Fipronil Parasiticidal Formulation High Flashpoint Safety

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Solution Overview

Problem

Existing Fipronil-based parasiticidal formulations have low flashpoints, posing safety risks during use, storage, and manufacture due to temperatures exceeding the flashpoint in many regions, necessitating a formulation with a higher flashpoint while maintaining parasiticidal efficacy.

Innovation Solution

A parasiticidal formulation comprising Fipronil, a C1-C6 alcohol co-solvent, an organic solvent, and a crystallization inhibitor, with specific weight percentages to achieve a flashpoint greater than 36°C, including Fipronil, ethanol, polyethylene glycol, and diethylene glycol monoethyl ether, which enhances safety without compromising efficacy.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Temperature

If conventional Fipronil formulations are used, then parasiticidal efficacy is maintained, but flashpoint remains low (36°C) causing safety risks

Engineering Contradiction:
ImproveflashpointVSAvoidsafety profile
Core Design Contradiction:
TemperatureVSReliability

Solution Approach 1:

The patent modifies the physical-chemical parameters of the formulation by replacing conventional solvents with high flashpoint solvents (ethylene glycol, propylene glycol, dipropylene glycol with flashpoints >100°C) and adjusting the solvent composition ratio. This parameter change increases the overall flashpoint of the formulation from 36°C to above 100°C while maintaining parasiticidal efficacy through proper solvent selection that preserves Fipronil's bioavailability.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite solvent system combining multiple high flashpoint solvents (ethylene glycol, propylene glycol, dipropylene glycol) rather than using a single solvent. This composite approach allows optimization of both safety (high flashpoint) and efficacy (proper solubility and delivery of Fipronil) by leveraging the complementary properties of each solvent component.

Inventive Principle:
Principle #40Composite materials

2Reliability

If flashpoint is increased to improve safety, then safety profile is improved, but formulation composition must be changed

Engineering Contradiction:
Improvesafety profileVSAvoidformulation composition
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent systematically changes the formulation composition parameters by specifying exact weight percentage ranges for each component: Fipronil (5-20%), ethylene glycol (10-40%), propylene glycol (10-40%), dipropylene glycol (10-40%), and water (5-30%). These defined parameter ranges provide a structured approach to achieving high flashpoint while maintaining simplicity in manufacturing and regulation.

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 formulation achieves a significantly higher flashpoint of 47-52°C, reducing the risk of ignitable mixtures and ensuring safer handling, storage, and use while maintaining effective parasiticidal activity against ectoparasites like ticks and fleas.

Implementation Method 1

A parasiticidal formulation comprising Fipronil, or a veterinarily acceptable derivative thereof; at least one C1-C6 alcohol co-solvent; at least one organic solvent which is not the C1-C6 alcohol co-solvent

Methodology Applied
Scientific EffectSolvation: Solvation

Implementation Method 2

at least one crystallisation inhibitor, wherein the total amount of crystallisation inhibitor is from 2 to 20% by weight of the formulation

Methodology Applied
Scientific EffectCrystallisation inhibition: Crystallisation

Data Source

PatentUS8829038B2Parasiticidal formulation
Publication Date: 2014.09.09 FIDOPHARM INC

AI summary

The present invention provides a parasiticidal formulation comprising: Fipronil, or a veterinarily acceptable derivative thereof; at least one C1-C6 alcohol co-solvent, wherein the total amount of C1-C6 alcohol is up to 8% by weight of the formulation; at least one organic solvent which is not the C1-C6 alcohol co-solvent; and at least one crystallization inhibitor, wherein the total amount of crystallization inhibitor is from 2 to 20% by weight of the formulation. The formulations of the invention have higher flash points than known parasiticidal formulations comprising Fipronil and therefore provide safer formulations for use in the home, storage, manufacture and distribution.