Isoxazoline Injectable Formulations for Parasite Control
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Solution Overview
Problem
Current isoxazoline compounds and compositions for treating parasitic infections in animals have limitations in efficacy, bioavailability, and duration of action, particularly in providing long-lasting protection against ectoparasites like fleas and ticks with minimal irritation at the injection site.
Innovation Solution
Development of long-acting injectable compositions comprising an isoxazoline compound, liquid polyethylene glycol (PEG), and optionally a co-solvent or neutral oil, which exhibit improved bioavailability and broad-spectrum efficacy against parasites with rapid onset and prolonged duration of action while minimizing injection site irritation.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If current isoxazoline compounds are used for treating parasitic infections, then antiparasitic efficacy is achieved, but duration of action is insufficient and injection site irritation occurs
Solution Approach 1:
The patent changes the physical and chemical parameters of the formulation by using liquid PEG as a solvent and incorporating specific co-solvents (such as ethanol, isopropanol, or oils) to optimize the solubility and release profile of the isoxazoline compound. This results in a sustained release formulation that extends duration of action while reducing local concentration peaks that cause irritation
Solution Approach 2:
The patent introduces liquid PEG and co-solvents as intermediary substances that mediate between the isoxazoline compound and the injection site. These intermediaries improve drug solubility, control release rate, and reduce direct tissue contact with the active compound, thereby extending duration of action while minimizing irritation
2Adaptability or versatility
If isoxazoline compounds are administered to provide broad-spectrum coverage, then efficacy against multiple parasites is improved, but bioavailability is limited
Solution Approach 1:
The patent optimizes formulation parameters including pH, solubility, and particle size by using liquid PEG and co-solvents to enhance the bioavailability of isoxazoline compounds. This improved bioavailability ensures reliable systemic exposure necessary for broad-spectrum antiparasitic efficacy
Solution Approach 2:
The liquid PEG and co-solvents act as intermediaries that improve the absorption and distribution of isoxazoline compounds across different parasite types. This formulation approach ensures consistent bioavailability required for reliable broad-spectrum coverage against various ectoparasites and endoparasites
3Speed
If rapid onset of action is achieved, then quick parasite control is obtained, but duration of protection is reduced
Solution Approach 1:
The patent creates a periodic release pattern where the liquid PEG formulation initially provides rapid drug release for quick onset of action, then transitions to sustained release over time. This periodic action pattern achieves both rapid initial parasite control and prolonged protection
Solution Approach 2:
The formulation exhibits dynamic release characteristics where the rate of drug release changes over time - initially rapid to achieve quick onset, then slowing to provide extended duration of protection. The liquid PEG and co-solvents enable this dynamic release profile by controlling drug solubility and diffusion rates
Data Source
AI summary
This invention relates to long-acting injectable compositions for combating parasites in animals, comprising at least one isoxazoline active agent, a liquid PEG and/or a neutral oil, optionally a co-solvent, and optionally a pharmaceutically acceptable additive or excipient. This invention also provides new isoxazoline active agents with long-lasting efficacy against ectoparasites. The invention also provides for improved methods for eradicating, controlling, and preventing parasite infections and infestations in an animal comprising administering the novel isoxazoline compounds and long-acting injectable compositions of the invention to the animal in need thereof.