Fluid-Jet Mill Recirculation for Drug Amorphization

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Solution Overview

Problem

Current drug/carrier co-grinding processes using air jet mills do not achieve the high-energy activation levels necessary for molecular dispersion and inclusion of drugs into carriers, leading to suboptimal biopharmaceutical properties in poorly soluble drugs.

Innovation Solution

Modifying fluid-jet mills to allow extended residence time of the drug/carrier mixture within the grinding chamber, utilizing a recirculation pipe to maintain the mixture under shock action from expanding fluid, achieving mechanochemical activation comparable to high-energy mills like ball or vibration mills.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Manufacturing precision

If conventional air jet mills are used for drug/carrier co-grinding, then the process is simple and contamination is minimized, but high-energy activation levels necessary for molecular dispersion and inclusion are not achieved

Engineering Contradiction:
Improvemolecular dispersion and inclusion qualityVSAvoidactivation energy level
Core Design Contradiction:
Manufacturing precisionVSUse of energy by moving object

Solution Approach 1:

The fluid-jet mill is pre-configured with specific nozzle arrangements and recirculation pathways to ensure that drug and carrier particles are continuously exposed to high-energy fluid shocks before the actual grinding process begins, pre-conditioning the particles for effective molecular dispersion and inclusion

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

A recirculation system is implemented where ground particles are continuously circulated back through the grinding chamber multiple times, ensuring continuous exposure to high-energy fluid shocks and maintaining sustained activation energy levels throughout the processing period

Inventive Principle:
Principle #20Continuity of useful action

2Manufacturing precision

If extended residence time is implemented in fluid-jet mills, then mechanochemical activation is achieved, but process complexity and equipment modification requirements increase

Engineering Contradiction:
Improveamorphization and nanocrystallinity qualityVSAvoidequipment modification complexity
Core Design Contradiction:
Manufacturing precisionVSDevice complexity

Solution Approach 1:

The system utilizes pneumatic recirculation pathways where pressurized gas flows carry particles through circulation loops, using fluid dynamics rather than mechanical means to achieve extended residence time and high-energy activation without complex mechanical modifications

Inventive Principle:
Principle #29Pneumatics and hydraulics

Solution Approach 2:

The process optimizes parameters such as fluid pressure, nozzle geometry, and circulation rate to achieve the desired extended residence time and activation effects, adjusting operational parameters rather than fundamentally redesigning the equipment structure

Inventive Principle:
Principle #35Parameter changes

3Manufacturing precision

If high-energy mills like ball or vibration mills are used, then mechanochemical activation is achieved, but contamination with media material and grinding chamber lining material occurs

Engineering Contradiction:
Improvemechanochemical activation qualityVSAvoidcontamination with media and lining material
Core Design Contradiction:
Manufacturing precisionVSObject-affected harmful factors

Solution Approach 1:

The patent replaces mechanical grinding systems (ball mills, vibration mills) with a fluid-jet-based system where high-velocity fluid shocks provide the necessary activation energy without physical contact between grinding media and particles, eliminating contamination from media and lining materials

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

Solution Approach 2:

A fluid medium (gas or liquid) serves as an intermediary that transfers energy to the drug and carrier particles through shock waves and turbulence, mediating the activation process without direct mechanical contact that would cause contamination

Inventive Principle:
Principle #24Intermediary (Mediator)

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

This approach results in significantly improved chemico-physical and biopharmaceutical characteristics, including high amorphization, nanocrystallinity, and enhanced solubilization kinetics of drugs, while preventing contamination and increasing co-grinding yield, thus producing better-quality drug/carrier composites.

Implementation Method 1

maintain the mixture under shock action from expanding fluid

Methodology Applied
Scientific EffectShock wave: Shock Wave

Implementation Method 2

achieve mechanochemical activation comparable to high-energy mills like ball or vibration mills

Methodology Applied
Scientific EffectMechanochemical activation:

Implementation Method 3

fluid-jet mills suitably modified to convert the co-grinding process into mechanochemical activation

Methodology Applied
Scientific EffectFluid jet: Jet

Implementation Method 4

a high percentage of amorphous phase, nanocrystallinity

Methodology Applied
Scientific EffectAmorphization:

Implementation Method 5

preparation by a high-energy co-grinding process using fluid-jet mills

Methodology Applied
Scientific EffectMechanical force: Mechanical Force

Data Source

PatentEP2806856B1Drug/carrier inclusion composites prepared by a mechanochemical activation process using high-energy fluid-jet mills
Publication Date: 2016.04.20 MICRO MACINAZIONE
  • EP2806856B1 patent drawingFigure 1
  • EP2806856B1 patent drawingFigure 2
  • EP2806856B1 patent drawingFigure 3

AI summary

Disclosed is a process for the preparation of drug/carrier inclusion composites which involves co-grinding the mixture of drug and carrier powders in a fluid-jet mill, in particular one using air or nitrogen as the fluid, which is suitably modified to allow mechanical fusion of the powders.