Oral Composition Dual-Layer Coating Intestinal Release
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Solution Overview
Problem
The challenge lies in achieving reliable bioavailability of sensitive pharmaceutical ingredients like proteins and peptides when administered orally, due to digestive enzymes and acidic stomach environments, which often result in unpredictable absorption in the gastrointestinal tract.
Innovation Solution
A solid oral composition with a core surrounded by a coating comprising two components, where the first component is resistant to the stomach environment and the second component is enzymatically active in the intestine, allowing targeted release of the entrapped material in the intestine.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If a sensitive active pharmaceutical ingredient is orally delivered, then the delivery route is easier and more convenient, but the bioavailability becomes unreliable due to digestive enzymes and acidic environment
Solution Approach 1:
The coating is divided into two functional segments: a first component that provides acid resistance in the stomach, and a second component that provides enzymatic degradation in the intestine. This segmentation allows the system to address different environmental challenges at different GI tract locations, resolving the contradiction between ease of oral delivery and reliable bioavailability.
Solution Approach 2:
The coating uses a composite structure combining two different materials with complementary properties: an acid-resistant material for gastric protection and an enzyme-degradable material for intestinal release. This composite approach enables the system to maintain reliability of bioavailability while preserving the ease of oral delivery route.
2Stability of the object's composition
If a coating is designed to protect entrapped material in the stomach, then stability is improved, but controlled release in the intestine becomes more difficult to achieve
Solution Approach 1:
The coating transitions from a static protective barrier to a dynamic system that responds to environmental changes. The second component remains stable in acid but becomes actively degraded by intestinal enzymes, automatically switching from protection mode to release mode. This dynamic behavior resolves the contradiction between maintaining stability in the stomach and enabling controlled release in the intestine.
Solution Approach 2:
The coating's degradation behavior is controlled by changing the pH parameter and enzyme presence. The first component withstands low pH while the second component degrades at higher pH in the presence of intestinal enzymes. This parameter-based control allows simultaneous achievement of stomach stability and intestinal release without complex manufacturing.
3Productivity
If the coating degrades rapidly in the intestine, then release of entrapped material is enhanced, but premature degradation in the stomach may occur
Solution Approach 1:
The first component acts as an intermediary protective layer that shields the second component from acidic degradation in the stomach. This intermediary structure allows the second component to remain intact during gastric passage and only then degrade rapidly in the intestine, resolving the contradiction between rapid release and protection during stomach passage.
Solution Approach 2:
The first component provides preliminary protection against acid degradation before the material reaches the intestine. This pre-protection prevents premature degradation of the second component, ensuring that rapid degradation and release occur only at the intended location in the intestine, not in the stomach.
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 coating effectively protects the entrapped material during stomach passage and ensures controlled release in the intestine, enhancing bioavailability and stability of sensitive compounds like proteins, peptides, and small molecules.
Implementation Method 1
the second component enzymatically digest the first component when subjected to the more basic environment of the intestine compared to the more acidic environment of the stomach
Data Source
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AI summary
The present invention relates to a solid oral composition for targeted release in an intestine of a mammal comprising a core and a coating completely surrounding the core, wherein the core comprises an entrapped material to be released in the intestine, and wherein the coating or part of the coating comprises a first and a second component, and the first component is resistant to the environment in the stomach of a mammal and the second component enzymatically digest the first component when subjected to the more basic environment of the intestine compared to the more acidic environment of the stomach.