Gastro-resistant Matrix Using Swellable Polymers
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Solution Overview
Problem
Existing gastro-resistant pharmaceutical forms require lengthy film coating processes, which are limited to solid dosage forms and struggle with achieving delayed release in multilayered tablets without affecting other layers, and are inefficient for active ingredients with different release kinetics.
Innovation Solution
A solid gastro-resistant pharmaceutical form is created using a mixture of three hydrophilic polymers: a swellable pH-independent polymer, a swellable polymer insoluble at pH lower than 4.0 and soluble at higher pH, and an oligomer that forms a soluble complex with the active ingredient, forming a transient gelled barrier that delays release until intestinal pH is reached, eliminating the need for film coating.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If film coating techniques are used to create gastro-resistant dosage forms, then the active ingredient is protected from gastric environment, but the manufacturing process becomes particularly long and complex
Solution Approach 1:
The invention extracts and eliminates the film coating step from the manufacturing process. Instead of coating the core with gastro-resistant film, the gastro-resistant matrix is directly compressed from a powder mixture containing swellable polymers and pH-dependent polymers, achieving gastro-resistance without the time-consuming coating process
Solution Approach 2:
The gastro-resistant matrix is segmented into multiple functional components: swellable polymers (first and second polymers) that provide structural framework and pH-dependent polymer (third polymer) that provides the gastro-resistant mechanism. This segmentation allows each component to perform its specific function efficiently
2Reliability
If film coating is applied to achieve delayed release in multilayered tablets, then one layer gains gastro-resistance, but all other layers are also coated and affected
Solution Approach 1:
The invention applies local quality by incorporating the gastro-resistant matrix composition specifically into the layer requiring delayed release, while other layers can have different compositions and release characteristics. Each layer can be independently formulated with the appropriate polymer mixture to achieve its specific release profile without affecting other layers
3Reliability
If film coating techniques are used, then gastro-protection is achieved, but the process is inefficient for active ingredients with different release kinetics
Solution Approach 1:
The gastro-resistant matrix composition based on swellable and pH-dependent polymers is a universal solution that can be applied to any active ingredient requiring gastro-protection or delayed release, regardless of its specific release kinetics requirements. The polymer composition can be adjusted to accommodate different release profiles while maintaining the same fundamental mechanism
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 efficiently delays the release of active ingredients through the gastric tract, providing gastro-resistance or gastro-protection without the need for film coating, and allows for single gastro-resistant layers in multilayered tablets, simplifying the manufacturing process and ensuring controlled release at intestinal pH.
Implementation Method 1
the first polymer is swellable and pH-independent
Implementation Method 2
they form together a strong transient barrier of gelled polymer
Implementation Method 3
the second polymer is swellable, insoluble at pH lower than 4.0 and soluble at pH higher than 4.0
Implementation Method 4
the third polymer is an oligomer able to make a soluble complex with the active ingredient
Implementation Method 5
The gelled barrier reduces the diffusion of the active ingredient when the dosage form containing these polymers is immersed in an acid solution
Data Source
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AI summary
A solid gastro-resistant delayed release pharmaceutical form obtained without using gastro-resistant film coating is described.