DMSO-Free Fipronil Veterinary Composition

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Solution Overview

Problem

Existing veterinary compositions for treating fleas and ticks face challenges with the solubility and crystallization of N-phenylpyrazole derivatives, leading to formulation instability and potential toxicity issues when using dimethyl sulfoxide (DMSO) as a solvent.

Innovation Solution

A DMSO-free topical antiparasitic composition using fipronil as the active ingredient, combined with a glycol ether as the main solvent, a mono alkyl ester co-solvent, and a crystallization inhibitor, along with an antioxidant, to create a stable formulation that prevents crystallization and reduces toxicity by applying different active ingredients to separate spots on the animal.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If DMSO is used as a solvent for N-phenylpyrazole derivatives, then solubility is improved, but toxicity increases and formulation stability deteriorates due to crystallization

Engineering Contradiction:

Improvesolubility of N-phenylpyrazole derivativeVSAvoidtoxicity

Core Design Contradiction:

Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent removes DMSO from the formulation entirely, extracting the harmful solvent while maintaining solubility through alternative means (co-solvent system with ethanol and surfactant). This resolves the contradiction by eliminating the toxic substance while achieving the same solubility function through different mechanisms.

Inventive Principle:

Principle #2Taking out (Extraction)

Solution Approach 2:

The patent changes the formulation parameters by introducing a co-solvent system (ethanol with specific concentration ranges) and surfactant combinations, altering the chemical environment to maintain solubility without DMSO. This parameter change allows achieving solubility while avoiding toxicity.

Inventive Principle:

Principle #35Parameter changes

2Quantity of substance

If DMSO is used as a solvent, then solubility of active ingredient is improved, but formulation stability worsens due to crystallization

Engineering Contradiction:

Improvesolubility of active ingredientVSAvoidformulation stability

Core Design Contradiction:

Quantity of substanceVSStability of the object's composition

Solution Approach 1:

The patent introduces surfactants as intermediary substances that mediate between the active ingredient and the solvent system. The surfactant molecules act as intermediaries that prevent crystallization by stabilizing the active ingredient in solution, replacing DMSO's stabilizing function without its toxicity.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent creates a composite formulation system combining multiple components (ethanol, surfactants, active ingredient) that work synergistically. The composite nature of the formulation provides both solubility and stability, with the surfactant-ethanol combination preventing crystallization that would occur with simple solvent systems.

Inventive Principle:

Principle #40Composite materials

3Reliability

If multiple active ingredients are applied to the same spot, then treatment efficacy is improved, but toxicity risk increases

Engineering Contradiction:

Improvetreatment efficacyVSAvoidtoxicity risk

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent segments the application by using multiple separate spots on the animal's skin rather than concentrating all active ingredients in one location. This spatial segmentation maintains treatment efficacy through distributed delivery while reducing local toxicity risk by dispersing the concentration of active ingredients across multiple sites.

Inventive Principle:

Principle #1Segmentation

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 is stable, easy to prepare, and reduces the risk of toxicity by applying multiple active ingredients to different spots, ensuring effective treatment of fleas and ticks while maintaining formulation stability and safety.

Implementation Method 1

a crystallization inhibitor, to create a stable formulation that prevents crystallization

Methodology Applied

Scientific EffectCrystallization inhibition: Crystallisation

Implementation Method 2

combined with a glycol ether as the main solvent

Methodology Applied

Scientific EffectSolvation: Solvation

Implementation Method 3

along with an antioxidant, to create a stable formulation

Methodology Applied

Scientific EffectOxidation prevention: Oxidation

Data Source

PatentUS9034912B1Veterinary composition and method

Publication Date: 2015.05.19 BELCHER PHARMACEUTICALS LLC

AI summary

A stable liquid pharmaceutical formulation contains an N-phenylpyrazole derivative, a crystallization inhibitor/viscolizer, and a solvent/co-solvent system including a glycol ether solvent and at least one mono alkyl ester co-solvent; an improved topical veterinary applicator system; and the use of the formulation for the prevention and treatment of infestations with fleas and ticks.