Oral Pharmaceutical Coating with pH-Responsive Polymers
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Solution Overview
Problem
Existing oral pharmaceutical formulations, particularly orodispersible tablets, face challenges in providing a protective coating that is stable in saliva and soluble in gastric juice, while also ensuring rapid dissolution in the stomach, especially for APIs with unpleasant tastes or causing heartburn, and in managing the release behavior of silicas and fatty acids in coating compositions.
Innovation Solution
The use of a coating composition comprising 10-50% silica and 5-10% solid fatty acids, along with gastro-soluble (meth)acrylate-based polymers, which creates a stable film in saliva and dissolves effectively in gastric juice, delaying API release in the mouth but not in the stomach, thereby masking unpleasant tastes and ensuring timely gastric release.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Object-affected harmful factors
If a protective coating is applied to mask unpleasant taste of APIs, then taste masking is improved, but the coating must remain stable in saliva while dissolving rapidly in gastric juice
Solution Approach 1:
The coating composition is designed with different functional components that respond to different local environments: silica and fatty acids provide saliva stability for taste masking, while gastro-soluble polymers ensure rapid dissolution in the acidic gastric environment. This local quality differentiation resolves the contradiction between needing coating stability in the mouth and rapid dissolution in the stomach.
Solution Approach 2:
The coating utilizes parameter changes in the gastrointestinal tract, specifically the pH difference between saliva (neutral pH) and gastric juice (acidic pH). The gastro-soluble polymers remain stable at neutral pH but dissolve rapidly at acidic pH, enabling the coating to mask taste in the mouth while releasing the API quickly in the stomach.
2Speed
If silica is used in coating composition to improve dissolution, then dissolution rate is improved, but release behavior of silicas must be managed
Solution Approach 1:
The coating employs a composite material system combining silica, fatty acids, and gastro-soluble polymers. This composite approach allows silica to contribute to dissolution rate enhancement while the polymer matrix controls the overall release behavior, managing the contradictory requirements of rapid dissolution and controlled release.
Solution Approach 2:
The gastro-soluble polymer acts as an intermediary that mediates between silica and the aqueous environment. It controls the interaction between silica particles and saliva/gastric juice, managing the release behavior while allowing silica to enhance dissolution when conditions are appropriate.
3Object-affected harmful factors
If solid fatty acids are added to coating composition, then taste masking is improved, but the combination with silica and polymers must be optimized
Solution Approach 1:
The invention merges multiple functional components (silica for dissolution enhancement, fatty acids for taste masking, gastro-soluble polymers for environmental responsiveness) into a single integrated coating composition. This merging allows all components to work synergistically, improving taste masking while maintaining controlled release without requiring separate coating layers.
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
This composition effectively delays API delivery in the mouth while maintaining rapid dissolution in the stomach, improving taste masking and release profiles, as demonstrated by improved dissolution profiles in various pH conditions, including those simulated for oral and gastric environments.
Implementation Method 1
a gastro-soluble (meth)acrylate-based polymer... which creates a stable film in saliva and dissolves effectively in gastric juice
Implementation Method 2
a coating composition... comprises... silica... delaying API release in the mouth
Implementation Method 3
a coating composition... comprises... solid fatty acids... masking unpleasant tastes
Data Source
AI summary
Described herein are oral pharmaceutical formulations comprising a core component and a coating composition applied on the core component. Also described is a process for producing said oral pharmaceutical formulations.