Semi-solid Topical Composition for Acne Treatment

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Solution Overview

Problem

Current topical compositions for treating skin disorders like acne are unstable, require frequent compounding, and can be irritating, leading to compliance issues and adverse side effects due to high alcohol content and the need for refrigeration, making them difficult to store and apply effectively.

Innovation Solution

A storage-stable topical composition combining benzoyl peroxide, an antibiotic, and a retinoid, with a pH range of 3 to 8, encapsulated in a solid or semi-solid ingredient, maintaining at least 90% of the active ingredient concentration, and stable at room temperature for extended periods without refrigeration, reducing irritation and the need for frequent application.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If topical compositions contain high alcohol content to dissolve active ingredients, then solubility and homogeneity are improved, but skin irritation and drying effects worsen

Engineering Contradiction:
Improvesolubility of active ingredientsVSAvoidskin irritation
Core Design Contradiction:
Ease of operationVSObject-affected harmful factors

Solution Approach 1:

The patent changes the physical state parameter of the composition from liquid to semi-solid by incorporating petrolatum and other occlusive agents. This transformation allows the composition to maintain active ingredients without requiring high alcohol content, thereby reducing skin irritation while preserving solubility through the semi-solid matrix.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If topical compositions are formulated as stable mixtures of multiple active ingredients, then treatment effectiveness is improved, but storage stability worsens due to ingredient incompatibility

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidstorage stability
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent segments the composition into distinct functional phases within a semi-solid matrix. Benzoyl peroxide, antibiotic, and retinoid are incorporated as separate dispersed phases in the petrolatum-based continuous phase, allowing each active ingredient to maintain its stability while being delivered together topically.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent creates a composite semi-solid formulation combining petrolatum (occlusive base), microemulsion components (for drug solubilization), and suspended active ingredients. This composite structure provides both storage stability and therapeutic effectiveness by accommodating multiple incompatible active ingredients in a unified stable matrix.

Inventive Principle:
Principle #40Composite materials

3Stability of the object's composition

If topical compositions require refrigeration to maintain stability, then composition stability is improved, but ease of storage and patient compliance worsen

Engineering Contradiction:
Improvecomposition stabilityVSAvoidease of storage
Core Design Contradiction:
Stability of the object's compositionVSEase of operation

Solution Approach 1:

The patent changes the storage temperature parameter requirement by formulating a composition that is stable at room temperature. The semi-solid petrolatum-based formulation with controlled pH (3-6) and specific ingredient concentrations maintains stability without refrigeration, improving ease of storage and patient compliance.

Inventive Principle:
Principle #35Parameter changes

4Reliability

If topical compositions are applied frequently to maintain effectiveness, then treatment effectiveness is improved, but patient compliance worsens due to inconvenience

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidpatient compliance
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent achieves continuous therapeutic action through a once-daily application regimen. The semi-solid formulation provides sustained release of active ingredients throughout the day, maintaining effectiveness without requiring frequent reapplication, thereby improving patient compliance.

Inventive Principle:
Principle #20Continuity of useful action

5Reliability

If topical compositions contain benzoyl peroxide for antibacterial action, then antibacterial effectiveness is improved, but oxidation stability worsens leading to composition degradation

Engineering Contradiction:
Improveantibacterial effectivenessVSAvoidoxidation stability
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent introduces antioxidants (vitamin E, vitamin C, or vitamin A) as intermediary substances that protect benzoyl peroxide from premature oxidation and degradation. These antioxidants act as mediators between the benzoyl peroxide and environmental oxygen, maintaining antibacterial effectiveness while preventing composition degradation during storage.

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 provides improved stability, reduced irritation, and enhanced patient compliance by maintaining active ingredient potency and skin safety, allowing for once-daily application and extended storage without refrigeration, addressing the limitations of existing treatments.

Implementation Method 1

benzoyl peroxide, which exerts its antibacterial action via its potent oxidizing properties

Methodology Applied
Scientific EffectOxidation: Oxidation

Implementation Method 2

a retinoid or a pharmaceutically acceptable salt thereof in suspension

Methodology Applied
Scientific EffectSuspension: Suspension

Data Source

PatentUS9107844B2Topical skin treating compositions
Publication Date: 2015.08.18 STIEFEL LABORATORIES INC

AI summary

A topical composition and methods of using same for treating various skin disorders or conditions. In a particular aspect, these compositions comprise a storage-stable benzoyl peroxide-containing composition in suspension and an antibiotic or pharmaceutically acceptable salt or ester thereof in solution and a retinoid or a pharmaceutically acceptable salt thereof in suspension, wherein the topical composition has a final pH of about 3 to about 8. In an alternative embodiment, these compositions comprise a storage-stable mixture of a retinoid or a pharmaceutically acceptable salt thereof and either a benzoyl peroxide-containing composition or clindamycin or a pharmaceutically acceptable salt thereof.