Bi-layer Coated API Particles for Taste Masking
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Solution Overview
Problem
Traditional fluidized bed coating processes for active pharmaceutical ingredients (APIs) often result in agglomeration of API particles, leading to unpleasant gritty mouth feel and high polymer loading, making dosages unpalatable and costly to produce.
Innovation Solution
A process involving a bi-layer coating of API particles with a first partially water-soluble polymer layer and a second water-insoluble polymer layer, using nanoparticles like silica to minimize agglomeration and reduce polymer loading, while maintaining taste masking and controlled release properties.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Object-affected harmful factors
If traditional fluidized bed coating processes are used to coat API particles, then taste masking is achieved, but agglomeration of API particles occurs leading to gritty mouth feel
Solution Approach 1:
The coating process is divided into multiple sequential stages: first a water-soluble polymer layer is applied, then a water-insoluble polymer layer is applied. This segmentation allows each layer to perform its specific function without causing agglomeration, as the water-soluble layer provides initial protection while the water-insoluble layer provides final taste masking without the drawbacks of traditional single-step coating
Solution Approach 2:
The invention uses a composite coating structure with two different polymer materials having complementary properties. The water-soluble polymer (e.g., HPMC) provides initial coating and protection, while the water-insoluble polymer (e.g., ethyl cellulose) provides the final taste masking barrier. This composite approach allows the coating to achieve taste masking without the agglomeration problems of traditional single-material coatings
2Object-affected harmful factors
If traditional coating methods are used to mask API taste, then high polymer loading is required, but this increases production cost and dosage form size
Solution Approach 1:
The coating process applies different polymer materials with different properties to different layers of the particle surface. The water-soluble polymer layer provides initial protection with lower polymer loading, while the water-insoluble polymer layer provides the primary taste masking function. This local differentiation of material properties allows efficient taste masking with reduced overall polymer loading compared to uniform high-loading coatings
Solution Approach 2:
By combining water-soluble and water-insoluble polymers in a layered composite structure, the invention achieves effective taste masking with lower total polymer loading. The water-insoluble layer provides the primary barrier function while the water-soluble layer provides structural support and controlled release properties, allowing each material to work at optimal concentrations rather than requiring high loading of a single material
3Ease of manufacture
If larger microcapsule sizes are used for chewable tablets, then manufacturing and packaging become easier and less expensive, but the microcapsules may fracture during chewing and release drug
Solution Approach 1:
The bi-layer composite coating structure provides enhanced mechanical integrity for larger microcapsules. The water-soluble polymer layer provides flexibility and elasticity, while the water-insoluble polymer layer provides structural strength. This composite structure allows larger microcapsule sizes to be used without fracturing during chewing, as the two materials work together to distribute and absorb mechanical stresses
Solution Approach 2:
The water-soluble polymer layer acts as a cushioning layer that absorbs and distributes mechanical stresses before they reach the water-insoluble polymer layer and the API core. This prior cushioning effect prevents fracture of larger microcapsules during chewing, allowing the use of larger sizes for easier manufacturing and packaging while maintaining integrity
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 process effectively reduces agglomeration, lowers polymer loading, and enhances the palatability and production efficiency of taste-masked API powders, ensuring quick release in the digestive tract and maintaining the desired taste masking attributes.
Implementation Method 1
coating the at least partially coated core particles in a fluidized bed with a first polymer layer
Implementation Method 2
a first polymer layer from a first polymer; and coating the first polymer layer with a water insoluble second polymer layer
Data Source
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AI summary
A taste masked particulate pharmaceutical formulation include a core that comprises an active pharmaceutical ingredient; at least a partial nanoparticle material layer on the core that comprises a nanoparticle material with a median particle size not greater than 100 nm; a first polymer layer that is at least partially water soluble and a second polymer layer that is water insoluble. The active pharmaceutical ingredient is completely released in 30 minutes in the USP Dissolution Test. A process of making the particulate pharmaceutical formulation using sequential fluidized bed coating steps under controlled conditions is also described.