Spot-on Parasite Formulation Using Cyclic Carbonate Solvents

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Solution Overview

Problem

Existing compositions for controlling parasites on animals using neonicotinoids and pyrethroids face challenges such as low efficacy against ticks, skin irritations, and systemic absorption due to solvents like N-methylpyrrolidone and dimethyl sulfoxide, which are toxic and cause unwanted side effects.

Innovation Solution

A composition comprising 2.5-12.5 wt.% neonicotinoids, 30.0-60.0 wt.% pyrethroids, 8.0-48.0 wt.% aliphatic cyclic carbonate, 8.0-48.0 wt.% aromatic alcohol, and sorbitan monolaurate (Span 20), which improves solubility and stability, reducing skin penetration and toxicity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If high amounts of neonicotinoids and pyrethroids are used to effectively control ticks and fleas, then parasitic insect control efficacy is improved, but skin irritations and undesired side effects occur

Engineering Contradiction:
Improveparasitic insect control efficacyVSAvoidskin irritations
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent introduces a specific formulation system comprising aliphatic cyclic carbonate, aromatic alcohol, and sorbitan monolaurate as intermediary components. This formulation system acts as a mediator between the active substances (neonicotinoids and pyrethroids) and the animal skin, enabling effective delivery of high amounts of active ingredients while reducing direct skin irritation and minimizing systemic absorption through safer dermal penetration characteristics

Inventive Principle:
Principle #24Intermediary (Mediator)

2Quantity of substance

If solvents like N-methylpyrrolidone and dimethyl sulfoxide are used to dissolve active substances, then solubility is improved, but systemic absorption and toxicity increase

Engineering Contradiction:
Improvesolubility of active substancesVSAvoidsystemic absorption
Core Design Contradiction:
Quantity of substanceVSObject-generated harmful factors

Solution Approach 1:

The patent changes the chemical parameters of the solvent system by replacing conventional solvents (N-methylpyrrolidone and dimethyl sulfoxide) with a novel combination of aliphatic cyclic carbonate, aromatic alcohol, and sorbitan monolaurate. This parameter change maintains the necessary solubility for high concentrations of neonicotinoids and pyrethroids while fundamentally altering the penetration and toxicity profile to reduce systemic absorption and associated harmful effects

Inventive Principle:
Principle #35Parameter changes

3Device complexity

If permethrin alone is used in spot-on formulations, then formulation simplicity is maintained, but activity against fleas is low

Engineering Contradiction:
Improveformulation simplicityVSAvoidactivity against fleas
Core Design Contradiction:
Device complexityVSReliability

Solution Approach 1:

The patent merges two distinct active substance classes (neonicotinoids and pyrethroids) into a single spot-on formulation, creating a synergistic combination that simultaneously addresses flea and tick control. This combination approach integrates the high flea activity of neonicotinoids with the broad-spectrum efficacy of pyrethroids, overcoming the limitations of single-active formulations while maintaining practical applicability

Inventive Principle:
Principle #5Merging (Combining)

4Reliability

If neonicotinoids alone are used in spot-on formulations, then high flea activity is achieved, but effectiveness against ticks is lost

Engineering Contradiction:
Improveactivity against fleasVSAvoideffectiveness against ticks
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent creates a universal spot-on formulation that performs multiple functions: it maintains the high flea activity provided by neonicotinoids while adding tick control capability through pyrethroids. The formulated combination enables a single application to address multiple parasitic threats (fleas and ticks), transforming a flea-specific treatment into a multi-functional parasitic control solution

Inventive Principle:
Principle #6Universality (Multi-functionality)

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 new formulation provides effective, long-term control of parasites with reduced side effects and improved skin compatibility, maintaining efficacy while minimizing systemic absorption and toxicity.

Implementation Method 1

a composition comprising 2.5-12.5 wt.% neonicotinoids, 30.0-60.0 wt.% pyrethroids, 8.0-48.0 wt.% aliphatic cyclic carbonate, 8.0-48.0 wt.% aromatic alcohol

Methodology Applied
Scientific EffectSolubility: Solvation

Implementation Method 2

sorbitan monolaurate (Span 20), which improves solubility and stability, reducing skin penetration and toxicity

Methodology Applied
Scientific EffectSurface activity: Surfactant

Data Source

PatentUS10271553B2Spot-on active substance formulation
Publication Date: 2019.04.30 EVERGREEN ANIMAL HEALTH LLC
  • US10271553B2 patent drawing
  • US10271553B2 patent drawing
  • US10271553B2 patent drawing

AI summary

The invention relates to an improved composition for the control of parasites on animals, comprising comparably high amounts of active substances from the group of agonists of the nicotinergic acetylcholine receptors of insects (neonicotinoids) and from pyrethroids in a new and improved formulation comprising an aliphatic cyclic carbonate, an aromatic alcohol, sorbitan monolaurate (Span 20) and optionally additionally further active and/or auxiliary substances. In particular, the invention relates to the use of such compositions for the control of ectoparasites such as, in particular, lice, fleas, ticks, mosquitoes and sand flies in pets such as, in particular, in dogs and ferrets.