Solid Veterinary Dosage Form Using Spray-Drying and Milling

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Solution Overview

Problem

Existing veterinary pharmaceutical formulations for drinking water medication face challenges such as sedimentation, stability issues, and inefficiencies due to low water solubility of antimicrobials and antiparasitic drugs, leading to ineffective dosing and potential resistance development.

Innovation Solution

Development of spray-dried solid pharmaceutical multiparticulate dosage forms comprising a non-ionic surfactant with an HLB of at least 8 and maltodextrin with a DE of at least 10, which are milled to reduce particle size and then spray-dried to create a stable, easily dispersible powder that remains stable in drinking water.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If liquid formulations are used to improve water solubility of drugs, then solubility is improved, but transportation efficiency decreases due to large amounts of liquid and non-active ingredients

Engineering Contradiction:
Improvewater solubilityVSAvoidtransportation efficiency
Core Design Contradiction:
Quantity of substanceVSProductivity

Solution Approach 1:

The patent transitions the drug formulation from liquid phase to solid phase by spray-drying the suspension to create a powder or granule. This solid formulation maintains the solubility benefits of the liquid suspension during storage but eliminates the transportation inefficiency of large liquid volumes, as only the dry powder needs to be transported and can be redispersed in water at the point of use

Inventive Principle:
Principle #36Phase transitions

2Stability of the object's composition

If solid formulations are used to improve stability and reduce transportation volume, then stability is improved, but sedimentation occurs after a certain period in drinking water

Engineering Contradiction:
Improveformulation stabilityVSAvoidsuspending ability
Core Design Contradiction:
Stability of the object's compositionVSReliability

Solution Approach 1:

The patent performs preliminary milling of the suspension before spray-drying to reduce particle size to the low micrometer range. This pre-treatment ensures that when the solid formulation is later redispersed in drinking water, the fine particles remain suspended effectively for a prolonged period without settling, thus maintaining reliability while preserving stability

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The patent changes the physical parameters of the formulation by controlling particle size through milling and using spray-drying to create a specific powder morphology. These parameter changes optimize both the stability during storage and the suspending ability in water, resolving the contradiction between the two properties

Inventive Principle:
Principle #35Parameter changes

3Ease of manufacture

If conventional spray-drying is used without proper suspension preparation, then production is simplified, but particle size increases leading to sedimentation

Engineering Contradiction:
Improveproduction simplicityVSAvoidparticle size control
Core Design Contradiction:
Ease of manufactureVSManufacturing precision

Solution Approach 1:

The patent applies preliminary milling to the suspension before spray-drying to pre-reduce particle size. This preliminary action ensures that even with a simple spray-drying process, the final particles are fine enough to prevent sedimentation, thus maintaining manufacturing precision without complicating the production process

Inventive Principle:
Principle #10Preliminary action

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 solution provides a stable and efficient delivery system that prevents sedimentation, maintains effective dosing for a longer period, and allows for use in proportioners, reducing the risk of resistance and improving animal health management.

Implementation Method 1

a non-ionic surfactant having an Hydrophilic Lipophilic Balance (HLB) of at least 8

Methodology Applied
Scientific EffectSurfactant: Surfactant

Implementation Method 2

improve the wettability of the compound

Methodology Applied
Scientific EffectWetting: Wetting

Implementation Method 3

spray-drying said milled suspension

Methodology Applied
Scientific EffectEvaporation: Evaporation

Implementation Method 4

milling said suspension

Methodology Applied
Scientific EffectMechanical Force: Mechanical Force

Data Source

PatentEP3258920B1Solid pharmaceutical dosage form suitable for use as drinking water medication
Publication Date: 2023.03.29 OROTECH NV
  • EP3258920B1 patent drawing
  • EP3258920B1 patent drawing

AI summary

The present invention relates to solid pharmaceutical dosage forms suitable for use as drinking water medication. More in particular, the present invention provides solid pharmaceutical dosage forms comprising a pharmaceutically active agent, a non-ionic surfactant having an Hydrophilic Lipophilic Balance (HLB) of at least 8, and a maltodextrin. The present invention also provides the use of such pharmaceutical dosage forms in veterinary medicine, more in particular as drinking water medication; as well as methods for preparing such pharmaceutical dosage forms.