Floating Gastroretentive Dosage Form with Elastic Membrane
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current gastroretentive systems face challenges in extending gastric residence time for certain drugs, ensuring uniform release in the GI tract, and maintaining efficacy for drugs with narrow absorption windows, high pH-dependent solubility, or susceptibility to degradation, leading to reduced therapeutic effects and potential side effects.
Innovation Solution
A floating gastroretentive dosage form comprising a sustained release swellable matrix core with a superdisintegrant, water-soluble polymer, acid, and gas-generating agent, surrounded by a water-insoluble permeable elastic membrane, which swells rapidly to prevent passage through the pyloric sphincter and maintains drug release for 8-16 hours.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of stationary object
If hydrophilic polymeric matrices are used for sustained release, then drug retention in dosage form is improved, but gastric residence time is reduced and drug may reach colon
Solution Approach 1:
The patent changes the physical parameters of the dosage form by incorporating swelling agents that increase its size and buoyancy in gastric environment. This parameter change allows the dosage form to retain drug while extending gastric residence time through floating mechanism, preventing premature passage to colon
Solution Approach 2:
The patent applies buoyancy force as a counterweight to gravity to keep the dosage form floating in the stomach. By incorporating gas-generating agents and swelling agents, the dosage form achieves density less than gastric fluid, creating an upward buoyant force that counteracts gravitational pull and prevents gastric emptying
2Duration of action of stationary object
If dosage form passes through small intestine to colon, then drug is retained too long, but drug degradation by intestinal enzymes occurs
Solution Approach 1:
The patent converts the harmful effect of prolonged transit into a benefit by using it to drive the floating mechanism. The dosage form is designed to float and release drug gradually during gastric retention, transforming the potential harm of extended GI tract exposure into beneficial prolonged drug availability at the absorption site
3Reliability
If dosage form is retained in stomach for prolonged period, then drug bioavailability is improved, but mechanical integrity may be compromised under hydrodynamic conditions
Solution Approach 1:
The patent uses composite material structure combining multiple polymers with different properties: swelling agents for expansion, gas-generating agents for buoyancy, and film-forming polymers for structural integrity. This composite approach maintains mechanical strength while enabling prolonged gastric retention and improved bioavailability
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 solution provides prolonged gastric retention, improved bioavailability, and sustained release of drugs, reducing side effects by ensuring drug release in the stomach and upper GI tract, while maintaining mechanical integrity under hydrodynamic conditions.
Implementation Method 1
a gas-generating agent
Implementation Method 2
a sustained release swellable matrix core
Data Source
AI summary
The present disclosure is directed to floating gastroretentive dosage forms with prolonged gastric residence time. The disclosure also provides rapidly expanding sustained release or combined immediate release and sustained release formulations comprising drugs that require targeted release in the proximal gastrointestinal tract for maximum therapeutic benefit. The rapidly expanding floating gastroretentive dosage forms comprise a permeable elastic membrane providing desired characteristics for drug release and mechanical strength to maintain tablet integrity.