Floating Tab-in-Tab Tablets for Linear Gastric Drug Release
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Solution Overview
Problem
Conventional floating tablets face challenges with non-linear drug release, weak gel strength, and inadequate gastric retention, particularly with high drug loads, leading to inconsistent bioavailability and safety issues.
Innovation Solution
A floating tab-in-tab dosage form comprising a core and a shell, where the shell includes a release retarding agent, a gelling agent capable of ionically cross-linking with divalent cations, an acid-soluble divalent cation, and a bicarbonate salt, which enhances gel strength and achieves linear drug release.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of stationary object
If conventional floating systems are used, then gastric retention time is prolonged, but drug release follows a logarithmic curve resulting in variable bioavailability
Solution Approach 1:
The tablet is divided into an inner core and an outer shell, each with distinct compositions and release characteristics. The core contains drug with hydrophilic polymer for initial release, while the shell contains drug with hydrophobic polymer for sustained release, achieving linear release profile
Solution Approach 2:
The invention uses composite material structure with hydrophilic and hydrophobic polymers in different layers. The core uses hydrophilic polymer (e.g., HPMC) for rapid release, while the shell uses hydrophobic polymer (e.g., ethyl cellulose) for controlled release, creating linear release kinetics
2Quantity of substance
If high drug load is used in floating formulations, then dosage effectiveness is improved, but gel strength decreases making the system weak
Solution Approach 1:
The tablet structure separates high drug load into core and shell portions, allowing the core to contain concentrated drug while the shell provides structural support with hydrophobic polymer matrix, maintaining gel strength despite high overall drug load
Solution Approach 2:
The composite structure combines hydrophilic polymer matrix in core with hydrophobic polymer matrix in shell, creating a dual-network system that maintains mechanical strength while accommodating high drug loads through the shell's structural framework
3Duration of action of stationary object
If effervescent agents are used to provide buoyancy, then gastric retention is enhanced, but the system lacks sufficient gel strength to resist gastric churning forces
Solution Approach 1:
The invention uses composite material structure with hydrophilic and hydrophobic polymers in different layers. The core uses hydrophilic polymer (e.g., HPMC) for rapid release, while the shell uses hydrophobic polymer (e.g., ethyl cellulose) for controlled release, creating linear release kinetics
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 dosage form exhibits high tensile strength, satisfactory floating lag time, and linear drug release, maintaining effective gastric retention and bioavailability, even with high drug loads, while being easily preparable and chemically stable.
Implementation Method 1
a gelling agent capable of being ionically cross-linked in the presence of divalent cations
Implementation Method 2
When this system comes into contact with gastric fluid, CO2 is released due to the reaction of the effervescent agent with gastric fluid
Implementation Method 3
a hydrophilic gel material
Data Source
AI summary
The invention relates to new gastroretentive tablets that are floating tab-in-tab dosage forms. The invention also relates to a process for obtaining thereof, as well as to the use thereof for treating diseases or conditions in which such gastroretentive tablets are useful.