Low Viscosity Hydroxyalkyl Cellulose Binder for Tablet Aggregation
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Solution Overview
Problem
Current methods using hydroxypropyl cellulose as a binder for core particles with a particle size of 100 µm or less fail to completely inhibit aggregation and ensure efficient drug layering, often resulting in prolonged disintegration times and reduced tablet hardness.
Innovation Solution
A hydroxyalkyl cellulose with a viscosity of 1.10 mPa·s to 1.95 mPa·s in a 2%-concentration aqueous solution at 20°C is used as a binder, reducing aggregation and enhancing drug layering efficiency while maintaining sufficient tablet strength and disintegration properties.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If hydroxypropyl cellulose with viscosity of 2.0-2.9 mPa·s is used as a binder, then aggregation of core particles is suppressed to some extent, but drug layering efficiency is not sufficiently increased and disintegration time is prolonged
Solution Approach 1:
The patent changes the viscosity parameter of hydroxypropyl cellulose from the conventional range of 2.0-2.9 mPa·s to a lower range of 1.10-1.95 mPa·s. This parameter change enables the binder to effectively suppress aggregation of core particles with 100 μm or less diameter while simultaneously improving drug layering efficiency and reducing disintegration time, thus resolving the technical contradiction between aggregation suppression and disintegration time reduction.
2Reliability
If coating agent with weak binding force is used to inhibit aggregation, then aggregation is reduced, but binding force between core particles and drug particles is weakened and drug particles are easily detached
Solution Approach 1:
The patent changes the viscosity parameter of the binder to a specific low range of 1.10-1.95 mPa·s, which optimizes the balance between binding force and aggregation inhibition. This parameter change allows the coating agent to provide sufficient binding force to prevent particle detachment while simultaneously inhibiting aggregation of core particles, resolving the contradiction between these two requirements.
3Loss of time
If amount of binder is reduced to shorten disintegration time, then disintegration time is reduced, but tablet hardness is reduced and rapid disintegration properties cannot be obtained with high degree of hardness
Solution Approach 1:
The patent changes the viscosity parameter of hydroxypropyl cellulose to 1.10-1.95 mPa·s, which enables effective aggregation suppression and drug layering at lower binder concentrations. This parameter change allows formulation of tablets with both high hardness and rapid disintegration properties, resolving the contradiction between tablet hardness and disintegration time without requiring increased binder amounts.
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 hydroxyalkyl cellulose effectively prevents core particle aggregation, ensures nearly complete drug coverage, and produces tablets with improved hardness and disintegration times.
Implementation Method 1
the core particles having a particle size of 100 μm or less are extremely easily aggregated due to binding of interparticle bridges that are formed by a coating agent containing the binder
Data Source
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AI summary
The present invention provides a hydroxyalkyl cellulose having a viscosity of 1.10 mPa·s to 1.95 mPa·s in a 2%-concentration aqueous solution at 20°C, and a solid formulation containing the hydroxyalkyl cellulose.