Functional Polymer Film-Coated Drug Particles for Orally Disintegrating Tablets
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Solution Overview
Problem
Conventional methods for manufacturing orally disintegrating tablets with high drug content result in large particle diameters and low moldability, requiring excessive excipients to achieve suitable tablet hardness, which complicates the manufacturing process.
Innovation Solution
The use of spray drying fluidized bed granulation to produce bare drug particles with high drug content (70% or more by weight) without core particles, followed by coating with a functional polymer film to achieve high drug content and small particle diameters, along with a broad particle size distribution, enhancing moldability and reducing the need for high-moldability excipients.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional layering methods are used to produce core fine particles with functional films, then the particles have controlled drug release and masking properties, but the particle diameter becomes large and drug content ratio decreases
Solution Approach 1:
The invention extracts and eliminates the core particles (crystalline cellulose or lactose) from the conventional three-layer structure, retaining only the essential functional components (drug layer and functional polymer film). This extraction reduces particle size while maintaining the critical functions of controlled drug release and taste masking.
Solution Approach 2:
The invention uses composite material structure where the core fine particles consist of drug particles coated with functional polymer film. This composite structure integrates the drug and functional film in a way that achieves high drug content (70% or more by weight) while maintaining small particle diameter (400 μm or less).
2Quantity of substance
If high drug content particles are produced by conventional methods, then the drug content increases, but the number of components other than drug increases, making tablets large and difficult to take
Solution Approach 1:
The invention removes unnecessary core particles and excipients from the conventional formulation, achieving high drug content (70% or more by weight) in the core fine particles. This extraction allows high drug content while keeping tablet size small and suitable for oral administration.
Solution Approach 2:
The invention changes the formulation parameters by eliminating core particles and using only essential components (drug and functional polymer). This parameter change enables high drug content while maintaining small tablet size and improved patient compliance.
3Reliability
If conventional core particles and polymeric materials are used in large amounts, then the functional film can be applied, but the tablet becomes large and moldability deteriorates
Solution Approach 1:
The invention extracts and eliminates the unnecessary core particles (crystalline cellulose, lactose) from the conventional structure, retaining only the functional polymer film and drug components. This extraction improves moldability while preserving the essential functions of the functional film.
Solution Approach 2:
The invention applies functional polymer film with specific properties (water-insoluble but water-permeable) only where needed on the drug particles, rather than using bulk polymeric materials throughout the formulation. This local application maintains film functionality while improving overall tablet moldability.
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
This approach allows for the production of orally disintegrating tablets with high drug content and improved moldability, enabling the manufacture of small-sized tablets with sufficient hardness and targeted disintegration properties using reduced amounts of excipients.
Implementation Method 1
spray drying fluidized bed granulation to produce bare drug particles with high drug content
Implementation Method 2
coating with a functional polymer film to achieve high drug content and small particle diameters
Data Source
Figure 1(a)~1
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AI summary
Provided are functional drug-containing particles which can be compressed into tablets and in particular, to orally disintegrating tablets by employing any of a dry molding method, a wet molding method, or a humidifying drying method. The functional drug-containing particles comprise substantially spherical drug-containing particles essentially including drug and a binder, the functional drug-containing particles including a functional polymer film selected from the group consisting of an enteric film, a release control film, and a bitter taste masking film, an average particle diameter of said functional drug-containing particles being 400 µm or less, a particle diameter ratio D90/D10 of the functional drug-containing particles with respect to particle size distribution calculated on a volumetric basis being 1.65 or more, or a coefficient of variation in particle diameters being 24% or more.