Reservoir Microparticles Preventing Alcohol-Induced Dose Dumping
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Solution Overview
Problem
Current pharmaceutical forms with modified release (MR) are susceptible to accelerated drug release when consumed with alcohol, posing safety risks due to altered solubility and system modification, leading to potential overdose or ineffectiveness, especially for medications with narrow therapeutic windows.
Innovation Solution
Development of a multimicroparticulate pharmaceutical form with reservoir-type microparticles coated with a polymer, plasticizer, and optional surfactant, incorporating an agent D that hydrates or solvates more slowly in alcoholic solutions, maintaining the modified release profile and preventing dose dumping.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If a pharmaceutical form with modified release is used to maintain plasma concentration and avoid overdose, then the duration of action is improved and toxicity is reduced, but the system becomes vulnerable to accelerated drug release in the presence of alcohol causing dose dumping
Solution Approach 1:
The patent introduces agent D as an intermediary substance that modulates the interaction between the modified release system and alcohol. Agent D preferentially binds to alcohol or alters the solvent properties of the alcoholic medium, preventing alcohol from disrupting the polymer coating or matrix structure. This intermediary mechanism allows the modified release system to maintain its controlled release properties even in the presence of alcohol, resolving the contradiction between reliability and alcohol sensitivity
Solution Approach 2:
The patent modifies the chemical and physical parameters of the release system by incorporating agent D, which changes the solubility characteristics, hydration properties, or polymer-coating stability. These parameter changes make the release system less sensitive to alcohol-induced alterations, maintaining controlled release kinetics across different alcoholic concentrations and preventing dose dumping while preserving the extended duration of action
2Reliability
If the coating or matrix structure is made more resistant to alcohol, then the reliability in alcoholic solution is improved, but the complexity of the formulation increases
Solution Approach 1:
The patent combines agent D with existing formulation components (polymer coating, matrix materials, or excipients) to create an integrated release system. Rather than adding a separate complex alcohol-resistant layer or structure, agent D is merged into the existing formulation architecture, providing alcohol resistance through chemical interaction or compositional modification. This merging approach maintains reliability in alcoholic solutions while minimizing increases in formulation complexity
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 formulation ensures sustained release of active principles in both aqueous and alcoholic solutions, reducing the risk of dose dumping and maintaining therapeutic efficacy even when alcohol is present, thus enhancing patient safety.
Implementation Method 1
agent D which is a pharmaceutically acceptable compound and whose speed or capacity to hydrate or to solvate is greater in an aqueous medium free of alcohol than in an alcoholic solution
Implementation Method 2
agent D which is a pharmaceutically acceptable compound and whose speed or capacity to hydrate or to solvate is greater in an aqueous medium free of alcohol than in an alcoholic solution
Implementation Method 3
In another group, that of matrix systems, the AP, intimately dispersed in a matrix, for example based on a polymer, is released from the tablet by diffusion and erosion
Implementation Method 4
In another group, that of matrix systems, the AP, intimately dispersed in a matrix, for example based on a polymer, is released from the tablet by diffusion and erosion
Data Source
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AI summary
The invention aims at minimizing the risks of release of the dose associated with the concurrent consumption of alcohol and certain pharmaceutical or dietary forms with modified release. The invention concerns an oral form comprising reservoir-type microparticles, with modified release of at least one active principle. The invention is characterized in that it is resistant to the immediate release of the dose of active principle in the presence of alcohol. In particular, the inventive oral form is characterized in that the releasing time of 50% of the active principle, in an alcohol-containing solution is not reduced by more than 3 times compared to the releasing time of 50% of the active principle in an alcohol-free aqueous medium. The form comprises an agent D which is a pharmaceutically acceptable compound of which the hydrating or solvating speed and capacity is higher in an alcohol-free aqueous medium than in an alcohol-containing solution.