Mosapride Double-Layer Tablet for 24-Hour Gastrointestinal Release
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Solution Overview
Problem
Mosapride, a drug used for treating gastrointestinal disorders, has a short half-life requiring multiple daily administrations and conventional sustained-release formulations fail to maintain effective pharmacological activity for 24 hours due to rapid drug absorption and short gastrointestinal retention time.
Innovation Solution
A sustained-release formulation with a fast-release layer and a controlled-release matrix using high-viscosity and low-viscosity hydroxypropyl methylcellulose (HPMC) at specific ratios, allowing for controlled release and absorption over 18-24 hours, maintaining effective pharmacological activity for 24 hours.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If Mosapride is administered as a conventional immediate-release tablet, then rapid pharmacological activity is achieved, but the duration of action is too short requiring multiple daily administrations
Solution Approach 1:
The tablet is divided into two distinct layers: a fast-release layer containing immediate-release Mosapride for rapid onset, and a sustained-release layer containing controlled-release Mosapride for extended duration. This segmentation allows each layer to fulfill different functional requirements simultaneously.
Solution Approach 2:
Different regions of the tablet have different release characteristics - the fast-release layer provides rapid drug release for immediate effect, while the sustained-release layer provides gradual release for prolonged effect. Each layer is optimized with specific excipients and formulations to achieve its local release profile.
2Duration of action of moving object
If conventional sustained-release formulations are used, then duration of action is extended, but the initial pharmacological activity is delayed
Solution Approach 1:
The tablet is divided into two distinct layers: a fast-release layer containing immediate-release Mosapride for rapid onset, and a sustained-release layer containing controlled-release Mosapride for extended duration. This segmentation allows each layer to fulfill different functional requirements simultaneously.
Solution Approach 2:
The fast-release layer is designed to release drug immediately upon contact with gastrointestinal fluids, providing preliminary pharmacological action before the sustained-release layer begins its gradual release. This ensures rapid onset while maintaining extended duration.
3Speed
If the gastrointestinal retention time is short, then drug absorption is rapid, but the sustained-release effect cannot be maintained for 24 hours
Solution Approach 1:
The formulation uses specific excipients including hydroxypropyl methylcellulose (HPMC) with controlled viscosity, lactose, and other polymers to modify the dissolution rate and release profile. By adjusting the viscosity and concentration of HPMC, the release kinetics are controlled to maintain therapeutic levels for 24 hours.
Solution Approach 2:
The sustained-release layer combines multiple materials including HPMC, lactose, and other excipients in specific ratios to create a composite matrix that controls drug release. This composite structure provides both mechanical integrity and controlled dissolution characteristics for extended release.
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 achieves rapid pharmacological activity and sustained drug effect for 24 hours, improving patient compliance and reducing the frequency of dosages while maintaining therapeutic concentrations in the blood.
Implementation Method 1
a sustained-release layer comprising the active ingredient, a filler, a disintegrating agent, a controlled-release matrix, and an additive
Implementation Method 2
the sustained-release layer is prepared by mixing the high-viscosity hydroxypropyl methylcellulose (HPMC) having a viscosity of from 80 Pa·s to 120 Pa·s (80,000 cps to 120,000 cps) and the low-viscosity HPMC having a viscosity of 2 Pa·s to 20 Pa·s (2,000 cps to 20,000 cps)
Data Source
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AI summary
The formulation for oral administration of the present invention containing Mosapride or its salt is a double layer formulation consisting of a fast-release layer for rapid release of a drug and a sustained-release layer for slow release in order to simultaneously satisfy the rapid exhibition of pharmacological activities and sustained maintenance of pharmacological activities for 24 hours, wherein the high-viscosity hydroxypropyl methylcellulose (HPMC) and the low-viscosity HPMC are used in mixture such that the content of a high viscosity HPMC as a controlled-release matrix within the sustained-release layer has a higher content, thereby capable of controlling the dissolution rate in the regions having different pH values within the gastrointestinal tract and/or the retention time in the gastrointestinal tract. Additionally, the formulation of the present invention is a small-sized preparation with a total weight of 200 mg or less, preferably from 150 mg to 160 mg, thus capable of improving drug compliance of patients.