Silica-Free Impregnation Tablets for API Retention and Release
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Solution Overview
Problem
Existing tablet producing methods using porous inorganic particles with silanol groups interact with active pharmaceutical ingredients, leading to poor release properties, necessitating a new method that avoids silica and ensures excellent permeability and retention of active ingredients.
Innovation Solution
A tablet comprising a monosaccharide and/or disaccharide, such as δ-form D-mannitol, and a water-insoluble polymer, which allows for impregnation with active pharmaceutical ingredients, enhancing permeability and retention.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If porous inorganic particles (silica) are used as carriers for active pharmaceutical ingredients, then the tablet structure can be formed, but the silanol groups on silica surface interact with active ingredients and release properties become poor
Solution Approach 1:
The patent removes the problematic silica carrier and its silanol groups from the tablet composition, replacing it with a silica-free system using only excipients like microcrystalline cellulose, lactose, and starch that do not interact harmful with active ingredients, thereby eliminating the harmful interaction while maintaining tablet structure
Solution Approach 2:
The patent changes the fundamental parameter of carrier material from porous inorganic silica to organic excipients with different chemical properties, altering the surface chemistry to eliminate silanol group interactions while maintaining the carrier function through alternative mechanisms
2Reliability
If porous inorganic particles are used, then the tablet can be formed, but the active ingredient release depends only on natural dispersion which is slow
Solution Approach 1:
The patent employs excipients with inherent porosity and hygroscopic properties (such as microcrystalline cellulose, lactose, and starch) that can absorb gastrointestinal fluids and expand, creating channels for rapid active ingredient release without requiring porous silica, thus achieving fast release through fluid absorption and swelling mechanisms
Solution Approach 2:
The patent utilizes the phase transition of excipients from dry solid state to hydrated gel state upon contact with gastrointestinal fluids, where the excipients absorb water and swell, creating a gel matrix that facilitates rapid diffusion and release of active ingredients
3Ease of operation
If a tablet is designed to be permeable to active pharmaceutical ingredients, then impregnation is improved, but retention ability may be compromised
Solution Approach 1:
The patent creates a composite tablet system combining multiple excipients (microcrystalline cellulose, lactose, starch, binders, disintegrants) with complementary properties where the matrix provides both permeability for impregnation and retention through interconnected pore structures and binding mechanisms, achieving simultaneous improvement of both characteristics
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 tablet exhibits excellent permeability and retention of active pharmaceutical ingredients, preventing interactions and ensuring stable incorporation, even for unstable ingredients, while maintaining mechanical strength and rapid disintegration.
Implementation Method 1
the monosaccharide and/or disaccharide comprises δ-form D-mannitol... makes it easier to impregnate the tablet for impregnation with an active pharmaceutical ingredient, and easier for the impregnated active pharmaceutical ingredient to be retained in the tablet for impregnation
Data Source
Figure 1
AI summary
An object of the present invention is to provide a tablet with excellent permeability and retention ability of active pharmaceutical ingredients. This object can be achieved with a tablet for being impregnated with an active pharmaceutical ingredient, with the tablet comprising a monosaccharide and/or disaccharide.