Orally Disintegrating Tablet with Mannitol Binding
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Existing orally disintegrating tablets with high active ingredient concentrations face challenges in achieving both rapid disintegrability and sufficient strength for handling and automatic packaging, as they often require reduced amounts of excipients and disintegrants, compromising either property.
Innovation Solution
A tablet composition and production method involving granulation of the active ingredient with a binding solution containing mannitol and corn-derived pregelatinized starch, combined with at least one disintegrant such as cornstarch, hydroxypropylstarch, or crospovidone, followed by compression molding, to achieve rapid disintegration and adequate strength.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If the amount of excipient and disintegrant is reduced to increase active ingredient concentration, then the active ingredient content is improved, but the rapid-disintegrability and tablet strength deteriorate
Solution Approach 1:
The patent changes the chemical composition parameters of the binding solution by specifying precise ratios of mannitol (5-20 wt%) and pregelatinized starch (80-95 wt%), along with controlled amounts of disintegrants (crospovidone 0.1-5 wt%, carmellose 0.1-5 wt%). These parameter adjustments enable the tablet to achieve both high active ingredient content (≥25 wt%) and sufficient mechanical strength (absolute hardness ≥1.8 N/mm²) without requiring traditional high amounts of excipients.
Solution Approach 2:
The patent creates a composite binding system combining mannitol (a sugar alcohol providing structural support) with pregelatinized starch (a modified starch providing binding and disintegration properties). This composite material approach allows the formulation to simultaneously achieve tablet strength for handling and rapid disintegration in the oral cavity, resolving the contradiction between strength and disintegrability while maintaining high active ingredient concentration.
2Quantity of substance
If the amount of excipient and disintegrant is reduced to increase active ingredient concentration, then the active ingredient content is improved, but the rapid-disintegrability in oral cavity deteriorates
Solution Approach 1:
The patent optimizes disintegrant parameters by incorporating specific types (crospovidone and/or carmellose) at controlled concentrations (0.1-5 wt% each). These disintegrants work synergistically with the pregelatinized starch in the binding solution to ensure rapid tablet disintegration (within 30 seconds) in the oral cavity, even when active ingredient content is high (≥25 wt%).
Solution Approach 2:
The patent utilizes the phase transition properties of pregelatinized starch, which undergoes gelatinization upon contact with saliva moisture. This phase change from a dry, bound state to a hydrated, expanded state creates rapid disintegration channels, enabling the tablet to break down quickly in the oral cavity despite high active ingredient content and reduced traditional disintegrant amounts.
3Ease of manufacture
If traditional binding solutions are used, then the manufacturing process is simple, but the tablet strength and disintegrability cannot be simultaneously optimized
Solution Approach 1:
The patent establishes precise parameter ranges for the binding solution components (mannitol 5-20 wt%, pregelatinized starch 80-95 wt%, disintegrants 0.1-5 wt% each) that can be applied using conventional granulation and compression equipment. This parameter optimization ensures consistent tablet performance (absolute hardness ≥1.8 N/mm², disintegration ≤30 seconds) while maintaining manufacturing simplicity and compatibility with existing production lines.
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 method results in tablets that are rapidly disintegrated in the oral cavity with a disintegration time of 40 seconds or less and an absolute hardness of 1.8 N/mm2 or more, improving compliance for children and elderly individuals with decreased swallowing ability.
Implementation Method 1
granulating a powder containing an active ingredient with a binding solution containing mannitol and corn-derived pregelatinized starch
Implementation Method 2
adding at least one kind of disintegrant selected from cornstarch, hydroxypropylstarch, carmellose and crospovidone to the granules
Data Source
AI summary
The invention relates to a tablet which is rapidly disintegrated in an oral cavity containing an active ingredient at a high content and a production method thereof. That is, the present invention provides a tablet which is rapidly disintegrated in an oral cavity containing an active ingredient in not less than 25% of the total weight, having a disintegration time of within 40 seconds and an absolute hardness of 1.8 N/mm2 or more, which is obtained by granulating a powder containing an active ingredient with a binding solution containing mannitol and corn-derived pregelatinized starch, mixing the resulting granules with at least one kind of a disintegrant selected from cornstarch, hydroxypropylstarch, carmellose and crospovidone, and compression molding the mixture.