Eprinomectin Parenteral Composition Stability

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Solution Overview

Problem

Current eprinomectin formulations for veterinary use face challenges with stability, bioavailability, and the need for prolonged action, especially in lactating dairy cows, where they often require withdrawal periods due to milk residue concerns and can cause discomfort with high doses for injection.

Innovation Solution

A parenteral composition comprising eprinomectin and dimethylsulfoxide as a solvent, optionally with other excipients, which enhances stability, bioavailability, and allows for a single injection site administration without residue issues, maintaining efficacy and reducing animal discomfort.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Stability of the object's composition

If eprinomectin is formulated as a parenteral composition with dimethylsulfoxide, then stability and bioavailability are improved, but the complexity of formulation increases

Engineering Contradiction:

ImprovestabilityVSAvoidformulation complexity

Core Design Contradiction:

Stability of the object's compositionVSDevice complexity

Solution Approach 1:

Dimethylsulfoxide serves as an intermediary solvent that facilitates the dissolution and stabilization of eprinomectin in the parenteral composition, enabling improved stability and bioavailability without requiring complex formulation systems

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent modifies the physical-chemical parameters of the formulation by incorporating dimethylsulfoxide, which changes the solubility and stability characteristics of eprinomectin, allowing for improved pharmacokinetic properties

Inventive Principle:

Principle #35Parameter changes

2Reliability

If eprinomectin is administered at high doses for injection, then therapeutic efficacy is improved, but animal discomfort increases

Engineering Contradiction:

Improvetherapeutic efficacyVSAvoidanimal discomfort

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent optimizes the concentration and formulation parameters of eprinomectin to achieve effective therapeutic doses while minimizing animal discomfort through improved pharmacokinetic profiles and reduced local tissue reactions

Inventive Principle:

Principle #35Parameter changes

3Reliability

If eprinomectin formulations are used in lactating dairy cows, then parasitic control is improved, but milk residue concerns arise requiring withdrawal periods

Engineering Contradiction:

Improveparasitic controlVSAvoidmilk residue

Core Design Contradiction:

ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent modifies the pharmacokinetic parameters of eprinomectin through improved formulation, enabling effective parasitic control in lactating dairy cows while minimizing milk residue to achieve zero milk withholding period

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The formulation enables a zero milk withdrawal period, effectively making the drug residue-free enough for immediate milk production without requiring a withdrawal period, thus eliminating the harmful effect of milk residue

Inventive Principle:

Principle #27Cheap short-living objects (Disposable)

4Ease of operation

If eprinomectin is administered via pour-on method, then applicator safety is improved, but dosage precision deteriorates due to skin condition variations

Engineering Contradiction:

Improveapplicator safetyVSAvoiddosage precision

Core Design Contradiction:

Ease of operationVSManufacturing precision

Solution Approach 1:

The patent replaces the mechanical pour-on application method with a parenteral injection system, eliminating the variability introduced by skin conditions while maintaining ease of administration through standardized injection protocols

Inventive Principle:

Principle #28Mechanics substitution (Replace mechanical system)

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 eprinomectin-dimethylsulfoxide composition provides improved stability, bioavailability, and prolonged action, enabling zero milk withholding for lactating dairy cows while minimizing residue levels and injection site discomfort, effectively controlling endo- and ectoparasites with a single injection.

Implementation Method 1

A parenteral composition comprising eprinomectin and dimethylsulfoxide as a solvent

Methodology Applied

Scientific EffectSolvent dissolution: Solvation

Implementation Method 2

The pharmaceutical activity of these molecules increases the permeability of parasites muscle and nervous cells to chlorine ions, thus causing the parasite's paralysis and death. They bind to the glutamate-controlled chlorine channels of invertebrates' cells.

Methodology Applied

Scientific EffectIon channel binding:

Data Source

PatentEP3220888B1Eprinomectin parenteral compositions

Publication Date: 2021.10.27 CEVA SANTE ANIMALE SA

AI summary

The invention relates to a parenteral composition, wherein the formulation comprises eprinomectin and a vehicle comprising dimethylsulfoxide. It also relates to said composition for use in the treatment of infections caused by ectoparasites and endoparasites.