Granulated Composite for Rapid Release Tablets
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Solution Overview
Problem
Orally rapidly disintegrating tablets face challenges with reduced hardness and prolonged disintegration time due to moisture absorption, affecting storage stability and ease of administration, especially for patients with low swallowing ability.
Innovation Solution
A granulated composite comprising low-substituted hydroxypropyl cellulose and D-mannitol with low D-sorbitol content, combined with a drug, is produced using a direct dry-tableting method without special equipment, enhancing binding capability and disintegrability while maintaining stability under humid conditions.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Productivity
If direct dry-tableting method is used to produce orally rapidly disintegrating tablet, then productivity is improved and special apparatus is not needed, but tablet hardness is reduced and disintegration time is prolonged during storage
Solution Approach 1:
The invention changes the chemical composition parameters of the granulated composite by specifying low-substituted hydroxypropyl cellulose with degree of substitution of 0.02-0.08 and D-mannitol with D-sorbitol content of 0.9% by weight or less. These parameter changes enable the tablet to maintain both high hardness and rapid disintegration during storage while using the simple direct dry-tableting method.
Solution Approach 2:
The invention uses a composite material system consisting of low-substituted hydroxypropyl cellulose and D-mannitol with controlled D-sorbitol content. This specific composite combination provides both binding capability for tablet hardness and disintegrability for rapid dissolution, resolving the contradiction between mechanical strength and disintegration performance during storage.
2Strength
If granulated composite with high binding capability is used to improve tablet hardness, then strength is improved, but disintegration time is prolonged
Solution Approach 1:
The invention optimizes the degree of substitution of low-substituted hydroxypropyl cellulose to 0.02-0.08 and controls D-sorbitol content in D-mannitol to 0.9% by weight or less. These parameter changes create a balance where the material provides sufficient binding for tablet hardness while maintaining rapid disintegration capability during storage.
Solution Approach 2:
The invention applies different functional properties to different aspects of the granulated composite: low-substituted hydroxypropyl cellulose provides binding capability for hardness, while the controlled D-mannitol composition ensures rapid disintegration. This local quality differentiation resolves the contradiction between strength and disintegration speed.
3Ease of operation
If tablet is designed for rapid disintegration in oral cavity, then disintegrability is improved, but tablet hardness is reduced making it prone to breakage during production or transport
Solution Approach 1:
The invention changes the substitution degree parameter of hydroxypropyl cellulose to 0.02-0.08 and controls D-sorbitol content to 0.9% by weight or less. These parameter changes enable the tablet to simultaneously achieve high hardness for breakage resistance and rapid disintegration for ease of administration.
Solution Approach 2:
The composite of low-substituted hydroxypropyl cellulose and controlled D-mannitol provides dual functionality: sufficient mechanical strength for handling and transport, plus rapid disintegration in the oral cavity. This composite material system resolves the contradiction between hardness and disintegrability.
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 resulting tablets exhibit high hardness, rapid disintegration, and excellent storage stability, ensuring ease of administration and handling, even under humid conditions, without requiring special technology or apparatus.
Implementation Method 1
a granulated composite comprising low-substituted hydroxypropyl cellulose and D-mannitol... excellent in binding capability
Implementation Method 2
since the orally rapidly disintegrating tablet sometimes has a reduced hardness and a prolonged disintegration time owing to moisture absorbed thereby when exposed to a humidified environment after opening
Implementation Method 3
The orally rapidly disintegrating tablet is required to have a short disintegration time in the oral cavity
Data Source
AI summary
Provided is a rapid release tablet excellent in binding capability and disintegrability and also excellent in storage stability and the like. More specifically, provided are a granulated composite comprising low-substituted hydroxypropyl cellulose having a degree of hydroxypropoxy substitution of from 5 to 16% by weight and D-mannitol, wherein the D-mannitol contains 0.9% by weight or less of D-sorbitol; a rapid release tablet comprising the granulated composite and a drug; and a method for producing a granulated composite comprising the steps of: mixing low-substituted hydroxypropyl cellulose having a degree of hydroxypropoxy substitution of from 5 to 16% by weight, first D-mannitol, and water to obtain an aqueous dispersion, and granulating while adding the aqueous dispersion to second D-mannitol, wherein the first D-mannitol and the second D-mannitol contain 0.9% by weight or less of D-sorbitol in total.