Moxidectin Topical Liquid Formulation Stability
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Solution Overview
Problem
Current moxidectin veterinary compositions are not sufficiently stable at high temperatures and humidity, and they contain high levels of impurities, which limits their effectiveness and safety for treating and preventing endo- and ectoparasites in animals.
Innovation Solution
A non-aqueous topical composition comprising moxidectin, isopropyl alcohol, a thickener, and a pharmaceutically acceptable oil, which is stable at high temperatures and humidity, has a low level of impurities, and is easier to administer than solid or injectable forms, making it suitable for treating mammals and farm animals.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If conventional moxidectin liquid compositions are used, then they are easy to administer topically, but they are not stable at high temperatures and humidity and contain high levels of impurities
Solution Approach 1:
The patent changes the chemical composition parameters by incorporating specific antioxidants (vitamin E, vitamin C, BHA, BHT) and stabilizers (alpha-tocopherol, ascorbic acid) in optimized concentrations. These parameter changes transform the formulation from an unstable conventional composition to a stable composition that maintains efficacy at high temperatures and humidity while reducing impurity formation.
Solution Approach 2:
The patent creates a composite formulation by combining moxidectin with multiple stabilizing components including polyethylene glycol, propylene glycol, vitamin E, vitamin C, and various antioxidants. This composite material approach allows the composition to benefit from the synergistic effects of multiple stabilizers, simultaneously achieving ease of topical administration and enhanced stability under challenging environmental conditions.
2Ease of operation
If conventional moxidectin liquid compositions are used, then they are easy to administer topically, but they contain high levels of impurities
Solution Approach 1:
The patent optimizes the concentration parameters of stabilizers and antioxidants in the formulation. By precisely controlling the amounts of vitamin E (0.01-5%), vitamin C (0.01-5%), and other stabilizing agents, the composition achieves reduced impurity levels while maintaining ease of topical administration. The parameter optimization prevents degradation reactions that would otherwise generate impurities.
Solution Approach 2:
The patent converts the potentially harmful effect of oxidation and degradation (which produces impurities) into a benefit by incorporating antioxidants that actively prevent these reactions. The stabilizers transform the degradation process into a protected state, reducing impurity formation while maintaining the liquid formulation's ease of administration.
3Quantity of substance
If conventional moxidectin compositions are used, then they can treat endo- and ectoparasites, but they are not stable under warm and humid conditions
Solution Approach 1:
The patent modifies the formulation parameters by incorporating temperature and humidity-resistant stabilizers. The composition includes vitamin E (0.01-5%), vitamin C (0.01-5%), and other antioxidants that specifically counteract degradation caused by heat and moisture. These parameter changes ensure the active ingredient remains stable and effective under warm and humid storage conditions while maintaining therapeutic effectiveness.
Solution Approach 2:
The patent applies beforehand cushioning by incorporating stabilizers and antioxidants that proactively protect the moxidectin from degradation before exposure to harsh conditions. The vitamin E, vitamin C, and other stabilizers are pre-added to the formulation to cushion against the harmful effects of heat and humidity, preventing impurity formation and maintaining composition stability before the product is actually used.
Data Source
AI summary
The present invention relates to topical liquid formulations comprising moxidectin, a method for their production and their use in the treatment and prevention of endoparasites and ectoparasites in animals.