Oral Corticosteroid Capsule with Enteric and Sustained Release Layers
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Solution Overview
Problem
Current oral corticosteroid treatments for gastrointestinal diseases like Crohn's and ulcerative colitis face challenges in achieving targeted, sustained drug delivery to specific intestinal regions, leading to systemic side effects and limited long-term use due to inadequate localized therapeutic effects.
Innovation Solution
Development of an oral drug delivery composition with a delayed and sustained release mechanism, utilizing a starch capsule coated with an alkali-containing ethyl cellulose material and an acid, which prevents initial drug release in the stomach and controls release in the intestine, ensuring targeted delivery of corticosteroids to specific intestinal areas for extended periods.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If oral corticosteroids are used for treatment, then therapeutic effect is achieved, but systemic exposure increases causing side effects
Solution Approach 1:
The capsule is segmented into two functional components: a delayed release component (enteric coating) that prevents premature release in the stomach, and a sustained release component (ethyl cellulose matrix) that controls drug release over time in the intestine. This segmentation allows the drug to be delivered specifically to the intestinal target site while minimizing systemic absorption and side effects.
Solution Approach 2:
The composition provides localized drug delivery to the intestine through site-specific release mechanisms. The enteric coating ensures drug release occurs only in the intestinal environment (pH > 5.5), and the ethyl cellulose matrix provides sustained release at the target site. This local quality concentration maximizes therapeutic effect at the disease location while minimizing systemic exposure.
2Ease of operation
If standard oral formulations are used, then drug delivery is simple, but drug release is not sustained leading to inadequate long-term treatment
Solution Approach 1:
The composition uses a composite material system combining two distinct release mechanisms: an enteric polymer coating (e.g., cellulose acetate phthalate, polyvinyl acetate phthalate) for delayed release, and an ethyl cellulose matrix for sustained release. This composite structure maintains the simplicity of oral administration while providing prolonged drug release action (typically 8-24 hours) that inadequate standard formulations cannot achieve.
3Object-affected harmful factors
If targeted delivery to intestine is achieved, then systemic exposure is minimized, but formulation complexity increases
Solution Approach 1:
The formulation employs a nested structure where the sustained release component (ethyl cellulose matrix containing the corticosteroid) is enclosed within the delayed release component (enteric coating). This nested doll approach minimizes systemic exposure by ensuring the drug is released only in the intestine, while the complexity is managed through a hierarchical rather than parallel structure, where each layer performs a specific function in sequence.
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 minimizes systemic exposure, providing sustained therapeutic effects in targeted intestinal regions, reducing side effects and enabling long-term treatment of gastrointestinal diseases by ensuring controlled and prolonged drug release in the desired areas of the gastrointestinal tract.
Implementation Method 1
They typically comprise tablets or pellets which are coated to prevent drug release in the upper regions of the gastrointestinal tract. Coatings described for this purpose include enteric (gastroresistant) materials which are insoluble in stomach acid and dissolve in intestinal fluid.
Implementation Method 2
The sustained release component prevents immediate release of all of the drug. The drug is released over a period of time as it passes through the intestine.
Implementation Method 3
Materials which are biodegraded by the microflora residing in the colon have also been described
Data Source
AI summary
The present invention provides an oral drug delivery composition comprising a sustained release component which comprises a corticosteroid drug and which is contained within a capsule that has been treated so that the sustained release component is predominately released from the capsule in the intestine following oral administration. The present invention also provides a drug delivery composition for delivering a corticosteroid drug to the intestine comprising: (a) a sustained release component comprising a corticosteroid drug, an alkali- containing ethyicellulose material and an acid; and (b) a delayed release component which substantially prevents release of the sustained release component until the composition reaches the intestine following oral administration. The compositions of the invention are useful for treating inflammatory diseases of the gastrointestinal tract such as Crohn's disease and ulcerative colitis and for treating glomerulonephritis.