Ethanol-Resistant Gastric Coating via Methacrylate Copolymer
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Solution Overview
Problem
Conventional gastric resistant pharmaceutical or nutraceutical compositions are not resistant to ethanol, leading to unintended release of active ingredients in the stomach when exposed to ethanol-containing media, which can result in suboptimal therapeutic effects or toxicity.
Innovation Solution
A gastric resistant composition with a core containing a pharmaceutical or nutraceutical active ingredient coated with a gastric resistant layer comprising at least 30% by weight of a (meth)acrylate copolymer, specifically polymerized units of acrylic or methacrylic acid and their alkyl esters, which maintains less than 10% release of the active ingredient at pH 1.2 for 2 hours, even in the presence of 20% ethanol.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If a conventional gastric resistant coating is used, then the composition maintains gastric resistance in acidic conditions, but the composition becomes susceptible to ethanol influence leading to unintended release
Solution Approach 1:
The coating layer uses a composite polymer system combining (meth)acrylate copolymers with specific monomer ratios (10-40% acrylic/methacrylic acid, 10-80% C4-C18 alkyl ester) to achieve both gastric resistance and ethanol resistance. This composite material approach allows the coating to maintain its barrier properties in both acidic and alcoholic environments, resolving the contradiction between gastric resistance and ethanol susceptibility.
Solution Approach 2:
The invention changes the chemical composition parameters of the coating polymer by specifying precise monomer ratio ranges and incorporating specific alkyl ester components. These parameter changes modify the coating's physical-chemical properties to resist both gastric acid and ethanol, transforming the coating from ethanol-susceptible to ethanol-resistant while maintaining gastric resistance.
2Manufacturing precision
If the coating is designed for aqueous medium only, then the release profile is optimized for water-based environments, but the release profile is altered by ethanol-containing media
Solution Approach 1:
The coating layer is designed with multi-functionality to perform effectively in both aqueous and ethanol-containing media. The specific (meth)acrylate copolymer composition enables the coating to maintain its controlled release function regardless of whether the environment is water-based or alcohol-based, making the composition adaptable to various media without compromising release profile precision.
3Reliability
If ethanol resistance is added to gastric resistant compositions, then the composition becomes resistant to both gastric acid and ethanol, but the coating complexity increases
Solution Approach 1:
Rather than adding multiple separate components, the invention achieves dual resistance by optimizing the parameters of a single polymer system - the (meth)acrylate copolymer with specific monomer ratios. This approach incorporates both gastric and ethanol resistance functions within one coating composition, avoiding the need for complex multi-layer or multi-component systems.
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 composition effectively protects the active ingredient from premature release in acidic conditions and maintains controlled release profiles, ensuring therapeutic efficacy while minimizing toxicity risks, even when exposed to ethanol.
Implementation Method 1
the release of the pharmaceutical or nutraceutical active ingredient is not more than 10 % under in-vitro conditions at pH 1.2 after 2 hours in medium according to USP with and without the addition of 20 % (v/v) ethanol
Implementation Method 2
a gastric resistant coating layer onto the core, whereby the release of the pharmaceutical or nutraceutical active ingredient is not more than 10 % under in-vitro conditions
Implementation Method 3
Controlled release pharmaceutical compositions with resistance against the influence of ethanol employing a coating comprising neutral vinyl polymers and excipients
Data Source
AI summary
The invention discloses a gastric resistant pharmaceutical or nutraceutical composition, comprising a core, comprising a pharmaceutical or nutraceutical active ingredient and a gastric resistant coating layer onto the core, wherein the gastric resistant coating layer comprises at least 30 % by weight of a (meth)acrylate copolymer comprising polymerized units of 10 to 40 % by weight of acrylic or methacrylic acid, 10 to 80 % by weight of a C4- to C18-alkyl ester of acrylic or methacrylic acid and optionally 0 to 60 % by weight of another vinylic monomer, whereby the release of the pharmaceutical or nutraceutical active ingredient is not more than 10 % under in-vitro conditions at pH 1.2 after 2 hours in medium according to USP with and without the addition of 20 % (v/v) ethanol.