Injectable Microsphere Composition for Long-Acting Parasite Control
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Solution Overview
Problem
Existing injectable veterinary compositions struggle to provide long-term protection against parasites such as fleas, ticks, mites, and helminths with a single injection, while ensuring stable active ingredient content, ease of application, and minimal side effects.
Innovation Solution
An injectable veterinary composition comprising microspheres of physiologically active macrocyclic lactones and isoxazoline compounds suspended in an aqueous carrier, which allows for extended release and high bioavailability of both active agents.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If current veterinary pharmaceutical compositions are used, then they can treat parasites, but they require repeated administrations and do not provide long-term protection
Solution Approach 1:
The composition is segmented into two distinct particle types: microspheres containing macrocyclic lactone (for sustained release over months) and particles containing isoxazoline compound (for rapid initial effect). This segmentation allows each component to address different temporal needs, achieving long-term protection without requiring repeated administrations.
Solution Approach 2:
The isoxazoline compound particles provide preliminary action by rapidly killing parasites upon initial administration, while the macrocyclic lactone microspheres provide sustained prevention over subsequent months. This preliminary action eliminates the need for repeated doseings to maintain initial efficacy.
2Duration of action of moving object
If macrocyclic lactone and isoxazoline compound are combined, then long-term protection is achieved, but stability and bioavailability of active ingredients become challenging
Solution Approach 1:
By segmenting the two active ingredients into separate particle systems (microspheres for macrocyclic lactone, particles for isoxazoline), each component maintains its chemical stability independently without interfering degradation pathways. The microspheres provide controlled release protecting the macrocyclic lactone, while isoxazoline particles maintain bioavailability through their particle formulation.
Solution Approach 2:
The aqueous carrier acts as an intermediary medium that suspends both microsphere and particle formulations, enabling their co-administration while maintaining individual stability. The carrier system facilitates controlled release and prevents premature interaction between the two active ingredients that could compromise stability.
3Reliability
If high concentration of active ingredients is used, then efficacy against parasites is improved, but injection site irritation increases
Solution Approach 1:
The total antiparasitic efficacy is segmented between two active ingredients delivered via different mechanisms: isoxazoline particles provide rapid initial parasite kill, while macrocyclic lactone microspheres provide sustained lower-concentration prevention. This segmentation allows achieving high overall efficacy without requiring high local concentration at the injection site at any single time point, reducing irritation.
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 provides prolonged plasma levels of isoxazoline and macrocyclic lactones, ensuring effective parasite protection with minimal side effects and stable content, while being easy to administer and store.
Implementation Method 1
microspheres (a) and the particles of compound (b) are suspended in the aqueous carrier (c)
Implementation Method 2
The composition achieves sustained plasma levels of both moxidectin and isoxazoline compounds for extended periods
Data Source
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AI summary
The present invention relates to injectable compositions comprising the combination of an isoxazoline compound as well as a physiologically active macrocyclic lactone such as moxidectin.