Ethanol-Resistant Coated Pharmaceutical Core Using Methacrylate and Guar Gum
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Solution Overview
Problem
Conventional extended or sustained release pharmaceutical or nutraceutical compositions are not resistant to ethanol, leading to altered release profiles and potential adverse effects when exposed to alcoholic media, necessitating a composition that maintains stable release rates despite ethanol presence.
Innovation Solution
A pharmaceutical or nutraceutical composition featuring a core with a coating layer comprising 80-96% water-insoluble (meth)acrylate polymer and 4-20% guar gum, designed to provide ethanol resistance while ensuring short preparation times and flat release profiles, maintaining release rates in the presence of up to 40% ethanol.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional extended or sustained release compositions are used, then they provide controlled release in aqueous media, but they are not resistant to ethanol and show altered release profiles in alcoholic media
Solution Approach 1:
The coating layer combines water-insoluble (meth)acrylate polymer (80-96 wt%) with guar gum (4-20 wt%) to create a composite material that provides both controlled release properties and ethanol resistance. The (meth)acrylate polymer forms the base coating that controls drug release, while guar gum provides cross-linking in ethanol-containing media to prevent premature release, achieving both reliability in aqueous media and adaptability to ethanol environments.
Solution Approach 2:
The invention changes the chemical composition parameters of the coating layer by incorporating specific ratios of hydrophobic (meth)acrylate polymers and guar gum. This parameter change enables the coating to exhibit different behaviors in aqueous versus ethanol-containing media, maintaining stable release profiles across varying ethanol concentrations (0-40% v/v) while preserving controlled release characteristics in aqueous environments.
2Speed
If coatings with high water-soluble polymer content are used to ensure rapid hydration, then release is fast in aqueous media, but ethanol resistance is compromised
Solution Approach 1:
The invention optimizes the hydrophobicity parameter of the coating by using water-insoluble (meth)acrylate polymers with specific molecular weights and compositions. This ensures slow, controlled hydration in aqueous media while maintaining structural integrity in ethanol-containing media, achieving both adequate hydration speed and reliable ethanol resistance through precise parameter control of the polymer properties.
Solution Approach 2:
The composite coating structure combines the hydrophobic (meth)acrylate polymer matrix with guar gum that provides ethanol-responsive cross-linking. This composite approach allows the coating to maintain appropriate hydration characteristics in water while gaining ethanol resistance through the guar gum's ability to form cross-linked structures in the presence of ethanol, without compromising the controlled hydration rate.
3Reliability
If plasticized ethyl cellulose and guar gum are used as in prior art, then ethanol resistance is achieved, but preparation time is extended to one day
Solution Approach 1:
The invention replaces the need for long-term plasticized ethyl cellulose with a formulation using water-insoluble (meth)acrylate polymers that do not require extended plasticization periods. The coating can be prepared and applied much more quickly without sacrificing ethanol resistance, as the (meth)acrylate polymer-guar gum system achieves its ethanol-resistant properties through chemical cross-linking rather than prolonged plasticization, significantly reducing preparation time.
Solution Approach 2:
The invention changes the formulation parameters by selecting (meth)acrylate polymers with specific glass transition temperatures and molecular weights that eliminate the need for extended plasticization. This parameter optimization allows the coating to achieve adequate flexibility and ethanol resistance directly after application, reducing the one-day preparation time required by prior art formulations to a much shorter period.
4Reliability
If thick coating layers are applied to ensure ethanol resistance, then release profile stability improves, but device complexity and manufacturing difficulty increase
Solution Approach 1:
The invention optimizes the thickness parameter of the coating layer by formulating a concentrated coating solution with high polymer content. This allows achieving the required ethanol resistance and release profile stability with thinner coating layers (typically 1-10 micrometers), reducing manufacturing complexity and avoiding the complications associated with applying and drying thick coating layers, while still providing adequate protection against ethanol-induced premature release.
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 resists the influence of ethanol, maintaining intended release rates and profiles, as defined by +/- 20% deviation criteria, ensuring stable and safe therapeutic effects even in ethanol-containing environments.
Implementation Method 1
a coating layer b), comprising a mixture of 80 to 96 % by weight of a water-insoluble (meth)acrylate polymer and 4 to 20 % by weight of guar gum
Implementation Method 2
The coating layer comprises a mixture of 80-96% water-insoluble (meth)acrylate polymer and 4-20% guar gum, designed to provide ethanol resistance while ensuring short preparation times and flat release profiles
Implementation Method 3
Pharmaceutical or nutraceutical compositions are designed to release the active ingredient in a manner of reproducible release curves
Implementation Method 4
The composition effectively resists the influence of ethanol, maintaining intended release rates and profiles
Data Source
AI summary
The invention relates to a pharmaceutical or nutraceutical composition, comprising a) a core a), comprising a pharmaceutical or a nutraceutical active ingredient and b) a coating layer b), comprising a mixture of 80 to 96 % by weight of a water-insoluble (meth)acrylate polymer and 4 to 20 % by weight of guar gum, wherein the water-insoluble (meth)acrylate polymer is composed of polymerized units of more than 95 and up to 100 % by weight C1- to C4-alkyl esters of acrylic acid or of methacrylic acid and less than 5% by weight of acrylic acid or methacrylic acid.