Bioadhesive Multilayer Tablet for Extended GI Residence
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Solution Overview
Problem
Conventional oral drug administration methods result in shorter residence time of dosage forms in the gastrointestinal tract due to stomach voiding and intestinal peristaltic movements, especially during pathological conditions, leading to reduced bioavailability and therapeutic effectiveness.
Innovation Solution
Development of a novel pharmaceutical composition in the form of a multilayer tablet with at least one layer providing immediate or fast release and another layer extending the residence time through bioadhesive properties, using polymers like sodium alginate and polyethylene oxide to adhere to the gastrointestinal mucosa, thereby increasing the drug's presence in the absorption area.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If conventional oral dosage forms are administered, then the drug can be delivered to the gastrointestinal tract, but the residence time at the absorption site is short due to peristaltic movements and stomach voiding
Solution Approach 1:
The dosage form is segmented into multiple functional layers: a bioadhesive layer containing polymers like sodium alginate and carboxymethyl cellulose that adheres to the GI mucosa, a controlled release layer with hydrophilic matrices such as HPMC and xanthan gum that regulates drug release, and an immediate release layer providing initial therapeutic effect. This segmentation allows the drug to remain at the absorption site longer while controlling release kinetics.
Solution Approach 2:
The invention uses composite material systems combining multiple polymers with different properties: bioadhesive polymers (sodium alginate, carboxymethyl cellulose) for mucosal attachment, hydrophilic matrix formers (HPMC, xanthan gum) for controlled release, and immediate release excipients. This composite approach enables simultaneous achievement of prolonged residence time and controlled drug release profiles.
2Reliability
If the drug is released quickly for immediate therapeutic effect, then bioavailability is improved, but the duration of action is reduced requiring frequent dosing
Solution Approach 1:
The dosage form is segmented into multiple functional layers: a bioadhesive layer containing polymers like sodium alginate and carboxymethyl cellulose that adheres to the GI mucosa, a controlled release layer with hydrophilic matrices such as HPMC and xanthan gum that regulates drug release, and an immediate release layer providing initial therapeutic effect. This segmentation allows the drug to remain at the absorption site longer while controlling release kinetics.
Solution Approach 2:
The multilayer structure enables periodic drug release patterns: an initial burst release from the immediate release layer provides rapid therapeutic effect, followed by sustained release from the controlled release layer that maintains therapeutic levels over extended periods. This periodic action pattern satisfies both immediate efficacy and prolonged duration requirements.
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 bioadhesive multilayer tablet design enhances the gastrointestinal residence time of active principles, allowing for prolonged and controlled release, thereby improving bioavailability and reducing the frequency of dosing, particularly beneficial for drugs absorbed in the small intestine or colon.
Implementation Method 1
a bioadhesive polymer layer which provides an adhesive strength, measured as a force of detachment, of at least 100 mN when measured using advanced force gauge equipment
Data Source
AI summary
A novel pharmaceutical composition, which comprises a therapeutically effective amount of active principle(s) or a pharmaceutically acceptable salt or enantiomer or polymorph thereof, optionally one or more release controlling agent(s) and pharmaceutical acceptable excipient(s) thereof, wherein the composition is formulated to increase the residence time of the said pharmaceutical composition and/or active principle(s) in the gastrointestinal tract. A novel pharmaceutical composition comprising at least two entities wherein one entity is an immediate release/fast release and the other is controlled release. A pharmaceutical composition comprising at least two entities wherein one entity is an immediate release/fast release and the other is bioadhesive. A pharmaceutical composition comprising: at least two entities wherein one entity is controlled release and the other is bioadhesive All the three compositions are formulated to increase the residence time of active principle(s) in the gastrointestinal tract. A multilayered composition with active in a layer which provides immediate release or controlled release of active principles and layer providing increased residence time in the GI tract.