Directly Compressible PVA-MCC Co-mixture for Sustained-Release Tablets
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Solution Overview
Problem
Polyvinyl alcohols (PVAs) used in pharmaceutical formulations are challenging to directly compress due to their properties, leading to tablets with insufficient hardness and high abrasion, which complicates the production of sustained-release tablets with controlled release profiles.
Innovation Solution
A directly compressible co-mixture of polyvinyl alcohols (PVAs) and microcrystalline celluloses (MCCs) is developed, with specific ratios and processing methods to create tablets that can be compressed without granulation, ensuring prolonged release of active ingredients over several hours.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If polyvinyl alcohols (PVAs) are used as active ingredient carriers in sustained-release tablets, then prolonged release of active ingredient is achieved, but the tablets have insufficient hardness and high abrasion making them unsuitable for direct compression
Solution Approach 1:
The patent combines PVA with microcrystalline cellulose (MCC) to create a composite powder mixture. The MCC acts as a structuring agent that provides mechanical strength and compressibility to the PVA, enabling direct compression while maintaining the sustained-release properties. The composite leverages the gel-forming and swelling characteristics of PVA for prolonged release while MCC contributes to tablet hardness and structural integrity.
Solution Approach 2:
The patent modifies the physical parameters of PVA by controlling its degree of hydrolysis (72-90%) and molecular weight (20,000-150,000 g/mol). These parameter changes optimize the balance between swelling/gel-forming capacity for sustained release and compressibility for direct tablet formation. The specific parameter ranges enable PVA to form coherent structures that maintain tablet hardness while providing prolonged release.
2Duration of action of moving object
If polyvinyl alcohols (PVAs) are used as active ingredient carriers in sustained-release tablets, then prolonged release of active ingredient is achieved, but the tablets exhibit excessive abrasion and tendency to break
Solution Approach 1:
The combination of PVA and MCC creates a composite material where MCC provides mechanical reinforcement to the PVA matrix. This reinforcement reduces tablet friability and breakage while maintaining the gel-forming and swelling properties of PVA that are essential for sustained release over several hours.
Solution Approach 2:
By optimizing the degree of hydrolysis (72-90%) and molecular weight (20,000-150,000 g/mol) of PVA, the patent achieves a balance where the polymer forms sufficient gel structure for prolonged release while maintaining mechanical stability and reducing abrasion during handling.
3Quantity of substance
If conventional tabletting methods with PVAs are used, then active ingredient can be incorporated, but wet granulation and drying processes are required which consume energy and time
Solution Approach 1:
The patent modifies PVA parameters (degree of hydrolysis 72-90%, molecular weight 20,000-150,000 g/mol) to enable direct compression capability. This eliminates the need for wet granulation and drying steps, significantly reducing production time and energy consumption while maintaining effective active ingredient incorporation and sustained-release functionality.
4Quantity of substance
If conventional tabletting methods with PVAs are used, then active ingredient can be incorporated, but higher proportions of binders and lubricants are required which complicates the formulation
Solution Approach 1:
The PVA-MCC composite powder acts as a self-binding system where MCC provides structuring and binding properties. This reduces or eliminates the need for additional binders and lubricants, simplifying the formulation while enabling effective active ingredient incorporation and sustained-release tablet production through direct compression.
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 PVA-MCC co-mixture allows for the production of tablets with high hardness and low friability, achieving delayed release of active ingredients for at least 2 hours, preferably over 6-12 hours, using low pressing forces and reducing the need for lubricants, thus simplifying the tablet production process and improving therapeutic compliance.
Implementation Method 1
the tablets do not dissolve directly in the presence of liquid, such as in the mouth or gastrointestinal tract, but swell and the active ingredient is only gradually released through diffusion
Implementation Method 2
the active ingredient is only gradually released through diffusion
Implementation Method 3
The invention also relates to a process for producing corresponding directly compressible co-mixtures... containing polyvinyl alcohols (PVAs) and microcrystalline celluloses (MCCs)
Data Source
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AI summary
The present invention relates to directly compressible co-mixtures for the production of tablets with delayed release of active ingredient, which contain polyvinyl alcohols (PVAs) and micro-crystalline celluloses (MCCs). The invention also relates to a method for the production of corresponding directly compressible co-mixtures.