Dermatological Composition with PPAR-γ Activators

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Solution Overview

Problem

Current dermatological treatments for inflammatory skin diseases often rely on single active ingredients like anti-inflammatory drugs or corticoids, which can have side effects and are not effective when combined due to chemical stability and interaction issues, limiting their efficacy in addressing multiple inflammatory etiologies.

Innovation Solution

A pharmaceutical composition combining indometacin with topical antioxidants that activate PPAR-γ, such as lipoic acid, and optional corticoids or antibiotics, including manganese and pentoxifylline, to enhance anti-inflammatory effects and control inflammatory reactions, while using emollients and excipients like glycerin and propylene glycol for solubility and skin application.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Adaptability or versatility

If combinations of active ingredients are used to treat multiple inflammatory etiologies, then treatment efficacy is improved, but chemical stability and drug interactions worsen

Engineering Contradiction:
Improvetreatment efficacyVSAvoidchemical stability
Core Design Contradiction:
Adaptability or versatilityVSStability of the object's composition

Solution Approach 1:

The patent introduces a specialized vehicle system comprising a aqueous phase and an organic phase as intermediaries to facilitate the combination of multiple active ingredients. The aqueous phase contains water-soluble antioxidants and anti-inflammatories, while the organic phase contains lipophilic ingredients, with the two phases working together to maintain chemical stability and prevent harmful interactions while delivering synergistic effects.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention creates a composite pharmaceutical composition with a dual-phase structure combining aqueous and organic components. This composite system allows simultaneous incorporation of multiple active ingredients with different solubility characteristics, maintaining their individual stability while enabling synergistic interactions that enhance treatment efficacy against various inflammatory skin conditions.

Inventive Principle:
Principle #40Composite materials

2Reliability

If high doses of steroids and antibiotics are used to control inflammation and infection, then treatment effectiveness is improved, but side effects worsen

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent merges multiple active ingredients including antioxidants, anti-inflammatories, and antimicrobials into a single synergistic formulation. This combination allows the ingredients to work together at lower individual doses, achieving enhanced treatment effectiveness while reducing the cumulative side effects associated with high-dose monotherapy of steroids and antibiotics.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The invention changes the therapeutic parameters by using a multi-component active ingredient system that operates through multiple mechanisms simultaneously. This approach allows for reduced dosing of individual potent agents like steroids and antibiotics while maintaining or improving treatment effectiveness and minimizing harmful side effects through the synergistic action of multiple milder agents.

Inventive Principle:
Principle #35Parameter changes

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 achieves a synergistic anti-inflammatory effect, reducing the need for high doses of steroids and antibiotics, controlling inflammation and infection without side effects, and is adaptable to varying disease intensities by adjusting ingredient proportions.

Implementation Method 1

topical antioxidants to boost the anti-inflammatory effect by the activation of the peroxisome proliferator-activated receptor gamma (PPAR-γ)

Methodology Applied
Scientific EffectPPAR-γ activation:

Implementation Method 2

a blocking substance of tumor necrosis factor alpha (TNF-α) or other cytokines stimulant of inflammatory reactions

Methodology Applied
Scientific EffectCytokine blocking:

Implementation Method 3

The composition comprises a drug and a solvent system, wherein the solvent system comprises at least two solvent alcohols and wherein the solvent system is present in an amount sufficient to solubilize the drug

Methodology Applied
Scientific EffectSolubilization: Solvation

Implementation Method 4

topical compositions that are useful for delivering a therapeutic level of an NSAID to a target within a subject having a local inflammatory disorder

Methodology Applied
Scientific EffectTransdermal delivery: Permeation

Data Source

PatentEP2311454B1Dermatological pharmaceutical composition for the treatment of skin inflammation diseases, such as dermatitis, atopic dermatitis, vitiligo, alopecia areata, acne, psoriasis, pruritus or combinations of same
Publication Date: 2015.03.18 UMBERT MILLET IGNACIO

AI summary

The invention relates to a dermatological pharmaceutical composition for the treatment of skin inflammation diseases, such as dermatitis, atopic dermatitis, vitiligo, alopecia areata, acne, psoriasis and pruritus. The invention comprises a base anti-inflammatory agent, such as indometacin; one or more optional active ingredients selected alternatively from among at least a corticoid and an antibiotic; and a combination of topical antioxidants used to potentiate the anti-inflammatory effect, selected from among green tea, lipoic acid, curcumin, ascorbyl palmitate, Coenzyme Q10, resveratrol, Pycnogenol TM , L-camosine, taurine, vitamin E, vitamin C, papaya extract, isoflavones, manganese, lycopene and quercetin. At least one of the topical antioxidants is a peroxisome proliferator-activated receptor-gamma (PPAR-γ) activator. The invention also includes at least one antioxidant substance with an antiproliferative effect on keratonocytes, e.g. manganese, and at least one substance that blocks tumour necrosis factor-alpha (TNF-a) or other cytokines that provoke the acute phase of the inflammatory reaction, also with an antiproliferative effect, e.g. pentoxifylline.