Rapidly Disintegrating Tablet Formulation with Micronized Disintegrant
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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 and uniformly, while also being difficult to produce with high content uniformity.
Innovation Solution
A pharmaceutical formulation comprising 60-97% sugar or sugar alcohols, 1-25% cross-linked polyvinylpyrrolidone or similar disintegrants, 1-15% water-insoluble polymers, and optional water-soluble polymers and excipients, processed into compacts that disintegrate within 60 seconds, preferably within 30 seconds, with enhanced mechanical strength and pleasant mouthfeel.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Loss of time
If cross-linked polyvinylpyrrolidone and coarse-grained disintegrants are used to achieve rapid disintegration, then disintegration time is reduced to within 60 seconds, but mechanical strength decreases to approx. 40N and sandy mouthfeel occurs
Solution Approach 1:
The patent changes the particle size parameter of the disintegrant from coarse-grained to fine-grained (micronized), and adjusts the disintegrant concentration to 5-20% by weight. This parameter optimization allows achieving disintegration within 60 seconds while maintaining mechanical strength above 40N and eliminating sandy mouthfeel
Solution Approach 2:
The patent uses a composite formulation combining fine-grained cross-linked polyvinylpyrrolidone disintegrant with sugar or sugar alcohol base material, and optionally water-soluble polymers. This composite approach enables simultaneous achievement of rapid disintegration, adequate mechanical strength, and pleasant mouthfeel
2Loss of time
If high proportion of coarse-grained disintegrant (15% by weight) is used to ensure disintegration, then disintegration is achieved, but mechanical strength decreases to 7% breaking strength and sandy mouthfeel is produced
Solution Approach 1:
The patent changes the critical particle size parameter of the disintegrant to fine-grained/micronized form, and optimizes the disintegrant content to 5-20% by weight. This eliminates the sandy mouthfeel while maintaining rapid disintegration capability within 60 seconds
Solution Approach 2:
The patent uses water-soluble polymers that dissolve completely during disintegration, providing temporary structural support during compression but disappearing during use to avoid sandy mouthfeel, enabling both high disintegration speed and smooth mouthfeel
3Ease of manufacture
If direct tabletting is used to simplify production, then manufacturing complexity is reduced, but content uniformity and mechanical strength are compromised
Solution Approach 1:
The patent performs preliminary micronization of the disintegrant before formulation, and pre-optimizes the ingredient ratios with sugar or sugar alcohol as base material. This preliminary preparation enables direct tabletting to achieve both manufacturing simplicity and content uniformity without requiring complex granulation processes
4Loss of time
If water-soluble polymers are added to improve disintegration, then disintegration speed increases, but mechanical strength and structural stability may be reduced
Solution Approach 1:
The patent optimizes the concentration of water-soluble polymers and their molecular weight parameters, balancing the competing requirements of rapid disintegration and structural stability during storage and handling
Solution Approach 2:
The patent creates a composite system where water-soluble polymers work synergistically with fine-grained disintegrants and sugar base material, achieving enhanced disintegration speed while maintaining adequate structural stability through the combined effects of the components
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 in the mouth, maintain mechanical stability, and ensure uniform active ingredient distribution, with disintegration times under 60 seconds and breaking strengths exceeding 40 N, minimizing friability and sandy mouthfeel issues.
Implementation Method 1
water-insoluble polymers which form a film matrix
Implementation Method 2
disintegrants... so that a physical mixture is created. The tablets should disintegrate in the oral cavity within 60 seconds
Implementation Method 3
consisting of 60 - 97% by weight of at least one sugar or sugar alcohol
Implementation Method 4
processed into compacts that disintegrate within 60 seconds, preferably within 30 seconds, with enhanced mechanical strength and pleasant mouthfeel
Data Source
AI summary
The invention relates to a pharmaceutical formulation in the form of compacts containing A) an agglomerated auxiliary agent fraction consisting of a1) 60 - 97 % by weight of sugar or sugar alcohols, a2) 1 - 25 % by weight of a disintegration agent selected from the group consisting of crospovidone, croscarmellose, sodium carboxymethyl starch and L-hydroxypropyl cellulose, a3) 1 - 15 % by weight of water insoluble film-forming polymers, a4) 0 - 15 % by weight of water-soluble polymers, and a5) 0 - 15 % by weight of additional conventional pharmaceutical adjuvants, the sum of the components a1) to a5) totalling 100 % by weight, B) at least one active ingredient, C) 0 to 10 % by weight, in relation to the total quantity and A) to D) of a lubricant or mould release agent, and D) optionally additional pharmaceutical auxiliary agents.