Particulate Composition for Solid Preparation Outer Layer

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Solution Overview

Problem

Conventional methods for creating easy-to-take solid preparations are complex, require solvent-stable active ingredients, and struggle with forming a thick coating layer, while granulating sugar alcohols often necessitate organic solvents and strict conditions, leading to aggregation issues.

Innovation Solution

A particulate composition comprising sugar alcohol and a water-insoluble polymer, such as micro-fibrillated cellulose, combined with a gelling agent that becomes slippery when contacted with water, allowing for a dry compression-molding process to create a solid preparation with improved moldability and taste masking.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If conventional coating methods using gelling agent solutions are used, then the preparation surface shows slipperiness when contacted with water, but the process becomes complicated requiring preparation of gelling agent solution and transfer to coating machine

Engineering Contradiction:
Improveslipperiness when contacted with waterVSAvoidprocess complexity
Core Design Contradiction:
Ease of operationVSDevice complexity

Solution Approach 1:

The invention combines the gelling agent and outer layer forming materials into a single integrated composition that can be applied directly during compression molding, eliminating the separate coating step. The composition contains both the gelling agent (sodium carmellose) and outer layer materials (sugar alcohol and water-insoluble polymer) in one formulation that forms the outer layer during the compression process itself.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The invention extracts the gelling agent solution preparation step from the overall process and replaces it with a dry composition that achieves the same slipperiness effect when contacted with water, but without requiring solution preparation and coating equipment.

Inventive Principle:
Principle #2Taking out (Extraction)

2Object-generated harmful factors

If conventional coating methods are used to form a thick coating layer, then taste masking is improved, but the process requires solvent-stable active ingredients and becomes more complex

Engineering Contradiction:
Improvetaste maskingVSAvoidprocess complexity
Core Design Contradiction:
Object-generated harmful factorsVSDevice complexity

Solution Approach 1:

The invention merges the outer layer formation and taste masking function into the compression molding process itself. The composition is applied directly to the core during compression, forming a thick outer layer that masks the taste of the active ingredient without requiring separate coating operations or solvent-based formulations.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The invention changes the physical state parameter from liquid solution to dry powder composition, and changes the application timing from post-compression coating to during-compression application. This allows thick outer layer formation without requiring solvent stability of active ingredients.

Inventive Principle:
Principle #35Parameter changes

3Strength

If sugar alcohol granulation is performed to improve moldability, then tablet hardness is improved, but organic solvents are required and aggregation occurs under conventional conditions

Engineering Contradiction:
Improvetablet hardnessVSAvoidaggregation
Core Design Contradiction:
StrengthVSObject-generated harmful factors

Solution Approach 1:

The invention uses a composite material system consisting of sugar alcohol (for hardness and moldability) combined with water-insoluble polymer (for structural integrity) and gelling agent (for slipperiness). This composite approach achieves tablet hardness improvement without requiring organic solvents or causing aggregation, as the materials are compatible in the dry state and during water contact.

Inventive Principle:
Principle #40Composite materials

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 enables the production of easy-to-take solid preparations with enhanced swallowability and taste masking, using a dry process that maintains the stability of active ingredients and prevents aggregation, resulting in a thicker, more effective outer layer.

Implementation Method 1

a gelling agent that will show slipperiness when it is brought into contact with water

Methodology Applied
Scientific EffectGelling: Gel

Implementation Method 2

particulate composition comprising sugar alcohol and a water-insoluble polymer

Methodology Applied
Scientific EffectPhysical mixing and compression:

Data Source

PatentUS11058643B2Composition for outer layer of solid preparation, and easy-to-take solid preparation including said composition for outer layer
Publication Date: 2021.07.13 DAICEL CORP

AI summary

The purpose of present invention to provide a particulate composition that has the excellent provides moldability and useful as a composition that is used as an outer layer of a solid preparation, especially an easy-to-take solid preparation and the like; a composition for an easy-to-take solid preparation, which comprises the particulate composition and a gelling agent that will show slipperiness when it is brought into contact with water; and a solid preparation comprising the composition.The present invention relates to a particulate composition comprising sugar alcohol and a water-insoluble polymer; a composition for an easy-to-take solid preparation, which comprises the particulate composition and a gelling agent that will show slipperiness when it is brought into contact with water; and a solid preparation comprising the composition and the like.