Particle-Producing Method for Sustained Release

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Solution Overview

Problem

Existing methods for producing sustained-release particles face issues such as decreased active substance content, uneven particle size distribution, and initial burst due to water usage, wide particle size distribution, and inadequate encapsulation of active substances.

Innovation Solution

A particle-producing method and apparatus that discharge a liquid containing a physiologically active substance and a polymer through discharge holes, using volume-changing, constricted part-generating, or nozzle-vibrating devices to form droplets, which are then solidified, avoiding water usage and controlling particle size for precise sustained releasability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If spray drying method is used to produce particles, then particle production efficiency is improved, but particle size distribution becomes wide and active substance encapsulation becomes uneven

Engineering Contradiction:
Improveparticle production efficiencyVSAvoidparticle size distribution
Core Design Contradiction:
ProductivityVSManufacturing precision

Solution Approach 1:

The liquid containing active substance and polymer is segmented into individual droplets through discharge holes, with each droplet forming a separate particle. This segmentation approach ensures uniform particle size and consistent active substance encapsulation while maintaining high production efficiency through simultaneous multi-droplet discharge.

Inventive Principle:
Principle #1Segmentation

2Ease of manufacture

If water is used in particle production method, then particle formation is facilitated, but active substance content decreases due to dilution and initial burst occurs

Engineering Contradiction:
Improveparticle formation easeVSAvoidactive substance content
Core Design Contradiction:
Ease of manufactureVSQuantity of substance

Solution Approach 1:

The invention changes the liquid parameters by using non-aqueous solvents or solvent mixtures with controlled evaporation rates instead of water. This parameter change prevents active substance dilution and initial burst while still allowing proper particle formation through controlled solvent evaporation during droplet solidification.

Inventive Principle:
Principle #35Parameter changes

3Manufacturing precision

If liquid column resonance method is used for pulverization, then particle size distribution narrows, but active substance encapsulation and sustained releasability control become inadequate

Engineering Contradiction:
Improveparticle size distributionVSAvoidsustained releasability control
Core Design Contradiction:
Manufacturing precisionVSReliability

Solution Approach 1:

The active substance and polymer are thoroughly mixed and dissolved in the liquid before droplet formation, ensuring proper encapsulation is established in advance. This preliminary action guarantees that as the droplet solidifies, the active substance is uniformly distributed and properly encapsulated within the polymer matrix, enabling reliable sustained releasability control.

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 method produces particles with high active substance concentration and narrow particle size distribution, enabling precise control over sustained releasability and preventing initial bursts, improving the stability and effectiveness of pharmaceutical applications.

Implementation Method 1

a liquid-storing unit storing a liquid to be discharged, configured to discharge the liquid from discharge holes provided on the liquid-storing unit to make the liquid into droplets

Methodology Applied
Scientific EffectVolume change:

Implementation Method 2

constricted part-generating, or nozzle-vibrating devices to form droplets

Methodology Applied
Scientific EffectConstricted part generation:

Implementation Method 3

nozzle-vibrating devices to form droplets

Methodology Applied
Scientific EffectVibration: Vibration

Implementation Method 4

a solidification process of solidifying the droplets to produce a particle

Methodology Applied
Scientific EffectSolidification: Freezing

Data Source

PatentEP3524233B1Particle-producing method and particle-producing apparatus
Publication Date: 2023.08.16 RICOH CO LTD
  • EP3524233B1 patent drawingFigure 1
  • EP3524233B1 patent drawingFigure 2~3
  • EP3524233B1 patent drawingFigure 4

AI summary

A particle-producing method is provided including the processes of: discharging a liquid (14) from discharge holes provided on a liquid-storing unit (19) storing the liquid (14) to make the liquid (14) into droplets (21), the liquid (14) containing a physiologically active substance (322) and a polymer (323); and solidifying the droplets (21) into a particle (321).