Agglomerated Cellulosic Excipient for Direct Compression
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Solution Overview
Problem
The pharmaceutical industry seeks a multi-purpose excipient that functions as a binder, diluent, and disintegrating agent for solid dosage forms, particularly for humidity- and heat-sensitive drugs, which can also be used in cosmetic applications and as a dietary fiber source, while minimizing the need for additional ingredients and improving production efficiency.
Innovation Solution
A novel agglomerated microcrystalline cellulose excipient II is produced through alkaline treatment of cellulose from agro-industrial residues at low temperatures in an inert atmosphere, followed by sodium hydroxide treatment, neutralization, and the addition of a binder, resulting in a pulp that can be spray dried or subjected to sequential granulation, offering enhanced properties as a diluent, binder, and disintegrating agent.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If multiple separate excipients are used for binder, diluent, and disintegrating agent functions, then each function can be optimized independently, but the number of ingredients increases and production complexity increases
Solution Approach 1:
The patent applies universality by developing a single excipient material that performs multiple functions simultaneously - serving as binder, diluent, and disintegrating agent in tablet formulations. This multi-functional excipient eliminates the need for separate ingredients for each function, reducing formulation complexity while maintaining optimized performance for all three roles through the unique properties of the modified cellulose structure
2Reliability
If conventional excipients are used for humidity- and heat-sensitive drugs, then production is possible, but production time increases and costs increase due to additional processing steps
Solution Approach 1:
The patent applies merging by combining multiple excipient functions into a single material that can be directly compressed with the drug substance. This eliminates the need for separate binder addition, diluent mixing, and disintegrating agent incorporation steps required by conventional excipients, thereby reducing production time and costs while maintaining drug stability through the inherent properties of the modified cellulose
3Ease of manufacture
If microcrystalline cellulose is used as diluent and binder, then direct compression is enabled, but additional disintegrating agents and lubricants are required
Solution Approach 1:
The patent applies universality by creating an excipient that combines the direct compression capabilities of microcrystalline cellulose with inherent disintegrating and lubricating properties. This single multi-functional material eliminates the need for separate disintegrating agents and lubricants, allowing direct compression while reducing the total number of ingredients required in the formulation
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 novel excipient enables rapid disintegration of tablets, improved flow and adhesiveness, and versatility in producing both pharmaceutical and cosmetic products, including immediate-release tablets and compact make-up powders, while serving as a dietary fiber source, thus addressing the need for a multifunctional excipient that reduces production time and costs.
Implementation Method 1
treating the cellulose powder with sodium hydroxide within -10 and 10°C in the presence of an inert atmosphere for its polymorphic transformation
Implementation Method 2
The resulting pulp contains a humidity within 60 and 90% and it is spray drying
Data Source
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AI summary
The invention relates to a process for producing a novel multi-purpose agglomerated cellulosic excipient. This excipient replaces many ingredients in the production of tablets due to the fact that it functions as a diluent, a disintegrating agent and an agglutinant, all in the same material. This material is therefore ideal for producing tablets in a dry process such as direct compression and dry granulation, saving production times and costs, especially in humidity-and heat-sensitive drugs. The tablets produced using said excipient disintegrate rapidly by explosion when they come into contact with water. In addition, said excipient can be used to produce loose and compact make-up powders due to its self-agglutinating and sensory properties on the skin, and also functions as a dispersant agent that can be used in the production of semisolid products. It can further be used to produce granules and beads or as a diluent in formulations of hard gelatin capsules, and since it is a source of high fiber, it is a good replacement for insoluble dietary fiber.