N-arylpyrazole and Pyrethroid Parasite Control Formulation

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Solution Overview

Problem

Existing formulations of N-arylpyrazoles and pyrethroids for controlling parasites have limitations in efficacy and safety, particularly against ticks and fleas, due to antagonistic effects from oxidative metabolism inhibitors and difficulties in application, leading to reduced duration and concentration of active compounds on animals.

Innovation Solution

A novel composition combining an N-arylpyrazole with a pyrethroid in a formulation comprising aliphatic cyclic carbonates and aliphatic cyclic or acyclic polyethers, which improves arthropodicidal efficacy and user safety by avoiding antagonistic effects, ensuring longer-lasting action and better target animal safety.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If N-arylpyrazoles are formulated with high DEE content to facilitate penetration into sebaceous glands, then the initial concentration of active compound is improved, but the duration of action is reduced due to rapid passage into circulation

Engineering Contradiction:
Improveconcentration of active compoundVSAvoidduration of availability on animal
Core Design Contradiction:
Quantity of substanceVSDuration of action of moving object

Solution Approach 1:

The patent changes the formulation parameters by replacing DEE with alternative carriers (caprylic/capric triglycerides, isopropyl myristate, polyethylene glycol derivatives) that modify the release kinetics and penetration profile of the N-arylpyrazole, achieving sustained availability without rapid systemic absorption

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent uses composite formulation systems combining multiple carrier components (triglycerides, esters, polyethylene glycol derivatives) that work synergistically to control the release and penetration of the active compound, providing both initial concentration and prolonged duration

Inventive Principle:
Principle #40Composite materials

2Reliability

If pyrethroids are combined with N-arylpyrazoles to broaden spectrum of activity, then efficacy against different parasites is improved, but antagonistic effects from oxidative metabolism inhibitors reduce overall efficacy

Engineering Contradiction:
Improveefficacy against parasitesVSAvoidantagonistic effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent extracts or removes the antagonistic component (oxidative metabolism inhibitors) from the formulation system while retaining the beneficial pyrethroid and N-arylpyrazole combination, eliminating the harmful interaction that reduced efficacy

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent converts the potential harm of combining pyrethroids with N-arylpyrazoles (which can have antagonistic effects) into a benefit by carefully selecting specific pyrethroid compounds and formulation conditions that enhance synergistic effects rather than antagonistic ones

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

3Ease of operation

If conventional formulations are used to control parasites, then application is simplified, but user safety and target animal safety are compromised

Engineering Contradiction:
Improveease of applicationVSAvoidsafety for user and target animal
Core Design Contradiction:
Ease of operationVSObject-affected harmful factors

Solution Approach 1:

The patent changes the chemical composition parameters of the formulation by using safer carrier substances (food-grade triglycerides, esters, polyethylene glycol derivatives) that reduce toxicity to users and target animals while maintaining ease of application

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS9609871B2Combination product for controlling parasites on animals
Publication Date: 2017.04.04 ELANCO ANIMAL HEALTH GMBH
  • US9609871B2 patent drawing
  • US9609871B2 patent drawing
  • US9609871B2 patent drawing

AI summary

The invention relates to novel compositions for controlling parasites on animals, comprising an N-arylpyrazole and also a pyrethroid in a formulation comprising aliphatic cyclic carbonates and aliphatic cyclic or acyclic polyethers.