Fluralaner Cyclodextrin Complex for Water Solubility
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Solution Overview
Problem
Existing pharmaceutical compositions of fluralaner, a water-insoluble isoxazoline compound, face challenges with stability, solubility, and segregation when used in drinking water systems for animals, requiring anhydrous forms and avoiding organic solvents to maintain effectiveness and shelf life.
Innovation Solution
A combination of fluralaner in a hydroxypropyl beta cyclodextrin complex with an anhydrous polysorbate 80 powder enhances water solubility from 20 to 30 mg/ml, providing immediate dissolution and long shelf life, suitable for various formulations including chewables and injectables for cats, dogs, and poultry.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If fluralaner is used in anhydrous form to maintain shelf life, then stability is improved, but water solubility deteriorates
Solution Approach 1:
The patent uses hydroxypropyl beta cyclodextrin as an intermediary substance that forms an inclusion complex with fluralaner. This complex acts as a mediator that allows the hydrophobic fluralaner to be solubilized in water while maintaining its stability. The cyclodextrin molecule has a hydrophobic cavity that accommodates the fluralaner molecule, while the hydrophilic exterior of the cyclodextrin complex enables water solubility.
Solution Approach 2:
The patent creates a composite material system consisting of fluralaner complexed with hydroxypropyl beta cyclodextrin. This composite approach combines the stability properties of fluralaner in its anhydrous form with the water solubility enhancement provided by the cyclodextrin carrier, resolving the contradiction between stability and solubility.
2Quantity of substance
If organic solvents are used to enhance uptake of fluralaner, then solubility is improved, but safety and shelf life deteriorate
Solution Approach 1:
The patent changes the physical-chemical parameters of the fluralaner formulation by complexing it with hydroxypropyl beta cyclodextrin. This parameter change transforms fluralaner from a water-insoluble substance to one with enhanced water solubility, eliminating the need for organic solvents while maintaining safety and effectiveness.
3Ease of operation
If fluralaner is administered through drinking water system, then ease of administration is improved, but segregation and precipitation worsen
Solution Approach 1:
The cyclodextrin complex acts as a protective intermediary that prevents fluralaner from segregating or precipitating in the drinking water system. The inclusion complex structure keeps the hydrophobic fluralaner molecule solubilized and stable in the aqueous environment, allowing easy administration through water systems without the harmful effects of segregation.
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 enhanced solubility and stability of the fluralaner complex with polysorbate 80 powder improve bioavailability, taste masking, and shelf life, enabling effective administration through drinking water or feed, while maintaining stability and preventing precipitation, thus addressing the limitations of prior art compositions.
Implementation Method 1
fluralaner in a hydroxypropyl beta cyclodextrin complex
Implementation Method 2
anhydrous polypowder (poly80 adsorbed to hydroxypropyl beta cyclodextrin (hpbcd))
Implementation Method 3
anhydrous polypowder (poly80 adsorbed to hydroxypropyl beta cyclodextrin (hpbcd))
Data Source
AI summary
A shelf stable cyclodextrin complex of an isoxazoline, wherein the cyclodextrin is 2 hydroxypropyl beta cyclodextrin and the isoxazoline is fluralaner combined with a polypowder is made and used to treat husbandry animals, cats, and/or dogs.