Topical Composition with Atractylenolide and Hydroxamic Acid

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Solution Overview

Problem

Current cosmetic compositions for addressing dandruff and acne lack efficacious synergistic antimicrobial activity, with existing formulations not clearly specifying weight ratios of active ingredients like piroctone olamine and Atractylodes extracts, which limits their effectiveness.

Innovation Solution

A topical composition combining caprylhydroxamic acid or piroctone olamine with atractylenolide compounds in a weight ratio of at least 5:1, specifically using atractylenolide I or II, to enhance antimicrobial activity against Malassezia yeasts and Cutibacterium acnes, suitable for use in shampoos, body washes, and face care products.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional antimicrobial agents like piroctone olamine or zinc pyrithione are used alone, then they provide basic antimicrobial activity against Malassezia yeasts, but their efficacy is insufficient and no synergistic effect is achieved

Engineering Contradiction:
Improveantimicrobial efficacyVSAvoidsynergistic activity
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The patent combines piroctone olamine (or zinc pyrithione) with atractylenolide I or II in a specific weight ratio to create a synergistic antimicrobial composition. This merging of two different active ingredients produces an enhanced effect against Malassezia yeasts that neither ingredient achieves alone, directly resolving the contradiction between basic efficacy and synergistic activity.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The patent specifies a particular weight ratio parameter (piroctone olamine:atractylenolide I/II = 1:5 to 1:1280, preferably 1:40 to 1:100) to optimize the synergistic effect. By changing and controlling this compositional parameter, the composition achieves maximum antimicrobial efficacy while maintaining stability, thus improving reliability through parameter optimization.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If existing formulations include Atractylodes extracts without specifying weight ratios, then they may contain natural antimicrobial components, but the lack of defined ratios limits their effectiveness and reproducibility

Engineering Contradiction:
Improveantimicrobial consistencyVSAvoidweight ratio specification
Core Design Contradiction:
ReliabilityVSManufacturing precision

Solution Approach 1:

The patent transforms the undefined composition of natural Atractylodes extracts into a precisely defined formulation by specifying exact weight ratios between piroctone olamine and atractylenolide I or II (1:5 to 1:1280, preferably 1:40 to 1:100). This parameter specification ensures consistent manufacturing and reproducible antimicrobial results, resolving the contradiction between reliability and manufacturing precision.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent extracts and isolates the specific active component atractylenolide I or II from the complex Atractylodes plant material, then combines it with piroctone olamine in defined ratios. This extraction approach eliminates the variability inherent in whole plant extracts while maintaining the beneficial antimicrobial properties, achieving both consistency and precision.

Inventive Principle:
Principle #2Taking out (Extraction)

3Reliability

If higher concentrations of single antimicrobial agents are used to improve efficacy, then antimicrobial activity increases, but the risk of irritation and adverse effects increases

Engineering Contradiction:
Improveantimicrobial activityVSAvoidskin irritation
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent combines two antimicrobial agents with different mechanisms of action (piroctone olamine and atractylenolide) in a synergistic ratio, achieving enhanced antimicrobial efficacy at lower individual concentrations. This combination approach allows the composition to be more effective while reducing the concentration of each individual agent, thereby minimizing irritation and adverse effects.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The patent utilizes the synergistic interaction between two agents to convert the potential harm of high concentrations into a benefit: lower concentrations of each agent achieve the same or better effect when combined. This synergistic combination transforms what would be subtherapeutic individual doses into an highly effective composite formulation with reduced side effects.

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

Data Source

PatentEP4090311B1Topical composition comprising hydroxamic acid and atractylenolide
Publication Date: 2023.11.22 UNILEVER IP HLDG BV
  • EP4090311B1 patent drawing
  • EP4090311B1 patent drawing
  • EP4090311B1 patent drawing

AI summary

Disclosed is a topical composition comprising: (i) an antimicrobial active which is at least one of hydroxamic acids or hydroxamic acid derivatives; and (ii) an atractylenolide compound; wherein weight ratio of the amount of said atractylenolide compound to that of said antimicrobial active is at least 5:1. Also disclosed is a non-therapeutic method of providing topical antimicrobial benefit on a topical surface of a human or animal body comprising a step of applying a safe and effective amount of the topical antimicrobial composition.