Agglomerate Tablets with Polymers for Rapid Disintegration
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Solution Overview
Problem
Current pharmaceutical formulations for rapidly disintegrating tablets often fail to achieve rapid disintegration in the mouth, leave a gritty sensation, and lack mechanical stability, with existing products either being too soft or having low content uniformity.
Innovation Solution
The development of agglomerate tablets comprising 60-97% sugar or sugar alcohols, 1-25% disintegrants, 1-15% water-insoluble polymers, and 0-15% water-soluble polymers, along with an active ingredient, which disintegrate within 60 seconds, preferably within 30 seconds, and exhibit high mechanical strength and pleasant mouthfeel.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If conventional rapidly disintegrating tablet formulations are used, then disintegration speed is improved, but mechanical strength deteriorates (tablets are too soft)
Solution Approach 1:
The patent changes the physical and chemical parameters of the formulation by using specific ratios of water-soluble polymers (1-10% w/w), water-insoluble polymers (1-15% w/w), and sugar/sugar alcohols (60-97% w/w), along with controlling particle size and moisture content to achieve both rapid disintegration and high mechanical strength
Solution Approach 2:
The patent creates a composite tablet formulation combining multiple components with complementary properties: water-soluble polymers for disintegration, water-insoluble polymers for mechanical strength, and sugar/sugar alcohols as fillers, achieving synergistic effects that resolve the contradiction between softness and strength
2Speed
If disintegrants are added to achieve rapid disintegration, then disintegration time is reduced, but content uniformity deteriorates
Solution Approach 1:
The patent optimizes the quantity of disintegrants to 1-25% w/w and controls their particle size to maintain content uniformity while achieving rapid disintegration within 60 seconds
Solution Approach 2:
The patent ensures uniform distribution of disintegrants throughout the tablet matrix through proper mixing and granulation techniques, maintaining local homogeneity that prevents content uniformity issues while enabling rapid disintegration
3Speed
If coarse-particle disintegrants are used to reduce disintegration time, then disintegration speed is improved, but mouthfeel deteriorates (gritty sensation)
Solution Approach 1:
The patent controls the particle size of disintegrants to be fine particles rather than coarse particles, and optimizes the overall particle size distribution of the formulation to achieve rapid disintegration without creating a gritty sensation in the mouth
Solution Approach 2:
The patent uses fine-particle disintegrants that can uniformly distribute throughout the tablet and dissolve rapidly, providing local quality improvement by eliminating the gritty texture while maintaining disintegration speed
4Speed
If water-soluble polymers are increased to improve disintegration, then disintegration rate is improved, but mechanical strength deteriorates
Solution Approach 1:
The patent optimizes the concentration of water-soluble polymers to 1-10% w/w, which provides sufficient disintegration promotion while maintaining tablet mechanical strength through the balanced formulation with water-insoluble polymers and sugar/sugar alcohols
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 tablets achieve rapid disintegration, high mechanical strength, and content uniformity, with disintegration times under 60 seconds and hardness above 40 N, ensuring stability and pleasant mouthfeel, while maintaining reproducibility and avoiding gritty sensations.
Implementation Method 1
The invention relates to pharmaceutical formulations in the form of agglomerates for the production of rapidly disintegrating tablets
Implementation Method 2
1-25% by weight of a disintegrant
Data Source
AI summary
Pharmaceutical formulation in the form of agglomerates comprisingA) an excipient content composed ofa) 60-97% by weight of sugar or sugar alcohols,b) 1-25% by weight of a disintegrant,c) 1-15% by weight of water-insoluble, film-forming polymersd) 0-15% by weight of water-soluble polymers ande) 0-15% by weight of further pharmaceutically customary excipients the total of the components a) to e) being 100% by weight,andB) at least one active ingredient.