Homogeneous Veterinary Paste Formulation for Parasite Treatment

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Solution Overview

Problem

Existing veterinary anthelmintic formulations that combine praziquantel and macrolide compounds, such as avermectins and milbemycins, often result in low bioavailability due to the compounds not being dissolved in a solvent and dispersed in a carrier matrix, leading to ineffective treatment of endo- and ectoparasite infections in warm-blooded animals.

Innovation Solution

A stable oral homogeneous veterinary paste formulation is developed, comprising praziquantel and/or pyrantel, a macrolide anthelmintic compound, a solvent that dissolves both agents, and a thickening agent, along with fumed silica, PEG 400 as a viscosity modifier, and magnesium carbonate as an absorbent, to enhance bioavailability and stability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of manufacture

If anthelmintic agents are formulated as suspension in carrier matrix, then manufacturing is simplified, but bioavailability is reduced

Engineering Contradiction:
Improveformulation simplicityVSAvoidbioavailability
Core Design Contradiction:
Ease of manufactureVSReliability

Solution Approach 1:

The patent changes the physical state of the anthelmintic agents from suspended particles to dissolved state by selecting appropriate solvents. This parameter change (from solid suspension to liquid solution) dramatically improves bioavailability while maintaining paste formulation simplicity through the use of common veterinary paste carriers.

Inventive Principle:
Principle #35Parameter changes

2Adaptability or versatility

If multiple anthelmintic agents are combined in single formulation, then treatment spectrum is broadened, but formulation stability becomes problematic

Engineering Contradiction:
Improvespectrum of activityVSAvoidformulation stability
Core Design Contradiction:
Adaptability or versatilityVSStability of the object's composition

Solution Approach 1:

The patent uses solvents as intermediary substances that mediate between different anthelmintic agents with varying solubility requirements. The solvent acts as a common medium that can dissolve both praziquantel and macrolide compounds, enabling their stable coexistence in a single paste formulation without precipitation or separation.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The formulation combines multiple components (solvent, thickening agent, carrier matrix) into a composite paste system that maintains stability despite containing multiple chemically different anthelmintic agents. The composite structure provides a stable environment for both dissolved agents.

Inventive Principle:
Principle #40Composite materials

3Reliability

If anthelmintic agents are dissolved in solvent, then bioavailability is improved, but formulation complexity increases

Engineering Contradiction:
ImprovebioavailabilityVSAvoidformulation complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The selected solvent performs multiple functions simultaneously: it dissolves both praziquantel and macrolide anthelmintic agents, maintains formulation stability, and provides appropriate viscosity. This multi-functionality reduces the need for additional formulation components and simplifies the overall formulation process despite achieving dissolution of multiple agents.

Inventive Principle:
Principle #6Universality (Multi-functionality)

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 significantly improves the bioavailability of the anthelmintic agents, providing a broad spectrum of activity against parasites and enhancing the treatment efficacy for endo- and ectoparasite infections in warm-blooded animals.

Implementation Method 1

a solvent, which dissolves both the first anthelmintic agent and the macrolide anthelmintic compound

Methodology Applied
Scientific EffectDissolution: Solvation

Implementation Method 2

a thickening agent

Methodology Applied
Scientific EffectThickening:

Data Source

PatentEP1962598B1Homogeneous paste formulations
Publication Date: 2014.11.26 MERIAL LTD
  • EP1962598B1 patent drawingFigure 1
  • EP1962598B1 patent drawingFigure 2
  • EP1962598B1 patent drawing

AI summary

This invention provides for a pharmaceutical or veterinary paste formulation comprising: an effective amount of a therapeutic agent; fumed silica; an absorbent and a viscosity modifier; optionally a hydrophilic carrier and optionally, a colorant, stabilizer, surfactant, or preservative and methods of preparing these formulations. This invention also provides for, inter alia, oral homogeneous veterinary pastes for the treating, controlling and preventing of endo- and ectoparasite infections in warm-blooded animals, such as birds, horses and household pets.