PEG-PVA Graft Polymer Dry Binders for Tablet Cohesion

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Solution Overview

Problem

Current dry binders for direct tableting are inadequate in providing strong cohesion between tablet ingredients, leading to mechanically unstable tablets with poor resistance to crushing and friability, and are unsuitable for oxidation-sensitive active ingredients, while wet granulation is not feasible for such ingredients.

Innovation Solution

Development of a dry binder in powder form based on polyethylene glycol-polyvinyl alcohol graft polymer with a specific particle size range and packing fraction, produced through spray-drying, which enhances the binding properties and stability of tablets.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of manufacture

If conventional dry binders are used in direct tableting, then the process is cost-effective and simple, but the tablets exhibit poor mechanical stability, low resistance to crushing, and high friability

Engineering Contradiction:
Improveprocess simplicityVSAvoidtablet mechanical strength
Core Design Contradiction:
Ease of manufactureVSStrength

Solution Approach 1:

The invention changes the particle size parameter of the binder to a specific range (D[4,3] between 10-70 μm) and optimizes the packing fraction (k between 0.15-0.27). These parameter modifications enable the binder to form strong interparticle bridges during direct compression, achieving high tablet mechanical strength while maintaining process simplicity and cost-effectiveness

Inventive Principle:
Principle #35Parameter changes

2Strength

If a high proportion of binder is added to improve bonding, then cohesion between particles increases, but the tablet mass and volume increase making it difficult to swallow, and disintegration time is prolonged

Engineering Contradiction:
Improvebonding strengthVSAvoidtablet mass
Core Design Contradiction:
StrengthVSQuantity of substance

Solution Approach 1:

By changing the particle size parameter to 10-70 μm and optimizing packing fraction to 0.15-0.27, the binder achieves maximum binding efficiency at lower concentrations. The fine particles create numerous contact points and strong interparticle forces, providing adequate bonding strength with reduced binder quantity, thus maintaining acceptable tablet mass and disintegration characteristics

Inventive Principle:
Principle #35Parameter changes

3Ease of manufacture

If conventional dry binders are used, then the process avoids oxidation-sensitive ingredient degradation, but peroxide formation occurs in the binders themselves making them unsuitable for oxidation-sensitive active ingredients

Engineering Contradiction:
Improveprocess simplicityVSAvoidoxidation sensitivity
Core Design Contradiction:
Ease of manufactureVSObject-affected harmful factors

Solution Approach 1:

The invention uses a composite binder system consisting of polyvinyl alcohol and polyethylene glycol in a graft copolymer structure. This composite material combines the advantages of both polymers: PVA provides structural integrity while PEG segments prevent peroxide formation. The synergistic combination eliminates oxidation-related harmful effects while maintaining process simplicity and binder effectiveness

Inventive Principle:
Principle #40Composite materials

4Strength

If wet granulation is used for oxidation-sensitive and hydrolysis-sensitive active ingredients, then binding strength is achieved, but the process becomes infeasible due to moisture exposure causing hydrolysis

Engineering Contradiction:
Improvecohesion strengthVSAvoidhydrolysis sensitivity
Core Design Contradiction:
StrengthVSObject-affected harmful factors

Solution Approach 1:

The invention replaces the wet granulation process (which uses liquid binders and moisture) with a dry binding mechanism. The optimized fine particle binder (10-70 μm) creates strong bonds through mechanical interlocking and adhesion forces during direct compression, eliminating the need for moisture exposure. This substitution achieves comparable or superior cohesion strength while preventing hydrolysis of sensitive active ingredients

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

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 binder achieves high-strength tablets with improved mechanical properties, allowing for the compression of poorly compressible active ingredients and reducing tablet mass and volume, while maintaining flowability and preventing electrostatic charging.

Implementation Method 1

produced through spray-drying

Methodology Applied
Scientific EffectSpray-drying:

Implementation Method 2

spray-drying processes

Methodology Applied
Scientific EffectEvaporation: Evaporation

Data Source

PatentEP3641822B1Dry-binders for tablets based on polyethylene glycol-polyvinyl alcohol graft polymers, the production and use thereof
Publication Date: 2024.08.07 BASF SE

AI summary

A finely divided binder in powder form consisting of a polyethylene glycol-polyvinyl alcohol graft polymer particles, wherein the particles have an average particle size D[4,3] in the range of from 10 to 70 µm.