Crystalline Polyol Microspheres for Uniform Pharmaceutical Coating
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Solution Overview
Problem
Existing pharmaceutical beads are either reactive or insoluble, leading to incompatibility with active substances, loss of API, and limitations in size and surface smoothness, which affect the release of active substances and the manufacturing process.
Innovation Solution
Development of microspheres that are 100% soluble, perfectly spherical, with a uniform surface and limited peak to valley roughness, as small as 10 μm, and composed of a single crystal structure with low internal voids, low hygroscopicity, and moisture content less than 1%.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Shape
If conventional granulation process is used to make polyol beads, then beads can be formed with binder solution, but the surface becomes rough with crevices and bumps, and internal porosity is created
Solution Approach 1:
The invention changes the physical state of the polyol from solid particles to completely liquefied state during bead formation. By melting the polyol and forming beads from the liquid state, the process eliminates the rough surfaces and internal porosity created by conventional granulation of solid particles, achieving smooth, uniform surfaces without crevices or bumps.
Solution Approach 2:
The invention utilizes phase transition of polyol from solid to liquid state. By heating the polyol above its melting point to create a liquid melt, then forming beads from this liquid state and allowing controlled crystallization, the process produces beads with smooth surfaces and uniform internal structure, avoiding the defects associated with solid particle granulation.
2Ease of operation
If larger beads are used, then coating and layering processes can be performed, but tablet size increases and more cushioning materials are required
Solution Approach 1:
The invention produces perfectly spherical beads with uniform roundness, which enables effective coating and layering processes. The spherical shape allows for smooth tumbling and uniform coating application, while the controlled size (can be made small) reduces the volume required in tablets, minimizing the need for cushioning materials.
3Ease of manufacture
If reactive beads such as sucrose/starch are used, then beads can be formed, but incompatibility with active substances occurs and API is lost
Solution Approach 1:
The invention uses polyol in its melted liquid state for bead formation, then allows controlled crystallization to form the final solid bead structure. This parameter change from solid particle granulation to melt formation creates a non-reactive, stable matrix that does not cause incompatibility with active substances, eliminating API loss while maintaining ease of manufacture.
4Ease of manufacture
If beads are made with microcrystalline cellulose, starch or cellulose derivatives, then beads can be formed, but moisture content causes incompatibility and API loss
Solution Approach 1:
The invention uses polyol in melted state for bead formation, creating a hydrophobic matrix that inherently resists moisture absorption. This parameter change from using moisture-prone materials like cellulose and starch to using melted polyol produces beads with low moisture content, eliminating incompatibility issues and API loss while maintaining ease of manufacture.
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 microspheres provide improved uniformity and reproducibility in coating thickness, reduced risk of pinhole formations, and enhanced API delivery, allowing for smaller tablet sizes, reduced cushioning requirements, and increased dose loading.
Implementation Method 1
The polyol is melted and spun into droplets or onto a spinning disc
Implementation Method 2
spun into droplets or onto a spinning disc
Implementation Method 3
sprayed through a nozzle
Implementation Method 4
The microspheres are cooled
Implementation Method 5
composed of a single crystal structure
Data Source
AI summary
The present invention relates to microspheres comprising a core material, wherein the microsphere is perfectly spherical and has a moisture content less than 1%, and the method of manufacturing the same. The present invention is useful in the manufacture of sustained and modified release active pharmaceutical ingredient (API) microspheres, as a free flowing excipient for mini-tablets and in the manufacture of API dispersions.