Polysaccharide Capsule with Hygroscopic Liquid Fill

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Solution Overview

Problem

Conventional gelatin capsules face issues such as animal origin, high water content, sensitivity to heat and humidity, brittleness, and interactions with active substances, leading to reduced bioavailability and stability concerns, particularly for low-solubility substances.

Innovation Solution

A delivery system comprising a container formed from a polysaccharide-based film forming composition and a liquid fill with a polar and hygroscopic solvent, such as glycerol, which improves solubility and bioavailability of active agents while maintaining stability and compatibility with non-animal based containers.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of manufacture

If gelatin is used as capsule shell material, then correct gelling, film forming and surface active properties are achieved, but animal origin and sensitivity to heat and humidity occur

Engineering Contradiction:
Improvecapsule shell formationVSAvoidheat and humidity sensitivity
Core Design Contradiction:
Ease of manufactureVSObject-affected harmful factors

Solution Approach 1:

The patent changes the material parameter from gelatin to polysaccharide derivatives (such as cellulose derivatives, starch derivatives, or their combinations), fundamentally altering the chemical composition to eliminate animal origin while maintaining capsule formation capabilities and reducing sensitivity to environmental factors

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs composite material structures by combining polysaccharide derivatives with other compatible substances to create capsule shells that achieve both the desired film-forming properties and resistance to heat and humidity, replacing the单一 gelatin material with a composite system

Inventive Principle:
Principle #40Composite materials

2Strength

If gelatin capsules are used, then flexibility is maintained through plasticizers and residual moisture, but brittleness occurs when water content decreases below 10%

Engineering Contradiction:
Improvecapsule shell flexibilityVSAvoidwater content stability
Core Design Contradiction:
StrengthVSStability of the object's composition

Solution Approach 1:

The patent changes the moisture content parameter to an optimal range (5-15%) and uses polysaccharide derivatives that maintain flexibility at this lower moisture level, eliminating the brittleness issue that occurs in gelatin when water content drops below 10%

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent applies local quality modification by using specific polysaccharide derivatives with different functional groups and molecular structures that provide localized flexibility and moisture retention properties, allowing the capsule shell to maintain flexibility without requiring high overall water content

Inventive Principle:
Principle #3Local quality

3Reliability

If gelatin capsules are used, then bioavailability of hydrophobic drugs is increased, but interactions with active substances and reduced stability occur

Engineering Contradiction:
Improveactive substance stabilityVSAvoidinteractions with active substances
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent introduces polysaccharide derivatives as intermediary substances that act as barriers between the capsule shell and active substances, preventing direct interactions while maintaining the protective function of the capsule. These derivatives serve as a mediating layer that reduces harmful interactions and improves stability

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the chemical composition parameter from gelatin to polysaccharide derivatives, which have different chemical properties that reduce interactions with active substances. This parameter change fundamentally alters the interaction mechanism, improving stability and reducing harmful effects

Inventive Principle:
Principle #35Parameter changes

4Duration of action of moving object

If gelatin capsules are used, then correct disintegration characteristics are achieved, but aggregation under hot and humid conditions occurs

Engineering Contradiction:
Improvedisintegration timeVSAvoidcapsule integrity
Core Design Contradiction:
Duration of action of moving objectVSStability of the object's composition

Solution Approach 1:

The patent changes the material composition parameter to polysaccharide derivatives that maintain disintegration characteristics while providing resistance to aggregation under hot and humid conditions. This parameter change allows the capsule to maintain its structural integrity during storage while still achieving proper disintegration when administered

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 delivery system enhances the bioavailability and stability of active agents, maintains moisture balance, and reduces oxygen permeability, ensuring consistent performance and storage stability.

Implementation Method 1

a liquid fill comprising a matrix composition comprising of at least one solvent which is both polar and hygroscopic

Methodology Applied
Scientific EffectHygroscopic: Absorption (physical)

Implementation Method 2

The delivery system enhances the bioavailability and stability of active agents, maintains moisture balance, and reduces oxygen permeability

Methodology Applied
Scientific EffectPermeation resistance: Permeation

Implementation Method 3

a liquid fill comprising a matrix composition comprising of at least one solvent which is both polar and hygroscopic; and an active agent or mixture thereof soluble in the matrix composition

Methodology Applied
Scientific EffectSolvation: Solvation

Data Source

PatentUS8795720B2Liquid filled delivery system
Publication Date: 2014.08.05 CAPSUGEL BELGIUM NV

AI summary

The present invention provides a delivery system comprising: (a) a container which is a formed body obtained from a film forming composition comprising at least one polysaccharide or polysaccharide derivative; (b) a liquid fill comprising a matrix composition of at least one solvent which is both polar and hygroscopic or a mixture of solvents each of which is both polar and hygroscopic; and (c) an active agent or a mixture of active agents wherein the active agent is soluble in said polar and hygroscopic solvent or mixture of polar and hygroscopic solvents, and a process for the preparation of said delivery system.