Gastroretentive Formulation Using Composite Matrix for Stomach Retention
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Solution Overview
Problem
Current gastroretentive formulations fail to effectively retain active substances in the upper part of the gastrointestinal tract for sustained release, limiting the absorption and therapeutic efficacy of drugs like metformin and ciprofloxacin.
Innovation Solution
A gastroretentive formulation comprising an active substance granulated with a mixture of a weak gelling agent, a strong gelling agent, and a gas generating agent, which swells and floats in the stomach, controlling drug release through gas entrapment and slow dissolution, allowing prolonged retention and absorption.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If multilayer tablets or small tablets with disintegrating and effervescent agents are used, then the formulation can be retained in the stomach, but the sustained release effect and retention time are insufficient
Solution Approach 1:
The patent uses a composite matrix system combining hydrophilic polymers (for swelling and gel formation), effervescent agents (for gas generation and floating), and hydrophobic polymers (for controlled release). This multi-component composite material system achieves both prolonged retention through floating mechanism and reliable sustained release through the combined actions of different materials, resolving the contradiction between retention time and sustained release effectiveness.
2Ease of operation
If tablets are made small for easy ingestion, then ease of operation improves, but the ability to provide sustained release and maintain structural integrity deteriorates
Solution Approach 1:
The patent changes the physical and chemical parameters of the tablet matrix by incorporating hydrophilic polymers that undergo swelling upon contact with gastric fluid. This swelling transforms the tablet structure, creating a gel matrix that maintains structural integrity even in small tablet forms. The effervescent agents further modify the physical state by generating gas bubbles that provide internal support, enabling small tablets to maintain strength and provide sustained release while remaining easy to ingest.
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 ensures prolonged retention in the stomach, achieving sustained release and enhanced absorption of active substances, particularly for drugs like ciprofloxacin and metformin, with improved therapeutic effects.
Implementation Method 1
the effervescent agent, which liberate gas on reaction with the gastric medium, helps to keep the tablet floating in the stomach
Implementation Method 2
an active substance granulated with a mixture of a weak gelling agent, a strong gelling agent
Implementation Method 3
the weak gelling agent helps the matrix to swell faster due to its fast wetting property
Implementation Method 4
The released gas gets adsorbed on the surface of the gelled matrix forming a bubbled layer on the surface
Implementation Method 5
as the drug is diffused or delivered from the gelled matrix
Data Source
AI summary
The present invention concerns gastroretentive formulation comprising an active substance granulated with a mixture of a weak gelling agent, a strong gelling agent, and a gas generating agent and process for manufacturing said formulation.