Tigolaner Spot-On Formulation With Solketal for Transdermal Stability
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Solution Overview
Problem
Existing parasiticidal compositions for pets face challenges in meeting requirements for efficacy, safety, user convenience, and resistance to parasites, necessitating the development of novel formulations that improve activity, duration, and safety while addressing potential resistance.
Innovation Solution
A composition comprising tigolaner, optionally with praziquantel and emodepside, utilizing solvents like 1,2-isopropylideneglycerol (solketal) for transdermal application, providing broad-spectrum control over ectoparasites and endoparasites, including cestodes, trematodes, nematodes, and acantocephales, with enhanced solubility and stability through additives like BHA and lactic acid.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing parasiticidal compositions are used, then some level of parasite control is achieved, but efficacy, safety, and resistance issues persist
Solution Approach 1:
The patent combines tigolaner with praziquantel and emodepside to create a composite parasiticidal composition. This multi-component formulation addresses resistance issues by targeting parasites through multiple mechanisms simultaneously, while the specific combination enhances overall efficacy and safety profile compared to single-agent formulations.
Solution Approach 2:
The patent optimizes the concentration parameters of tigolaner (0.1-60% w/w), praziquantel (0.1-60% w/w), and emodepside (0.1-10% w/w) to achieve maximum parasite control while minimizing adverse effects. The specific ratio and concentration ranges are carefully selected to balance efficacy, safety, and resistance prevention.
2Adaptability or versatility
If broad-spectrum parasite control is achieved, then coverage of multiple parasite types is improved, but formulation complexity increases
Solution Approach 1:
The patent creates a universal composition that simultaneously controls ectoparasites (fleas, ticks, mites) and endoparasites (cestodes, trematodes, nematodes, acantocephales) using three active ingredients with complementary spectra of activity. Tigolaner targets ectoparasites and some endoparasites, praziquantel specifically targets cestodes and trematodes, and emodepside covers nematodes and acantocephales, providing comprehensive broad-spectrum protection in a single formulation.
3Ease of operation
If transdermal application is used, then user convenience is improved, but solubility and stability requirements become more stringent
Solution Approach 1:
The patent employs solketal (1,2-isopropylideneglycerol) as a key solvent and co-solvent system to facilitate transdermal delivery. This intermediary substance enables the dissolution of tigolaner, praziquantel, and emodepside at the required concentrations while maintaining stability and enabling effective transdermal penetration. The solvent system acts as a mediator between the active ingredients and the skin, ensuring both solubility and stability requirements are met for convenient topical application.
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 composition demonstrates high efficacy against a wide range of parasites, including fleas, ticks, and internal worms, with long-term protection and minimal adverse effects, suitable for spot-on application in pets.
Implementation Method 1
utilizing solvents like 1,2-isopropylideneglycerol (solketal) for transdermal application
Data Source
AI summary
The present invention relates to a composition comprising tigolaner and, optionally endoparasiticidal agents, a method for its manufacture and its use as a medicament for controlling parasites. Compositions can include tigolaner and 1,2-isopropylideneglycerol, or the composition can include praziquantel, emodepside a solvent component, and tigolaner. The composition can be used in the treatment and/or prevention of parasite infections in animals.