Multi-Layer Oral Formulation for Fat Soluble Antioxidant Delivery
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Solution Overview
Problem
Fat soluble antioxidants like flavonoids have low absorption in the human body due to their insolubility in water and degradation during storage and digestion, necessitating a delivery formulation that protects them until they can be released in the upper intestinal tract for optimal absorption.
Innovation Solution
A controlled release oral formulation comprising seed granules with multiple layers: a core of alkaline earth metal crystals, a protective microcrystalline cellulose and croscarmellose sodium layer, a fat soluble antioxidant layer, and an outer thermo-sensitive polymer gel layer, designed to withstand stomach acids and enzymes, and release the antioxidants in the small intestine for enhanced absorption.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If fat soluble antioxidants are administered orally, then they can be delivered to the body, but they degrade during storage and digestion and have low absorption due to water insolubility
Solution Approach 1:
The formulation is divided into multiple protective layers including an enteric coating layer and internal matrix layers, each serving specific protective functions to prevent degradation at different stages of storage and digestion
Solution Approach 2:
The patent introduces intermediate protective structures (enteric coating, matrix layers) that mediate between the antioxidants and the harsh digestive environment, protecting the antioxidants from degradation while enabling controlled release
2Speed
If fat soluble antioxidants are released in the stomach, then they can be released early, but the highly acidic and enzyme-active stomach environment degrades them before absorption
Solution Approach 1:
The enteric coating is designed to change its properties in response to pH changes, remaining intact in the acidic stomach environment (low pH) and dissolving in the more neutral intestinal environment (higher pH), thereby controlling the release timing and location
Solution Approach 2:
The formulation exploits the pH difference between stomach and intestine, using the acidic environment itself as a trigger for maintaining protection rather than releasing, and converts the harmful acidic environment into a selective barrier that protects until the desired release location
3Reliability
If fat soluble antioxidants are made more soluble in water, then absorption improves, but their fat soluble antioxidant properties are compromised
Solution Approach 1:
The patent introduces absorption-enhancing molecules as intermediaries that facilitate the transport of fat-soluble antioxidants across the intestinal membrane without changing the antioxidants' inherent fat-soluble properties
Solution Approach 2:
The formulation creates a composite system combining fat-soluble antioxidants with absorption-enhancing molecules, leveraging the properties of both components to achieve enhanced absorption while maintaining antioxidant efficacy
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 effectively protects fat soluble antioxidants during storage and digestion, ensuring their release and absorption in the intestinal tract, thereby improving bioavailability and extending shelf-life.
Implementation Method 1
The seed granules are made of microscopic (0.5 μm to 20 μm) alkaline earth metal crystal and include microscopic fissures formed therein
Implementation Method 2
an outer layer made of hardened, thermo-sensitive polymer gel
Data Source
AI summary
Oral formulation of particles made of an agglomeration of a plurality of seed granules or a single seed granule both surrounded by three layers and an outer gel coating. The seed granules are made of calcium carbonate with microscopic fissures. Disposed inside the fissures and in the interstitial spaces of the agglomerate seed granules are microscopic particles of alkali metal salts and other ions. Coating the agglomerate or single seed granules is an alkaline-resistant first layer made of microcrystalline cellulose and croscarmellose sodium that binds and protects the surrounding second layer. Surrounding the first layer is a second layer comprising a mixture of a flavonoid and polysaccharide or polypeptide binder or polymer gel. Surrounding the second layer is a third layer made of alkaline earth metal salt particles holding alkali metal hydroxide ions within a polysaccharide or polymer gel. Surrounding the third layer is at least one outer gel layer. The fourth and third layers dissolve in a low pH environment and release the fat soluble antioxidant and ions in the seed granule fissures.