Glucomannan Microparticles Sustained Release Hydrogel
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Solution Overview
Problem
Conventional sustained release solid dosage forms often fail to ensure complete bioavailability of active ingredients, as a portion remains unreleased in the digestive tract and is excreted before reaching the small intestine, leading to reduced therapeutic efficacy.
Innovation Solution
The use of glucomannan microparticles with an average particle size less than 50 μm, produced by suspending refined konjac flour in aqueous ethanol and grinding to create a hydrogel that releases the active ingredient within 6 hours, enhancing bioavailability by forming a hydrogel in the stomach and controlling dissolution time with additives like sugar alcohols and gums.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If conventional water-insoluble polymer coating is used for sustained release, then dissolution control is achieved, but complete bioavailability cannot be ensured as portion remains unreleased
Solution Approach 1:
The patent changes the particle size parameter of glucomannan to less than 50 μm, transforming it from a conventional coating material into microparticles that form hydrogels. This parameter change enables the material to swell and dissolve completely in gastrointestinal fluids, ensuring 100% or nearly 100% release of the active ingredient while maintaining sustained release over 6 hours or more.
Solution Approach 2:
The patent creates a composite system where glucomannan microparticles form a hydrogel matrix that encapsulates the active ingredient. This composite structure combines the sustained release properties of glucomannan with complete bioavailability, as the hydrogel gradually swells and releases the entire contents without leaving residual material.
2Reliability
If glucomannan microparticles with average particle size less than 50 μm are used, then complete bioavailability is achieved, but manufacturing complexity increases
Solution Approach 1:
The patent employs a self-grinding process where glucomannan particles are suspended in aqueous ethanol and subjected to high-speed stirring that automatically grinds them to the required microparticle size. This self-service approach eliminates the need for external grinding equipment or complex manufacturing steps, making the production of <50 μm microparticles simple and scalable.
Solution Approach 2:
The patent changes the physical state parameter of glucomannan by suspending it in aqueous ethanol, which facilitates the self-grinding process. This parameter change (from dry powder to suspended state) enables automatic size reduction through simple stirring, greatly simplifying the manufacturing process while achieving the required microparticle size for complete bioavailability.
3Duration of action of moving object
If conventional sustained release formulations are used, then dissolution control is achieved, but small intestine transit time is insufficient for complete release
Solution Approach 1:
The patent employs a dynamic hydrogel system where glucomannan microparticles continuously swell and adjust their structure in response to gastrointestinal conditions. This dynamic behavior allows the formulation to adapt its release rate to match the variable transit time through the digestive tract, ensuring complete release even within the limited 6-hour small intestine transit window.
Solution Approach 2:
The patent changes the structural parameter of the release matrix by using swellable hydrogel-forming microparticles instead of rigid water-insoluble coatings. This parameter change enables the formulation to transition from a static barrier to a dynamic release system that can fully dissolve and release 100% of the active ingredient within the constrained transit time of the small intestine.
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 approach ensures nearly complete release of the active ingredient within the small intestine transit time, improving bioavailability and therapeutic effectiveness by forming a hydrogel that releases the active ingredient over 6 hours, with adjustable dissolution times using blended substances.
Implementation Method 1
When administered orally, the sustained release solid dosage preparation according to present invention forms a hydrogel and essentially entire portion of the active ingredient is released from the hydrogel up to about 6 hours
Data Source
AI summary
A sustained release solid dosage preparation is provided comprising an active ingredient admixed with an excipient. At least part of the excipient consists of glucomannan microparticles having an average particle size less than 50 μm. The glucomannan microparticles forms, when absorbing water, a hydrogel matrix for the active ingredient capable releasing the active ingredient almost entirely up about 6 hours.