Orally Disintegrating Tablet Hardness and Rapid Disintegration
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Solution Overview
Problem
Current orally disintegrating tablets do not effectively combine rapid disintegration with sufficient hardness for production, transportation, and use, while also ensuring good taste and storage stability, particularly for edoxaban-based formulations.
Innovation Solution
An orally disintegrating tablet comprising edoxaban tosylate hydrate, 0.1 to 15% fumaric acid, 0.1 to 2.0% hydroxypropyl cellulose, and one or more disintegrants such as carmellose or pregelatinized starch, which are compression molded to achieve rapid disintegration and solubility with sufficient hardness.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If the tablet is made to disintegrate rapidly in the mouth, then patient compliance and ease of administration are improved, but the tablet hardness and mechanical strength deteriorate, making it difficult to withstand production and transportation
Solution Approach 1:
The patent applies parameter changes by carefully controlling the content ranges of specific excipients: microcrystalline cellulose (20-70 wt%), hydroxypropyl cellulose (0.1-5 wt%), and disintegrants (5-30 wt%). By adjusting these parameters within optimal ranges, the formulation achieves a balance where the tablet maintains sufficient hardness for handling while ensuring rapid disintegration (within 60 seconds) in the oral cavity through the synergistic action of these components.
Solution Approach 2:
The patent employs composite materials by combining multiple excipients with complementary functions: microcrystalline cellulose provides structural framework and hardness, hydroxypropyl cellulose acts as a binder and disintegration promoter, and disintegrants (such as crospovidone or sodium starch glycolate) create rapid water penetration channels. This composite formulation achieves both mechanical integrity and rapid disintegration properties that individual materials cannot provide alone.
2Ease of manufacture
If the tablet uses simple compression molding for easy production, then manufacturing complexity is reduced, but the tablet may lack sufficient hardness and structural integrity
Solution Approach 1:
The patent applies preliminary action by pre-optimizing the formulation composition before compression molding. The specific ratio of microcrystalline cellulose, hydroxypropyl cellulose, and disintegrants is predetermined to ensure that simple compression molding (without complex granulation or drying steps) produces tablets with adequate hardness. The formulation is designed so that the excipients self-organize into a structurally sound matrix during compression, eliminating the need for additional processing steps.
3Productivity
If the tablet is designed to dissolve rapidly in water, then dissolution properties are improved, but the tablet hardness and storage stability deteriorate
Solution Approach 1:
The patent applies local quality by creating different functional zones within the tablet structure. The disintegrant particles and hydroxypropyl cellulose create localized water penetration channels and swelling zones that rapidly absorb water and facilitate disintegration. Meanwhile, the microcrystalline cellulose matrix provides a stable, hard structural framework that maintains tablet integrity during storage. This spatial differentiation of functions allows rapid dissolution without compromising storage stability.
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 tablet disintegrates within 60 seconds, has excellent dissolution properties, and maintains hardness during production, transportation, and storage, making it suitable for elderly and dysphagic patients, with improved taste and stability.
Implementation Method 1
an orally disintegrating tablet comprising (A) edoxaban tosylate hydrate, (B) 0.1 to 15% by weight of fumaric acid relative to the total weight of the tablet, (C) 0.1 to 2.0% by weight of hydroxypropyl cellulose
Implementation Method 2
one or more disintegrants selected from the group consisting of carmellose, crospovidone, carmellose calcium, croscarmellose sodium, corn starch, sodium starch glycolate, and pregelatinized starch
Data Source
AI summary
An orally disintegrating tablet comprising edoxaban, a pharmacologically acceptable salt thereof, or a solvate thereof is provided. An orally disintegrating tablet comprising (A) edoxaban, a pharmacologically acceptable salt thereof, or a solvate thereof, (B) an organic acid, (C) 0.1 to 2.0% by weight of a water-soluble polymer relative to the total weight of the tablet, and (D) a disintegrant.