Alcohol-Resistant Oral Pharmaceutical Form via Hydrophobic Coating
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Solution Overview
Problem
Current sustained-release oral pharmaceutical forms are not resistant to immediate release of active ingredients when alcohol is consumed, posing a risk of 'dose dumping' and failing to maintain therapeutic levels over a long period, especially for severe pain management.
Innovation Solution
Development of microgranules with a neutral carrier coated with a hydrophobic polymer and an inert load, which prevents immediate release of the active ingredient even in the presence of alcohol, ensuring sustained release kinetics suitable for a single or two daily doses.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If a sustained-release oral pharmaceutical form is used to control release of active ingredient, then the duration of action is extended, but the form is vulnerable to alcohol-induced immediate release (dose dumping)
Solution Approach 1:
The patent employs a composite coating structure consisting of multiple layers: an inner layer containing the active ingredient and an outer hydrophobic polymer coating layer. This composite structure combines the sustained-release properties of the inner formulation with the alcohol-resistant barrier provided by the outer hydrophobic coating, preventing alcohol-induced dose dumping while maintaining extended duration of action.
Solution Approach 2:
The patent modifies the solubility parameter of the coating material by selecting hydrophobic polymers with specific solubility characteristics. The coating layer is designed to be insoluble or poorly soluble in alcohol, changing the dissolution behavior from alcohol-sensitive to alcohol-resistant. This parameter change in material solubility enables the formulation to maintain sustained release kinetics even in the presence of alcohol consumption.
2Reliability
If a carrier made insoluble in water or alcohol is used to prevent immediate release, then alcohol resistance is improved, but the dissolution kinetics are not compatible with single daily administration
Solution Approach 1:
The patent applies local quality by creating a differentiated structure where the inner core maintains the active ingredient in a controlled-release matrix, while the outer coating layer provides selective alcohol resistance. The coating layer has different properties from the core, being hydrophobic and alcohol-insoluble, which locally prevents alcohol penetration without affecting the overall dissolution kinetics of the inner sustained-release formulation.
3Reliability
If pH-dependent polymers are used to achieve alcohol resistance, then dissolution kinetics are not appreciably affected by ethanol, but the behavior changes in man depending on individual and conditions
Solution Approach 1:
The patent extracts the pH-dependent polymer component from the formulation and replaces it with a hydrophobic polymer coating layer. By removing the pH-dependent mechanism and using a purely hydrophobic barrier instead, the formulation achieves alcohol resistance without the variability introduced by pH-dependent behavior. This extraction of the problematic component eliminates the inconsistency in human response while maintaining alcohol resistance.
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 microgranules maintain a consistent therapeutic level over time, preventing dose dumping and ensuring safety and efficacy even with alcohol consumption, while being cost-effective and easy to produce industrially.
Implementation Method 1
at least one coating layer comprising: a hydrophobic coating polymer selected from non-water soluble cellulose derivatives
Data Source
AI summary
A sustained release oral pharmaceutical form suitable for single daily dose administration has a neutral microgranule coated with a mounting layer of active ingredient and pharmaceutically acceptable binder; and a coating layer of a hydrophobic coating polymer of a non-water soluble cellulose derivative, and at least 20% of inert load in relation to dry weight of hydrophobic coating polymer. The pharmaceutical form has improved resistance to rapid release of active ingredient, particularly in the presence of alcohol.