Low Viscosity Antibiotic Composition for Mastitis Treatment

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Solution Overview

Problem

Current antibiotic compositions for treating mastitis in lactating animals face challenges with poor controlled release profiles, leading to inadequate antibiotic concentrations, increased resistance, and difficulties in manufacturing and administration due to high viscosity, which results in prolonged withholding periods and reduced milk marketability.

Innovation Solution

A low viscosity composition comprising a therapeutically effective amount of an antibiotic, hydrophobic colloidal silica, and a surfactant, which provides a controlled release profile without significantly increasing viscosity, enhancing injectability, re-dispersability, and distribution within the udder.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If high viscosity compositions are used to provide controlled release of antibiotic, then the release profile is improved, but the injectability and distribution in the udder deteriorate

Engineering Contradiction:
Improvecontrolled release profileVSAvoidinjectability
Core Design Contradiction:
Duration of action of moving objectVSEase of operation

Solution Approach 1:

The patent uses microemulsion technology to fundamentally change the physical state and viscosity parameters of the composition. By forming a microemulsion system with specific oil-water-surfactant ratios, the composition achieves low viscosity (similar to water) while maintaining controlled release properties through the microemulsion structure rather than high bulk viscosity.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite microemulsion system combining water, oil, surfactant, and antibiotic in a specific arrangement. This composite structure allows the antibiotic to be released in a controlled manner through the microemulsion matrix without requiring high overall composition viscosity, thus improving both controlled release and injectability.

Inventive Principle:
Principle #40Composite materials

2Stability of the object's composition

If high viscosity compositions are used to stabilise the suspension, then physical stability is improved, but the with-holding period is prolonged

Engineering Contradiction:
Improvephysical stabilityVSAvoidwith-holding period
Core Design Contradiction:
Stability of the object's compositionVSLoss of time

Solution Approach 1:

The patent changes the stability mechanism from relying on high viscosity to relying on microemulsion thermodynamic stability. The microemulsion system provides physical stability through its structured composition and surfactant stabilization, allowing the antibiotic to be released faster into the milk without requiring prolonged high viscosity that would extend the with-holding period.

Inventive Principle:
Principle #35Parameter changes

3Duration of action of moving object

If thickeners or excipients are added to increase viscosity, then controlled release is improved, but the manufacturing process becomes more time consuming and costly

Engineering Contradiction:
Improvecontrolled release profileVSAvoidmanufacturing process
Core Design Contradiction:
Duration of action of moving objectVSEase of manufacture

Solution Approach 1:

The patent eliminates the need for thickeners by changing to a microemulsion formulation approach. The controlled release is achieved through the microemulsion structure itself rather than through viscosity modification with additional excipients, thereby simplifying the manufacturing process and reducing costs.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The microemulsion system serves multiple functions simultaneously: it provides the vehicle for antibiotic delivery, ensures physical stability, enables controlled release, and maintains low viscosity for easy injection - all without requiring separate thickeners or multiple excipients, thus streamlining manufacturing.

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

4Duration of action of moving object

If high viscosity compositions are used, then the antibiotic release is controlled, but the milk must be withheld from the market for longer periods

Engineering Contradiction:
Improveantibiotic release controlVSAvoidmilk marketability
Core Design Contradiction:
Duration of action of moving objectVSProductivity

Solution Approach 1:

The patent changes the release mechanism from viscosity-dependent slow release to microemulsion-based controlled release. This allows the antibiotic to be released in a controlled manner that maintains therapeutic levels without requiring prolonged high viscosity in the milk, thereby reducing the with-holding period and improving milk marketability.

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 composition maintains antibiotic concentrations above the minimum inhibitory concentration for an extended period, reduces withholding periods, and simplifies manufacturing and administration, while maintaining effective treatment efficacy and milk production.

Implementation Method 1

the release rate of the active agent from the composition may be altered by the type and/or amount of surfactant and/or colloidal silica used

Methodology Applied
Scientific EffectAdsorption: Adsorption

Implementation Method 2

a base including, an amount of hydrophobic colloidal silica at least one oil; and at least one surfactant

Methodology Applied
Scientific EffectSurfactant: Surfactant

Implementation Method 3

the viscosity of the composition is below 1000 mPas at a shear rate of 100 1/s and at a temperature of 20°C

Methodology Applied
Scientific EffectViscosity:

Implementation Method 4

the hydrophobic colloidal silica and the active agent are dispersed in the oil

Methodology Applied
Scientific EffectDispersion: Dispersion (of waves)

Data Source

PatentEP2819699B2Controlled release compositions and their methods of use
Publication Date: 2024.10.16 ELANCO NEW ZEALAND
  • EP2819699B2 patent drawingFigure 1
  • EP2819699B2 patent drawingFigure 2
  • EP2819699B2 patent drawingFigure 3

AI summary

The present invention relates to a composition, the composition including a therapeutically effective amount of at least one active agent, and a base including, an amount of colloidal silica; at least one oil; and at least one surfactant, wherein the viscosity of the composition is below 1000 mPas at a shear rate of 100 1/s and at a temperature of 20°C.