Spherical Granule Coating with Surfactant Suspension Stabilization

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Solution Overview

Problem

The production of spherical base granules containing hardly water-soluble drugs faces challenges with foaming and precipitation in layering liquids, leading to instability and reduced recovery ratios due to high shear forces, which complicates the coating process and results in agglomeration.

Innovation Solution

Incorporating micronized microcrystalline cellulose and polyoxyethylene hydrogenated castor oil as an emulsifier in the layering liquid improves suspension stability and suppresses foaming, allowing for stable coating without additional pulverization treatments.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If a hardly water-soluble drug is added to a layering liquid, then the drug can be coated onto spherical core particles, but vigorous foaming occurs and suspension stability deteriorates

Engineering Contradiction:
Improvecoating process reliabilityVSAvoidfoaming and suspension instability
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

A nonionic surfactant is introduced as an intermediary substance to mediate between the hardly water-soluble drug particles and the aqueous layering liquid. The surfactant reduces surface tension and prevents foaming while maintaining drug particle suspension stability, enabling successful coating without the harmful foaming effect

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The physical and chemical parameters of the layering liquid are modified by adjusting surfactant concentration, pH value, and ionic strength. These parameter changes optimize the suspension stability of hardly water-soluble drug particles and suppress foaming during the coating process

Inventive Principle:
Principle #35Parameter changes

2Stability of the object's composition

If the layering liquid is stirred constantly to maintain suspension uniformity, then drug particles remain dispersed, but tube or spray nozzle clogging occurs due to precipitated/agglomerated particles

Engineering Contradiction:
Improvesuspension uniformityVSAvoidparticle precipitation and clogging
Core Design Contradiction:
Stability of the object's compositionVSObject-affected harmful factors

Solution Approach 1:

The nonionic surfactant acts as a protective intermediary that coats drug particles and prevents them from aggregating and precipitating. This eliminates the need for constant stirring while avoiding clogging of transfer tubes and spray nozzles

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The surfactant is added to the layering liquid before drug particle addition, creating a pre-conditioned environment that prevents particle aggregation from the outset. This preliminary action eliminates subsequent precipitation and clogging problems

Inventive Principle:
Principle #10Preliminary action

3Stability of the object's composition

If drug particle size is reduced to improve suspension stability and recovery ratio, then suspension uniformity improves, but an extra pulverization treatment step is required

Engineering Contradiction:
Improvesuspension stabilityVSAvoidprocess steps
Core Design Contradiction:
Stability of the object's compositionVSDevice complexity

Solution Approach 1:

Instead of changing particle size through pulverization, the chemical parameters of the layering liquid are modified by adding surfactants. This achieves improved suspension stability of larger drug particles without requiring additional size-reduction equipment or process steps

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 method enables the stable production of spherical base granules with high productivity and reduced agglomeration, maintaining suspension stability and improving the adhesion of drug particles to core particles, thus enhancing recovery ratios.

Implementation Method 1

from 0.01 to 1 % by mass of a polyoxyethylene hydrogenated castor oil as an emulsifier

Methodology Applied
Scientific EffectSurfactant action: Surfactant

Implementation Method 2

from 0.1 to 2 % by mass of micronized microcrystalline cellulose

Methodology Applied
Scientific EffectSuspension stabilization: Suspension

Data Source

PatentEP2050439B1Process for production of spherical granule containing slightly water-soluble substance
Publication Date: 2016.11.23 ASAHI KASEI KOGYO KABUSHIKI KAISHA
  • EP2050439B1 patent drawingFigure 1~2
  • EP2050439B1 patent drawingFigure 3~4
  • EP2050439B1 patent drawingFigure 5

AI summary

Spherical base granules comprising a hardly water-soluble drug and suited for film coating thereon are produced by layering spherical core particles with a drug-containing layering liquid comprising both micronized microcrystalline cellulose and an emulsifier therein and therefore having improved suspension stability.