Injectable Isoxazoline-Moxidectin Composition With Lower Injection Irritation
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Solution Overview
Problem
Existing injectable veterinary formulations face challenges in providing prolonged release of isoxazoline compounds and moxidectin with stability, ease of application, and reduced injection site irritation, while maintaining effective parasite control.
Innovation Solution
An injectable composition comprising moxidectin microspheres and isoxazoline compound particles suspended in an aqueous carrier with suspending agents, wetting agents, and preservatives, ensuring physical and chemical stability, and minimizing injection site irritation.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If isoxazoline compounds and moxidectin are combined in injectable formulations, then efficacy against parasites is improved, but injection site irritation increases
Solution Approach 1:
Poloxamers are used as intermediary substances to solubilize both isoxazoline compounds and moxidectin in aqueous carriers, reducing direct tissue contact with potentially irritating compounds while maintaining efficacy. The poloxamers act as surfactants that form micelles, allowing the active ingredients to be delivered without direct irritation to the injection site.
Solution Approach 2:
The formulation changes the physical state and solubility parameters of the active ingredients by using poloxamers to create soluble complexes. This transforms the delivery system from direct compound administration to a solubilized form, reducing local concentration spikes that cause irritation while maintaining systemic availability.
2Stability of the object's composition
If excipients are added to improve solubility and stability, then formulation stability is improved, but interference with active ingredients may occur
Solution Approach 1:
Poloxamers serve as intermediary excipients that stabilize the formulation through micelle formation without chemically interacting with or deactivating the active ingredients. Their amphiphilic structure allows them to stabilize the aqueous environment while keeping the hydrophobic active ingredients sequestered in micellar cores, preventing degradation.
Solution Approach 2:
The formulation optimizes pH, ionic strength, and temperature parameters within specific ranges to ensure stability while maintaining ingredient compatibility. These parameter controls prevent excipient-active ingredient interactions that could lead to degradation or precipitation.
3Duration of action of moving object
If prolonged release is achieved through microspheres, then duration of action is improved, but manufacturing complexity increases
Solution Approach 1:
The formulation uses segmented micellar structures formed by poloxamers to create a multi-phase system that enables prolonged release. The micelles act as nanoscale carriers that slowly release active ingredients over time, achieving extended duration without requiring complex microsphere manufacturing processes.
Solution Approach 2:
The formulation achieves prolonged release by changing the solubility and aggregation parameters of the active ingredients through poloxamer interaction. This creates a kinetic barrier to release that extends duration of action while maintaining a relatively simple liquid formulation that avoids complex microsphere manufacturing.
4Reliability
If sterilization is performed to ensure safety, then microbial contamination is reduced, but degradation of active ingredients may occur
Solution Approach 1:
The formulation includes antioxidants and chelating agents as preliminary protective measures that prevent oxidation and degradation of active ingredients before sterilization. These preliminary actions create a chemically stable environment that withstands the stress of sterilization processes without compromising ingredient integrity.
Solution Approach 2:
The formulation optimizes pH and ionic composition to create a buffer system that maintains chemical stability during sterilization. These parameter adjustments prevent hydrolysis and oxidation reactions that could occur during heat or radiation sterilization, ensuring both sterility and ingredient stability are achieved.
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 efficacy against parasites with reduced injection site irritation and maintains stability, facilitating easy administration and effective parasite control.
Implementation Method 1
The particles of the isoxazoline compound are prepared by crystallization
Implementation Method 2
spinning disk atomization
Implementation Method 3
particles of an isoxazoline compound... suspended in an aqueous carrier comprising one or more suspending agents
Implementation Method 4
one or more wetting agents
Data Source
AI summary
An injectable pharmaceutical composition comprising an isoxazoline compound of Formula (I), or a salt or N-oxide and moxidectin microspheres and a method of preventing or treating a parasite infestation using the same.