Moxidectin Imidacloprid Spot-On Stabilization

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Solution Overview

Problem

Veterinary compositions containing Moxidectin and Imidacloprid have limited storage stability, requiring specific storage conditions, which complicates their handling and distribution.

Innovation Solution

Incorporating a physiologically acceptable amine base, such as triethanolamine, at low concentrations into the veterinary composition to stabilize Moxidectin against degradation, maintaining efficacy and stability without altering the desired routes of administration for both active ingredients.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If Moxidectin and Imidacloprid are combined in veterinary compositions, then broad-spectrum antiparasitic efficacy is achieved, but storage stability deteriorates requiring specific storage conditions

Engineering Contradiction:
Improveantiparasitic efficacyVSAvoidstorage stability
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent introduces an intermediary substance (antioxidant, chelating agent, or buffer) into the veterinary composition to mediate between Moxidectin and Imidacloprid, preventing their direct interaction that causes degradation. This intermediary stabilizes the formulation, allowing broad-spectrum efficacy while eliminating restrictive storage conditions.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Stability of the object's composition

If specific storage conditions are imposed on veterinary compositions, then storage stability is maintained, but handling and distribution complexity increases

Engineering Contradiction:
Improvestorage stabilityVSAvoidhandling convenience
Core Design Contradiction:
Stability of the object's compositionVSEase of operation

Solution Approach 1:

The patent converts the potentially harmful interaction between Moxidectin and Imidacloprid into a benefit by using it to identify and add stabilizing excipients. This transforms the stability problem into a solution, creating a formulation that is inherently stable under normal storage conditions, thereby improving handling convenience while maintaining stability.

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

3Reliability

If Moxidectin concentration is increased in the composition, then antiparasitic potency is improved, but degradation rate increases reducing shelf life

Engineering Contradiction:
Improveantiparasitic potencyVSAvoidshelf life
Core Design Contradiction:
ReliabilityVSDuration of action of stationary object

Solution Approach 1:

The patent changes the chemical environment parameters of the formulation by adding excipients such as antioxidants, chelating agents, or buffers. These parameter changes create a protective chemical atmosphere that allows higher Moxidectin concentrations to be maintained without increased degradation, thereby extending shelf life while preserving potency.

Inventive Principle:
Principle #35Parameter changes

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 amine base significantly improves storage stability, allowing the composition to be stored at higher temperatures without degradation, reducing the need for special storage conditions and minimizing impurities, thus enhancing the product's shelf life and usability.

Implementation Method 1

Incorporating a physiologically acceptable amine base, such as triethanolamine, at low concentrations into the veterinary composition to stabilize Moxidectin against degradation

Methodology Applied
Scientific EffectChemical stabilization:

Data Source

PatentEP3815677B1Stable veterinary composition comprising moxidectin and imidacloprid
Publication Date: 2023.08.30 KRKA D D NOVO MESTO
  • EP3815677B1 patent drawing
  • EP3815677B1 patent drawing

AI summary

The invention relates to a stabilized veterinary composition comprising Moxidectin in combination with Imidacloprid and an amine base for cutaneous topical application (spot-on), to the use of an amine base for stabilizing Moxidectin, and to the use of an amine base for producing a veterinary composition with improved Moxidectin stability.