Emulsion Coating System for Delayed Release in Small Intestine
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Solution Overview
Problem
Existing coating systems for particles fail to achieve controlled release of active ingredients in the gastrointestinal tract, particularly in delivering the active ingredient after passing the stomach in the small intestine.
Innovation Solution
A coating system comprising an emulsion with an aqueous phase containing water, emulsifier, plasticizer, film-forming agent, and pH adjuster, combined with an oily phase including enteric coating material and polyunsaturated fatty acids, which allows for delayed release of the active ingredient in the small intestine.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If a conventional coating system is used to coat particles, then the coating process is simple, but the active ingredient is released too early in the gastrointestinal tract before reaching the small intestine
Solution Approach 1:
The patent employs a composite coating system comprising multiple functional layers: an enteric coating layer (polyacrylic acid, polyvinyl alcohol, or cellulose derivatives) that resists stomach acid, a polyunsaturated fatty acid layer (omega-3 or omega-6) that provides delayed release properties, and a plasticizer layer (glycerol, triethyl citrate, or tributyl citrate) that modulates coating flexibility and release characteristics. This multi-layer composite structure achieves controlled release in the small intestine while maintaining coating integrity through the gastrointestinal tract.
Solution Approach 2:
The patent utilizes pH-dependent parameter changes to achieve controlled release. The enteric coating materials are selected to remain insoluble at low pH (stomach environment) and become soluble at higher pH (small intestine environment). The polyunsaturated fatty acids and plasticizers are selected based on their phase transition temperatures and glass transition temperatures, which change with temperature and pH, thereby controlling the release timing and rate of the active ingredient.
2Reliability
If the coating layer is made thicker to ensure delayed release, then the release is delayed, but the coating becomes more prone to defects and manufacturing becomes more difficult
Solution Approach 1:
The patent applies different coating materials and thicknesses to different functional requirements. The enteric coating layer is applied first as a base layer providing acid resistance, followed by a thinner polyunsaturated fatty acid layer for delayed release, and finally a plasticizer layer for flexibility. Each layer has optimized thickness and composition for its specific function, making the overall coating easier to manufacture while achieving the desired delayed release effect.
Solution Approach 2:
The coating system is segmented into distinct functional layers, each with specific materials and purposes. This segmentation allows independent optimization of each layer's properties and thickness, simplifying the coating application process while achieving complex release characteristics through the coordinated action of multiple thinner layers rather than one thick layer.
3Reliability
If polyunsaturated fatty acids are added to the coating system, then the delayed release is achieved, but the coating system becomes more sensitive to oxidation
Solution Approach 1:
The patent introduces plasticizers (glycerol, triethyl citrate, or tributyl citrate) as intermediary substances that protect the polyunsaturated fatty acids from direct exposure to oxidizing environments. The plasticizer layer acts as a barrier and stabilizing medium, reducing the oxidation sensitivity of the polyunsaturated fatty acids while maintaining the delayed release function. The plasticizer also provides flexibility to the coating and modulates the release characteristics.
Solution Approach 2:
The coating system uses a composite structure where polyunsaturated fatty acids are combined with plasticizers and enteric coating materials. This composite formulation protects the sensitive polyunsaturated fatty acids through the stabilizing and barrier effects of the other components, particularly the plasticizer layer, thereby reducing oxidation sensitivity while preserving the delayed release property.
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 described coating system enables a controlled and delayed release of active ingredients in the small intestine, ensuring effective delivery of pharmaceutical compounds, vitamins, minerals, and other nutrients.
Implementation Method 1
a coating system (CS) consisting of an (i) aqueous solution comprising a. water, and b. at least one emulsifier, and c. at least one plasticizer, and d. at least one film forming agent, and e. at least one pH adjuster, and (ii) oily phase comprising a. at least one enteric coating material, and b. at least one polyunsaturated fatty acid
Data Source
AI summary
The present invention relates to a new coating system useful for coating particles, which comprise an active ingredient. Such coated particles, when consumed, do show a controlled release in the human or animal body.