Enteric Core/Shell Polymer Coating for Ethanol-Resistant Drug Release
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Solution Overview
Problem
Conventional gastric resistant pharmaceutical or nutraceutical compositions are not resistant to ethanol, leading to unintended increases in active ingredient release in the stomach, which can be harmful, and existing coatings do not effectively protect against ethanol's influence while maintaining rapid release in intestinal environments.
Innovation Solution
A coating composition comprising at least 20% by weight of an enteric core/shell polymer derived from an emulsion polymerization process, where the core is formed by a water-insoluble, non-cross-linked polymer or copolymer and the shell is formed by an anionic polymer or copolymer, or vice versa, providing gastric resistance and controlled release in both acidic and neutral pH environments.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional gastric resistant coatings are used, then release control in acidic environment is achieved, but resistance against ethanol influence is lost leading to unintended increase in active ingredient release
Solution Approach 1:
The patent applies composite materials by combining multiple polymer components with distinct functions: a water-insoluble polymer matrix (Eudragit® NE or NM) provides gastric resistance and structural integrity, while water-soluble polymers (Eudragit® L or S) embedded as discrete phases provide ethanol resistance and controlled release. This composite structure resolves the contradiction by integrating both gastric resistance and ethanol resistance in a single coating system.
Solution Approach 2:
The patent implements local quality by creating a heterogeneous coating structure where water-soluble polymer particles are dispersed within the water-insoluble polymer matrix. This local distribution of different polymer phases allows the coating to exhibit different properties in different locations: the water-insoluble matrix provides overall gastric resistance while the localized water-soluble phases provide ethanol resistance and controlled release pathways.
2Object-affected harmful factors
If gastric resistant coatings are used to prevent stomach release, then therapeutic safety is improved, but unintended release acceleration by ethanol occurs
Solution Approach 1:
The patent applies parameter changes by modifying the chemical composition and physical structure of the coating to respond differently to ethanol presence. The water-soluble polymer phases (Eudragit® L or S) change their solubility state in the presence of ethanol, creating controlled release pathways that prevent unintended release acceleration while maintaining gastric resistance through the water-insoluble matrix.
3Ease of manufacture
If conventional coatings are used, then manufacturing simplicity is maintained, but ethanol resistance cannot be achieved
Solution Approach 1:
The patent applies preliminary action by pre-forming water-soluble polymer particles (Eudragit® L or S) as discrete phases before incorporating them into the water-insoluble polymer matrix. This preliminary preparation of functional phases simplifies the manufacturing process compared to creating complex cross-linked structures, while still achieving ethanol resistance through the pre-positioned water-soluble release pathways.
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 coating composition effectively prevents excessive release of active ingredients in the stomach due to ethanol, while ensuring rapid release in the intestine, thus maintaining therapeutic efficacy and safety by stabilizing release profiles across varying pH conditions.
Implementation Method 1
The core/shell polymer composition is gastric resistant with no dissolution but swelling at acidic pH values
Implementation Method 2
The core/shell polymer composition also confers gastric resistance in the presence of ethanol in the stomach and prevents absorption and distribution of ethanol into the intestinal environment
Implementation Method 3
but dissolves more or less rapidly at higher pH values
Data Source
AI summary
The invention relates to a coating composition suitable for the coating of a pharmaceutical or nutraceutical dosage form, comprising a core comprising one or more pharmaceutical or nutraceutical active ingredients, wherein the coating composition is comprising at least 20% by weight of an enteric core/shell polymer composition derived from an emulsion polymerization process, wherein either the core of the core/shell polymer composition is formed by a water-insoluble, not cross-linked polymer or copolymer and the shell of the core/shell polymer composition is formed by an anionic polymer or copolymer or vice versa.