Isoxazoline Injectable Formulation for Parasite Control

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Solution Overview

Problem

Current isoxazoline compounds and compositions for treating parasitic infections in animals have limitations in bioavailability, duration of efficacy, and irritation at injection sites, and lack broad spectrum coverage against ectoparasites like fleas and ticks.

Innovation Solution

Development of long-acting injectable compositions combining an isoxazoline compound with liquid polyethylene glycol (PEG) and a pharmaceutically acceptable neutral oil, optionally with a co-solvent or additive, to enhance bioavailability and reduce irritation while providing potent and sustained activity against parasites.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If isoxazoline compounds are administered as current formulations, then parasiticidal activity is achieved, but bioavailability is limited and duration of efficacy is short

Engineering Contradiction:

ImprovebioavailabilityVSAvoidduration of efficacy

Core Design Contradiction:

ReliabilityVSDuration of action of moving object

Solution Approach 1:

The patent modifies the physical and chemical parameters of the isoxazoline compound formulation by combining it with liquid PEG and neutral oil carriers, creating a long-acting injectable composition that changes the release profile and bioavailability characteristics of the active ingredient

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The invention creates a composite formulation system combining isoxazoline compound with liquid polyethylene glycol and pharmaceutically acceptable neutral oil, where the combination of these materials provides sustained release and extended duration of efficacy while improving bioavailability

Inventive Principle:

Principle #40Composite materials

2Duration of action of moving object

If isoxazoline compounds are administered at higher doses to extend duration, then duration of efficacy increases, but irritation at injection sites increases

Engineering Contradiction:

Improveduration of efficacyVSAvoidirritation at injection site

Core Design Contradiction:

Duration of action of moving objectVSObject-affected harmful factors

Solution Approach 1:

The liquid PEG and neutral oil act as intermediary carriers that facilitate the administration of isoxazoline compounds, reducing direct irritation at the injection site while enabling sustained release and extended duration of efficacy through controlled dissolution and distribution

Inventive Principle:

Principle #24Intermediary (Mediator)

3Adaptability or versatility

If current isoxazoline formulations are used, then activity against some parasites is achieved, but broad spectrum coverage against ectoparasites is lacking

Engineering Contradiction:

Improvebroad spectrum coverageVSAvoidparasiticidal activity

Core Design Contradiction:

Adaptability or versatilityVSReliability

Solution Approach 1:

The long-acting injectable composition of isoxazoline compound with liquid PEG and neutral oil provides multi-functional activity against diverse ectoparasites including fleas, ticks, and mites, achieving broad spectrum coverage while maintaining reliable parasiticidal activity through sustained release mechanism

Inventive Principle:

Principle #6Universality (Multi-functionality)

Data Source

PatentUS12083100B1Antiparasitic isoxazoline compounds, long-acting injectable formulations comprising them, methods and uses thereof

Publication Date: 2024.09.10 BOEHRINGER INGELHEIM ANIMAL HEALTH USA INC

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.