Fipronil Spot-On Formulation Preventing Crystallization
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Solution Overview
Problem
Current topical veterinary compositions for controlling ectoparasites and endoparasites often suffer from low efficacy and aesthetic concerns due to fipronil crystallization on the animal's skin and hair coat, leading to inadequate long-term protection and potential toxicity.
Innovation Solution
Development of topical formulations containing high concentrations of fipronil, combined with insect growth regulators and crystallization inhibitors, such as polyvinylpyrrolidone, to prevent fipronil crystallization and provide extended protection against ectoparasites and endoparasites.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If high concentration of fipronil is used in topical formulations, then efficacy against ectoparasites is improved, but fipronil crystallization on skin and hair coat occurs
Solution Approach 1:
The patent introduces cyclomethicone as an intermediary substance that mediates between fipronil and the skin/hair coat environment. This volatile silicone fluid acts as a carrier that prevents fipronil crystallization while maintaining high concentration (15-20% w/v) on the animal's skin and hair coat, thereby resolving the contradiction between achieving high efficacy through high concentration and preventing unwanted crystallization.
Solution Approach 2:
The patent changes the physical and chemical parameters of the formulation by incorporating cyclomethicone, which has specific properties (volatile, lipophilic) that alter how fipronil behaves on the skin and hair coat. This parameter change allows fipronil to remain in solution at high concentrations without crystallizing, as the cyclomethicone modifies the solvent environment and evaporation characteristics.
2Duration of action of stationary object
If high concentration of fipronil is used in topical formulations, then duration of protection is extended, but aesthetic appeal deteriorates due to crystallization
Solution Approach 1:
Cyclomethicone serves as a mediator that prevents direct contact between crystalline fipronil and the visible hair coat, maintaining aesthetic appearance. The volatile nature of cyclomethicone allows it to evaporate over time, leaving behind the active fipronil in a non-crystalline state that provides extended protection without visual defects.
Solution Approach 2:
The formulation ensures continuous protection by preventing crystallization that would otherwise interrupt the protective action. The cyclomethicone maintains fipronil in a soluble, active state over the protection period (up to 8 weeks), ensuring continuous efficacy while maintaining cosmetic acceptability throughout the duration.
3Loss of time
If high concentration of fipronil is used in topical formulations, then reapplication frequency is reduced, but crystallization on skin occurs
Solution Approach 1:
Cyclomethicone acts as a time-extending intermediary that prevents crystallization during the entire protection period. By maintaining fipronil in solution through the volatile silicone fluid, the formulation achieves the desired extended interval between reapplications (8 weeks or longer) without the crystallization that would normally limit the concentration and duration.
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 formulations offer superior broad-spectrum efficacy against ecto- and endoparasites for up to two months with minimal crystallization on the skin or hair coat, enhancing aesthetic appeal and reducing reapplication frequency.
Implementation Method 1
compositions comprising a high concentration of fipronil (> 10% w/v) and cyclomethicone which prevents fipronil crystallization on the animal's skin and hair coat
Implementation Method 2
The formulations offer superior broad-spectrum efficacy against ecto- and endoparasites for up to two months
Data Source
AI summary
The invention provides for spot-on formulations comprising fipronil in a high concentration for the treatment or prophylaxis of parasites of mammals and birds, and in particular, cats, dogs, horses, chickens, sheep and cattle with the aim of ridding these animals of all the parasites commonly encountered by birds and mammals. The invention also provides for effective and lasting destruction of ectoparasites, such as fleas, ticks, itch mites and lice, and of endoparasites, nematodes, such as filariae, and roundworms of the digestive tract of animals and humans.