Injectable Veterinary NSAID Formulation with Polymeric Surfactants
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Solution Overview
Problem
Conventional non-steroidal anti-inflammatory drug (NSAID) formulations for injection in veterinary medicine often cause local irritation and haemolytic side effects, and require refrigerated storage due to instability.
Innovation Solution
Formulating NSAIDs, such as carprofen, with physiologically acceptable oxygenated polymeric surfactants like polyoxypropylene/polyoxyethylene block co-polymers (poloxamers) in aqueous solutions, which are stable at room temperature and reduce side effects.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If conventional NSAID formulations are used for injection, then the drugs can be administered parenterally, but they cause local irritation and haemolytic side effects
Solution Approach 1:
The patent introduces polymeric surfactants as intermediary substances that mediate between the NSAID and the biological system. These surfactants form mixed micelles with the NSAID, allowing the drug to be administered parenterally while the surfactant layer prevents direct contact between the drug and biological tissues, thereby reducing local irritation and haemolytic side effects.
Solution Approach 2:
The patent changes the physical-chemical parameters of the NSAID formulation by incorporating polymeric surfactants. This alters the drug's solubility, surface properties, and interaction with biological systems, enabling parenteral administration while modifying the harmful effects through changed formulation parameters.
2Object-affected harmful factors
If cholanic acid/lipid formulations are used, then side effects are reduced, but the compositions require refrigerated storage due to instability at room temperature
Solution Approach 1:
The patent changes the formulation parameters by replacing cholanic acid/lipid systems with polymeric surfactant-based systems. This parameter change maintains the beneficial reduction of side effects while fundamentally altering the stability characteristics, allowing the formulation to remain stable at room temperature without requiring refrigeration.
Solution Approach 2:
The patent uses composite material systems where polymeric surfactants are combined with NSAIDs in aqueous solutions. This composite formulation achieves both reduced side effects and room temperature stability, overcoming the limitation of previous cholanic acid/lipid formulations that required refrigeration.
3Object-affected harmful factors
If cholanic acid/lipid formulations are used, then side effects are reduced, but the formulations become complex and require multiple auxiliary ingredients
Solution Approach 1:
The patent extracts and eliminates the need for cholanic acid and lipid components from the formulation. By taking out these complex auxiliary ingredients and replacing them with polymeric surfactants, the formulation maintains its ability to reduce side effects while significantly simplifying the composition and reducing the number of auxiliary ingredients required.
Solution Approach 2:
The patent employs composite material systems using polymeric surfactants that can achieve the same protective effect against side effects as complex cholanic acid/lipid formulations, but with simpler composition. The polymeric surfactant-based composite system reduces formulation complexity while maintaining therapeutic effectiveness.
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 formulation provides stable, low-side-effect injectable solutions for veterinary use, maintaining potency at room temperature and achieving bioequivalence with cholanic acid/lipid formulations while reducing the need for refrigeration and minimizing auxiliary ingredients.
Implementation Method 1
Ferro and Steffen teach the formulation of NSAIDs, by utilising salts of cholanic acid and certain lipids to form mixed micelles in aqueous systems
Implementation Method 2
the formulation of such drugs in solutions suitable for injection... to the effect that the problems of local irritancy and haemolysis associated with conventional formulations of these drugs are avoided or at least greatly reduced
Data Source
AI summary
An injectable aqueous composition for veterinary use containing a non-steroidal anti-inflammatory compound in an amount of from about 0.25 to 30% (w/v) together with a physiologically acceptable oxygenated polymeric surfactant in an amount of from about 0.5 to 20% (w/v).