Solid Particle Composition for Dysphagia Swallowing

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Solution Overview

Problem

Current solid oral compositions, such as tablets and capsules, pose difficulties in swallowing for approximately 35% of the population, particularly among the elderly and those with dysphagia, leading to poor compliance with treatments due to their fragility, moisture sensitivity, and the need for disintegrating agents that can affect bioavailability and taste.

Innovation Solution

A solid composition comprising non-agglomerated particles with high apparent density Ps particles (≥0.6 g/cm³) and active ingredient Pa particles, where Ps particles rapidly dissolve in saliva, facilitating ingestion without disintegration, reducing the volume of solid matter, and eliminating the need for disintegrating agents.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If tablets or capsules are used for solid oral administration, then the composition can be delivered in a stable solid form, but swallowing becomes difficult for approximately 35% of the population

Engineering Contradiction:
Improveswallowing easeVSAvoidtreatment compliance
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The invention divides the solid composition into small individual particles instead of using traditional tablets or capsules. This segmentation allows the particles to be easily swallowed without requiring significant swallowing effort, while still delivering the complete therapeutic dose when taken together as a bulk powder

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention changes the physical parameter of particle size and morphology, creating small particles with specific surface area characteristics that facilitate easy swallowing. The particles are designed to flow freely and can be taken as a bulk powder, fundamentally changing the physical form from compacted tablet to loose particulate matter

Inventive Principle:
Principle #35Parameter changes

2Speed

If lyophilisates are used to achieve rapid disintegration, then breakdown occurs very rapidly in the mouth, but the compositions become highly fragile and sensitive to atmospheric moisture

Engineering Contradiction:
Improvedisintegration speedVSAvoidmechanical stability
Core Design Contradiction:
SpeedVSStrength

Solution Approach 1:

The invention uses conventional pharmaceutical excipients and standard manufacturing processes instead of complex lyophilization technology. The particles are designed to disintegrate rapidly upon contact with saliva through conventional mechanisms, achieving the desired speed without requiring the fragile, moisture-sensitive structure of lyophilisates

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

Solution Approach 2:

The invention changes the approach to rapid disintegration by using conventional compressed tablets or capsules with optimized formulation rather than lyophilized structures. This maintains mechanical stability and moisture resistance while achieving rapid breakdown through standard disintegration mechanisms

Inventive Principle:
Principle #35Parameter changes

3Speed

If effervescent tablets are used for rapid breakdown, then complete disintegration occurs in the mouth, but the tablets must be compact and emit gas with characteristic bad taste

Engineering Contradiction:
Improvebreakdown speedVSAvoidgas emission and taste
Core Design Contradiction:
SpeedVSObject-generated harmful factors

Solution Approach 1:

The invention extracts the effervescent mechanism from the dosage form, using only conventional compressed tablets or capsules without gas-generating excipients. This eliminates the harmful gas emission and bad taste while maintaining rapid disintegration through conventional mechanisms

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The invention uses simple conventional tablet formulations without complex effervescent couples, achieving rapid breakdown through standard disintegration agents and formulation optimization, thereby eliminating the need for gas emission and associated taste problems

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

4Ease of operation

If chewable tablets are used for easy ingestion, then swallowing is facilitated, but the tablets require significant time to break down in the oral cavity

Engineering Contradiction:
Improveingestion easeVSAvoidbreakdown time
Core Design Contradiction:
Ease of operationVSLoss of time

Solution Approach 1:

The invention segments the dosage into small particles that can be quickly ingested as a bulk powder without requiring chewing. The small particle size enables rapid disintegration and dissolution in the oral cavity and gastrointestinal tract, eliminating the time delay associated with chewable tablet breakdown

Inventive Principle:
Principle #1Segmentation

5Speed

If orally disintegrating tablets with high disintegrating agents content are used, then disintegration occurs within seconds, but chalky taste and dryness are generated

Engineering Contradiction:
Improvedisintegration speedVSAvoidchalky taste and dryness
Core Design Contradiction:
SpeedVSObject-generated harmful factors

Solution Approach 1:

The invention extracts the high-content disintegrating agents from the formulation, using only conventional amounts of standard disintegrating excipients in compressed tablets. This eliminates the chalky taste and dryness sensations while maintaining rapid disintegration through optimized formulation and particle size

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The invention uses conventional pharmaceutical excipients at standard concentrations rather than high amounts of specialized disintegrating agents, achieving rapid disintegration through formulation optimization without generating unpleasant sensory effects

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

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

Enables rapid and effortless ingestion of significant active ingredient quantities without altering bioavailability, reducing product loss, and overcoming issues of fragility and stability, while being more economical and comfortable for patients.

Implementation Method 1

Ps particles, rapidly soluble in saliva

Methodology Applied
Scientific EffectSolvation: Solvation

Data Source

PatentUS11304905B2Solid composition for quick ingestion with facilitated swallowing, in the form of solid, non-agglomerated particles, comprising two different types of particles
Publication Date: 2022.04.19 UNITHER PHARMA INC

AI summary

A solid composition with rapid ingestion and facilitated swallowing, in the form of non-agglomerated solid particles, said composition comprising the following two different types of particle:Pa particles, with very low solubility in saliva and comprising at least one active ingredient, andPs particles, rapidly soluble in saliva, characterised by an apparent density equal to or greater than approximately 0.6 g.cm−3, advantageously equal to or greater than approximately 0.7 g.cm−3, and preferably between 0.7 and 1.5 g.cm−3 inclusive.