60% to 80% by weight of a gelled aqueous phase including an anti-inflammatory substance, —from 20% to 40% by weight of a fatty phase including at least one oil and an emulsifying system including a combination of at least one emulsifying surfactant selected from the elements of the group consisting of alkylpolyglycoside compositions and alkylpolyglycoside and fatty alcohol compositions, and of at least one emulsifying surfactant selected from the elements of the group consisting of polyglycerol esters, alkoxylated polyglycerol esters, polyglycol polyhydroxystearates, polyglycerol polyhydroxystearates and alkoxylated polyglycerol polyhydroxystearates.