Rapidly Disintegrating Tablets via Fine-Grained Disintegrants
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Solution Overview
Problem
Existing rapidly disintegrating tablets lack mechanical strength, often produce an unpleasant sandy mouthfeel, and fail to disintegrate quickly enough, while also being difficult to produce efficiently.
Innovation Solution
Formulations comprising 60-97% sugar or sugar alcohols, 1-25% disintegrants like croscarmellose, 1-15% water-insoluble film-forming polymers, and optional water-soluble polymers and excipients, produced through agglomeration processes such as fluidized bed or spray drying, which enhance disintegration time and mechanical stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Loss of time
If spray-dried mannitol and cross-linked PVP are used to create rapidly disintegrating tablets, then disintegration time is reduced to within 60 seconds, but mechanical strength decreases to approx. 40N and sandy mouthfeel is produced
Solution Approach 1:
The patent changes the particle size parameter of the disintegrant from coarse-grained to fine-grained (average particle size 10-50 μm), which fundamentally alters the tablet properties. This parameter change enables achieving both rapid disintegration (within 30 seconds) and high mechanical strength (>50N breaking strength), resolving the contradiction between speed and strength that existed with coarse-grained disintegrants
Solution Approach 2:
The patent creates a composite formulation combining fine-grained disintegrant (1-25% by weight), water-insoluble polymer (1-15% by weight), and sugar/sugar alcohol (60-97% by weight). This composite structure allows the fine-grained disintegrant to provide rapid disintegration while the water-insoluble polymer matrix maintains mechanical integrity, achieving both quick disintegration and high strength simultaneously
2Loss of time
If high proportion of coarse-grained disintegrant is used, then disintegration is enhanced, but mechanical strength decreases and sandy mouthfeel is produced
Solution Approach 1:
The patent fundamentally changes the particle size parameter of the disintegrant from coarse-grained to fine-grained (average particle size 10-50 μm). This parameter change eliminates the sandy mouthfeel caused by coarse particles while maintaining rapid disintegration capability, as the fine particles can still effectively promote disintegration without providing a gritty sensation in the mouth
3Ease of manufacture
If direct tabletting is used, then production ease is improved, but mechanical strength may be insufficient to withstand packaging and transport
Solution Approach 1:
The patent develops a composite formulation specifically optimized for direct tabletting: fine-grained disintegrant (1-25% by weight), water-insoluble polymer (1-15% by weight), and sugar/sugar alcohol (60-97% by weight). This composite structure provides sufficient mechanical strength (>50N breaking strength) to withstand packaging and transport while maintaining the simplicity of direct tabletting production
Solution Approach 2:
The patent optimizes the particle size parameter of the disintegrant to fine-grained (10-50 μm) and adjusts the formulation ratios to achieve the right balance between compressibility and mechanical strength. This allows direct tabletting to produce tablets with sufficient strength for commercial distribution while keeping the manufacturing process simple and efficient
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 disintegrate within 20-40 seconds, have high mechanical strength (>50N breaking strength), and a pleasant mouthfeel, with improved reproducibility and ease of production.
Implementation Method 1
water-insoluble film-forming polymers
Implementation Method 2
the tablets disintegrate within 20-40 seconds
Implementation Method 3
disintegrants like croscarmellose, cross-linked sodium carboxymethyl starch, and L-hydroxypropyl cellulose
Implementation Method 4
disintegrating agent selected from the group consisting of croscarmellose, cross-linked sodium carboxymethyl starch and L-hydroxypropyl cellulose
Implementation Method 5
produced through agglomeration processes such as fluidized bed or spray drying
Implementation Method 6
spray drying
Implementation Method 7
fluidized bed
Data Source
AI summary
The invention relates to a pharmaceutical formulation in the form of compacts containing a) 60 - 97 % by weight of sugar or sugar alcohols, b) 1 - 25 % by weight of a disintegration agent selected from the group consisting of croscarmellose, sodium carboxymethyl starch and L-hydroxypropyl cellulose, c) 1 - 15 % by weight of water insoluble film-forming polymers, d) 0 - 15 % by weight of water-soluble polymers, and e) 0 - 15 % by weight of additional conventional pharmaceutical adjuvants, the sum of the components a) to e) totalling 100 % by weight.