Rapidly Disintegrating Tablet Formulation via Fine Particle Agglomeration
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Solution Overview
Problem
Existing rapidly disintegrating tablets fail to meet requirements of quick disintegration in the mouth, pleasant mouthfeel, and mechanical stability, often resulting in low breaking strength and friability, with existing formulations either being inadequate or producing an unpleasant sandy sensation.
Innovation Solution
The development of pharmaceutical formulations comprising 60-97% sugar or sugar alcohols, 1-25% cross-linked polyvinylpyrrolidone, 1-15% water-insoluble polymers, and 0-15% water-soluble polymers or other excipients, which are produced through agglomeration processes like fluidized bed or spray drying, using water-insoluble film-forming polymers like polyvinyl acetate to enhance disintegration and mechanical strength.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If coarse-grained cross-linked polyvinylpyrrolidone is used as disintegrant, then disintegration time is reduced, but mouthfeel becomes unpleasant and sandy
Solution Approach 1:
The patent changes the particle size parameter of cross-linked polyvinylpyrrolidone from coarse-grained (producing sandy mouthfeel) to fine-grained (≤50 μm, preferably ≤30 μm), thereby maintaining rapid disintegration while eliminating the unpleasant sandy sensation in the mouth
Solution Approach 2:
The patent applies different particle size qualities to different functional requirements: fine particles for mouthfeel and smooth texture, while maintaining sufficient particle presence for disintegration function, thus optimizing both sensory and functional properties
2Duration of action of moving object
If high proportion of coarse-grained disintegrant (15% by weight) is used, then disintegration speed increases, but mechanical strength decreases
Solution Approach 1:
The patent optimizes the particle size parameter of the disintegrant to fine grains (≤50 μm), which allows achieving rapid disintegration at lower dosages (1-25% by weight) while maintaining tablet mechanical strength, unlike coarse-grained disintegrants that require higher dosages and weaken tablets
Solution Approach 2:
The patent creates a composite formulation combining fine cross-linked polyvinylpyrrolidone with water-insoluble polymers and sugars/sugar alcohols, where the fine disintegrant particles work synergistically with other components to achieve both rapid disintegration and adequate mechanical strength
3Ease of manufacture
If direct tabletting is used instead of wet granulation, then manufacturing simplicity increases, but mechanical strength and stability decrease
Solution Approach 1:
The patent changes the particle size parameter of the excipients (especially cross-linked polyvinylpyrrolidone to ≤50 μm) to enable direct tabletting to produce tablets with breaking strengths >50 N, matching or exceeding the quality of wet granulated tablets while simplifying manufacturing
Solution Approach 2:
The patent replaces the wet granulation mechanical process with direct tabletting, using fine particle size excipients that provide sufficient cohesion and mechanical strength without requiring binding agents or granulation steps
4Duration of action of moving object
If rapid disintegration is achieved using conventional formulations, then disintegration time is reduced, but tablet stability and appearance deteriorate
Solution Approach 1:
The patent develops a composite formulation combining fine cross-linked polyvinylpyrrolidone (1-25%), water-insoluble polymers (1-15%), and sugars/sugar alcohols (60-97%), where the water-insoluble polymer matrix maintains tablet stability and appearance while the fine disintegrant ensures rapid disintegration within 30 seconds
Solution Approach 2:
The patent applies different functional qualities to different components: water-insoluble polymers provide structural stability and maintain appearance, while fine cross-linked polyvinylpyrrolidone particles localized throughout the matrix provide rapid disintegration without compromising overall tablet integrity
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 formulations achieve rapid disintegration within 20-40 seconds, high mechanical strength with breaking strengths over 50 N, and a pleasant mouthfeel, while maintaining stability and appearance, even under wet conditions, significantly improving upon existing technologies.
Implementation Method 1
water-insoluble film-forming polymers like polyvinyl acetate to enhance disintegration and mechanical strength
Implementation Method 2
produced through agglomeration processes like fluidized bed or spray drying
Implementation Method 3
1 - 25% by weight of a cross-linked polyvinylpyrrolidone
Data Source
AI summary
The invention relates to a pharmaceutical formulation in the form of agglomerates containing a) 60 - 97 % by weight of sugar or sugar alcohols, b) 1 - 25 % by weight of cross-linked polyvinylpyrrolidone, 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 other pharmaceutically suitable adjuvants, the sum of components a) to e) adding up to 100 % by weight.