Cellulose-Polyphenol Composite Enteric Coating

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Solution Overview

Problem

Current enteric film coatings used in pharmaceutical and food materials lack sufficient pH-dependent dissolution characteristics, leading to unsatisfactory release profiles and stability issues, with pharmaceutical materials being brittle and requiring excessive excipients, and food materials not providing desired enteric quality.

Innovation Solution

A composition comprising a cellulose-based compound, a polyphenol-based compound, and an antioxidant, specifically hydroxypropyl methylcellulose (HPMC) with green tea extract, which forms a composite with pH-dependent solubility, enabling enteric coating with improved stability and safety for use in both pharmaceutical and food applications.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Adaptability or versatility

If alginates or shellac are used for food materials, then they can be used in food applications, but they do not have sufficient pH dependent dissolution characteristics and dissolve slowly not only in the stomach but also in the intestine

Engineering Contradiction:
Improveusability in food materialsVSAvoidpH dependent dissolution characteristics
Core Design Contradiction:
Adaptability or versatilityVSReliability

Solution Approach 1:

The patent uses a composite material consisting of polyphenol-based compound and cellulose-based compound to achieve both food material compatibility and sufficient pH-dependent dissolution characteristics. The synergistic combination of these two natural polymers creates a coating that dissolves rapidly in intestinal environment while being safe for food applications.

Inventive Principle:
Principle #40Composite materials

2Reliability

If pharmaceutical materials with enteric coating are used, then they have pH dependent dissolution characteristics, but they have low transparency, are brittle at low water concentration, and require large amounts of additional excipients

Engineering Contradiction:
ImprovepH dependent dissolution characteristicsVSAvoidamount of additional excipients
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent extracts and eliminates the need for additional excipients by using only the essential components - polyphenol-based compound and cellulose-based compound. The formulation achieves enteric coating functionality without requiring plasticizers, talc, or other additives, thereby reducing complexity and improving transparency.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent changes the chemical composition parameters by selecting specific polyphenol-based compounds and cellulose-based compounds with appropriate molecular weights and structural characteristics, enabling the coating to achieve desired properties without additional excipients.

Inventive Principle:
Principle #35Parameter changes

3Reliability

If materials having phthalic acid are used, then they provide enteric coating, but they have problems such as formation of free phthalic acid

Engineering Contradiction:
Improveenteric coating functionVSAvoidformation of free phthalic acid
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent converts the potential harm of using synthetic polymers into benefit by selecting natural polyphenol-based and cellulose-based compounds that provide enteric functionality without generating harmful degradation products like free phthalic acid. The natural origin of these polymers ensures safe degradation into benign substances.

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

4Adaptability or versatility

If natural products such as polyphenol-based compound and cellulose-based compound are mixed without antioxidants, then they can be used in food applications, but their long-term stability decreases

Engineering Contradiction:
Improvefood material compatibilityVSAvoidlong-term stability
Core Design Contradiction:
Adaptability or versatilityVSStability of the object's composition

Solution Approach 1:

The patent applies preliminary protection by incorporating antioxidants into the coating formulation before application. This preventive measure protects the polyphenol-based and cellulose-based compounds from oxidation during storage, maintaining long-term stability while preserving food compatibility.

Inventive Principle:
Principle #10Preliminary action

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 composite provides enhanced long-term storage stability, improved film quality, and enteric properties equivalent to pharmaceutical coatings, with the added benefit of antioxidant effects, ensuring safety and health benefits, while being environmentally friendly and cost-effective.

Implementation Method 1

the composite has pH-dependent solubility, and thus, may be used as a coating material or capsule material having enteric properties

Methodology Applied
Scientific EffectpH-dependent solubility:

Implementation Method 2

an antioxidant, specifically hydroxypropyl methylcellulose (HPMC) with green tea extract, which forms a composite with pH-dependent solubility, enabling enteric coating with improved stability and safety

Methodology Applied
Scientific EffectAntioxidation: Oxidation

Data Source

PatentEP2933290B1Composition for forming complex, complex formed therefrom, and composition for oral administration including said complex
Publication Date: 2019.09.18 LOTTE FINE CHEMICAL CO LTD
  • EP2933290B1 patent drawing

AI summary

Provide are a composition for forming a composite, the composition including a cellulose-based compound, a polyphenol-based compound, and a solvent, wherein an amount of the polyphenol-based compound is 1 to 40 parts by weight based on 100 parts by weight of the cellulose-based compound, a composite formed from the composition, and an orally ingestible composition including the composite. The composite has characteristics of being dissolved in a solvent in a various pH ranges depending on a mixing ratio of the cellulose-based compound and the polyphenol-based compound. Therefore, when the composite is used, a composite film may be easily prepared, and the composite film may be useful in medical or foods fields where film characteristics dependent on pH is required.