Proteinaceous Subcoating for Multiparticulate Stability

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Solution Overview

Problem

Existing multiparticulate formulations containing terpene-based active ingredients face challenges with storage stability due to volatility, leading to permeation, evaporation, or sublimation at elevated temperatures, which complicates processing and affects the integrity of the enteric coating.

Innovation Solution

A multiparticulate composition with a proteinaceous subcoating layer separating the terpene-based active ingredients from the enteric coating, using materials like gelatin or casein to prevent release of terpene-based active ingredients during processing and storage, ensuring stability at elevated temperatures.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If terpene-based active ingredients are used in multiparticulate formulations, then therapeutic efficacy is improved, but storage stability deteriorates due to volatility causing permeation, evaporation, or sublimation at elevated temperatures

Engineering Contradiction:

Improvestorage stabilityVSAvoidterpene-based active ingredient loss

Core Design Contradiction:

ReliabilityVSLoss of substance

Solution Approach 1:

A proteinaceous subcoating layer is introduced as an intermediary between the terpene-based active ingredient core and the enteric coating. This subcoating acts as a barrier that prevents terpene permeation and evaporation during processing and storage, while still allowing the enteric coating to function properly for controlled release in the gastrointestinal tract.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The formulation uses a composite structure with multiple coating layers: an inner proteinaceous subcoating (gelatin, casein, or soy protein) and an outer enteric coating. This composite material approach combines the volatility-blocking properties of proteins with the pH-dependent release properties of enteric coatings, solving both stability and therapeutic efficacy requirements.

Inventive Principle:

Principle #40Composite materials

2Reliability

If enteric coating is applied to protect terpene-based active ingredients, then controlled release is improved, but manufacturing complexity increases due to difficulty in processing at elevated temperatures

Engineering Contradiction:

Improvecontrolled release profileVSAvoidprocessing complexity

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The proteinaceous subcoating is applied first as a preliminary protective layer before applying the enteric coating. This preliminary action creates a stable base that prevents terpene loss during subsequent enteric coating processing at elevated temperatures, simplifying the overall manufacturing process by eliminating the need for specialized low-temperature processing techniques.

Inventive Principle:

Principle #10Preliminary action

3Reliability

If proteinaceous subcoating is used to prevent terpene loss, then storage stability is improved, but manufacturing cost increases

Engineering Contradiction:

Improvestorage stabilityVSAvoidmanufacturing cost

Core Design Contradiction:

ReliabilityVSEase of manufacture

Solution Approach 1:

The patent employs inexpensive protein materials such as gelatin, casein, or soy protein for the subcoating layer. These are cost-effective, readily available materials that provide the necessary protective function during storage and processing, making the enhanced stability solution economically viable for commercial pharmaceutical manufacturing.

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

The proteinaceous subcoating layer effectively maintains the stability of terpene-based active ingredients, allowing for successful enteric coating and controlled release profiles, enhancing storage stability and efficacy of the formulation.

Implementation Method 1

a proteinaceous subcoating layer covering the core and separating the core from their respective enteric coatings... prevents the terpene-based active ingredients from permeating, evaporating, or sublimating

Methodology Applied

Scientific EffectPermeation barrier: Physical Containment

Implementation Method 2

using a proteinaceous coating prevents the L-menthol based active ingredients in the core from permeating, evaporating, or sublimating at elevated temperatures

Methodology Applied

Scientific EffectEvaporation prevention: Physical Containment

Data Source

PatentUS11826475B2Enteric coated multiparticulate compositions with a proteinaceous subcoat

Publication Date: 2023.11.28 SOCIETE DES PRODUITS NESTLE SA

AI summary

A method of treating a gastrointestinal disorder includes administering to a patient an effective amount of a multiparticulate dosage form including a plurality of individual spheroidal enteric coated cores having a diameter of 0.1 mm to 3 mm. The individual spheroidal enteric coated cores have (a) a core including menthol, (b) a proteinaceous subcoating over the core, and (c) an enteric coating over the proteinaceous subcoating. The multiparticulate dosage form is configured to release most of the menthol in the area of the GI tract where the inflammation is occurring.