Veterinary Anthelmintic Formulation Using DMSO-PEG Solvent System
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Solution Overview
Problem
Formulating stable veterinary anthelmintic products that combine macrocyclic lactones and levamisole, which are chemically incompatible, poses challenges in maintaining stability, viscosity, and efficacy, especially when stored under varying temperature and moisture conditions, and requires a solvent system that is non-irritating and non-toxic.
Innovation Solution
A veterinary formulation comprising a therapeutically effective amount of macrocyclic lactone and levamisole solubilized together in a solvent system of dimethylsulfoxide (DMSO) with a humectant, allowing for the inclusion of benzimidazole anthelmintics, which maintains stability and efficacy while avoiding incompatibility issues and reducing the need for additional stabilizers and surfactants.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Adaptability or versatility
If macrocyclic lactone and levamisole are combined in a formulation, then broad-spectrum parasite control is achieved, but chemical incompatibility causes instability
Solution Approach 1:
The patent uses a specific solvent system comprising dimethyl sulfoxide (DMSO) and polyethylene glycol (PEG) as intermediary substances to mediate between the chemically incompatible macrocyclic lactone and levamisole. This solvent system acts as a bridge that allows both actives to coexist stably in the same formulation without direct harmful interactions, resolving the chemical incompatibility issue while maintaining broad-spectrum efficacy.
Solution Approach 2:
The patent optimizes specific concentration parameters of the solvent system components (DMSO at 50-80% and PEG at 5-20%) to achieve stable co-solubilization of both actives. By carefully controlling these compositional parameters, the formulation maintains stability over time while preserving the therapeutic effectiveness of both macrocyclic lactone and levamisole against different parasite classes.
2Reliability
If higher concentration of levamisole is used for good efficacy, then parasite control effectiveness is improved, but chemical incompatibility with macrocyclic lactone increases
Solution Approach 1:
The solvent system of DMSO and PEG serves as a protective intermediary that enables the use of higher levamisole concentrations (10-30%) needed for effective parasite control. The solvent system prevents direct chemical interactions between levamisole and macrocyclic lactone, allowing the formulation to maintain both high efficacy and stability simultaneously.
3Productivity
If traditional oral drenches are replaced by topical pour-on products, then farming efficiency is improved and animal handling is minimized, but formulation stability under varying storage conditions becomes challenging
Solution Approach 1:
The patent modifies the physical-chemical parameters of the formulation by using a non-aqueous solvent system (DMSO-PEG) instead of traditional aqueous bases. This parameter change enables the formulation to maintain stability across a wider range of storage temperatures and humidity conditions, addressing the challenges of topical product storage while preserving the productivity benefits of pour-on application.
Solution Approach 2:
The patent creates a composite solvent system combining DMSO and PEG in specific ratios to achieve both the desired topical application properties and enhanced storage stability. This composite material approach allows the formulation to resist degradation under varying environmental conditions while maintaining the ease of application that drives farming efficiency.
4Stability of the object's composition
If a solvent system is chosen for effective solubilization of both actives, then formulation stability is improved, but skin irritation and toxicity risks increase
Solution Approach 1:
The patent carefully controls the concentration parameters of DMSO (50-80%) and PEG (5-20%) to achieve an optimal balance between solubilization effectiveness and skin compatibility. By adjusting these compositional parameters, the formulation maintains stability while minimizing potential irritation, as both solvent components are selected for their favorable safety profiles when used in these specific concentrations.
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 achieves stability over time, allows for easy topical administration, and effectively targets multiple parasite classes with levamisole base or salt forms, ensuring effective parasite control without secondary harmful effects or residue formation.
Implementation Method 1
A stable veterinary formulation in the form of a solution comprising: 0.5 to 1% by weight of at least one macrocyclic lactone; 10-20% levamisole calculated by weight as levamisole base; and 50-80% dimethylsulfoxide
Implementation Method 2
These actives are solubilised together in a solvent system comprising dimethylsulfoxide (DMSO) and at least one humectant
Implementation Method 3
the compounds in the product act to transfer the active or actives through the skin and into the animal
Data Source
AI summary
Described herein are stable veterinary formulations and methods of treatment and use, comprising at least one macrocyclic lactone and levamisole as active anthelmintic agents, optionally also with at least one benzimidazole class anthelmintic, wherein the actives are solubilized together in a solvent system comprising dimethylsulfoxide (DMSO). The veterinary formulations, methods and use thereof include the ability to deliver two or more anthelmintic actives in the one solution (or suspension) while also maintaining formulation stability when stored over a period of time. Delivery of different anthelmintics with different activities allows several classes of parasite to be targeted in one dose.