Dispersible Daprodustat Tablet Composition for Small-Volume Suspension
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Solution Overview
Problem
Conventional tablets pose swallowing difficulties for pediatric, geriatric, and certain patient groups, and existing dispersible tablets either take too long to disintegrate or form soft masses, making them unsuitable for small volumes and poor mouthfeel.
Innovation Solution
A dispersible tablet design with specific granule and extragranular component compositions, including microcrystalline cellulose, silicified microcrystalline cellulose, and disintegrants, achieving a solid fraction of ≤0.9 and surface area ≤615 mm², allowing rapid disintegration in ≤3 minutes to form a freely flowing suspension.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Volume of stationary object
If dispersible tablets are designed to disintegrate rapidly in very small volumes (1-5 ml), then the volume of dispersion is reduced and fluid intake is restricted, but the suspension formed may become a soft mass with poor mouthfeel
Solution Approach 1:
The patent applies parameter changes by precisely controlling the particle size distribution of granules (≤140 microns with specific density 0.4-0.6 g/mL) and adjusting the solid fraction (≤0.9) to achieve optimal disintegration in small volumes while maintaining good mouthfeel. This resolves the contradiction by finding the right parameter values that satisfy both small volume requirement and suspension quality
Solution Approach 2:
The patent uses composite materials by combining specific excipients including microcrystalline cellulose, silicified microcrystalline cellulose, and specific binders in defined ratios. This composite formulation enables the tablet to disintegrate rapidly in small volumes while forming a free-flowing suspension with acceptable mouthfeel, rather than a soft mass
2Speed
If the tablet contains high levels of insoluble materials to facilitate rapid disintegration, then disintegration speed is improved, but the mouthfeel of the suspension deteriorates
Solution Approach 1:
The patent applies parameter changes by precisely controlling the particle size distribution of granules (≤140 microns with specific density 0.4-0.6 g/mL) and adjusting the solid fraction (≤0.9) to achieve optimal disintegration in small volumes while maintaining good mouthfeel. This resolves the contradiction by finding the right parameter values that satisfy both small volume requirement and suspension quality
Solution Approach 2:
The patent employs porous materials through the use of silicified microcrystalline cellulose which provides a porous structure that facilitates rapid water penetration and disintegration. The porous structure allows quick disintegration while the controlled particle size ensures the resulting suspension maintains good mouthfeel without forming a soft mass
3Ease of manufacture
If conventional tablets are used, then manufacturing is simple, but swallowing difficulties occur in pediatric, geriatric, and certain patient groups
Solution Approach 1:
The patent applies segmentation by dividing the tablet into granules with specific size distribution (≤140 microns). This segmentation allows the tablet to disintegrate rapidly in small volumes of liquid, making it suitable for pediatric, geriatric, and patients with swallowing difficulties, while still using conventional tablet manufacturing processes
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 rapidly in small volumes, forming a palatable suspension with acceptable mouthfeel, suitable for pediatric and challenging patient groups, and can be administered via syringe or feeding tube.
Implementation Method 1
the extragranular component comprises at least 20% (w/w in the dispersible tablet) silicified microcrystalline cellulose and a disintegrant
Implementation Method 2
which dispersible tablet comprises an extra-granular component and at least 40% (w/w in the dispersible tablet) granules
Data Source
AI summary
The present disclosure relates to a dispersible tablet capable of disintegrating in very small volumes of water rapidly (e.g. within a period of 3 minutes) to form a suspension that is free flowing and has an acceptable mouthfeel. A dispersible tablet of daprodustat and medical uses of this tablet are also disclosed.