Spray-Dried Sorbitol Plasticizer for Hot Melt Extrusion
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Solution Overview
Problem
Hot melt extrusion processes face challenges in stabilizing active pharmaceutical ingredients, particularly with polyvinyl alcohol (PVA) carriers, due to high temperatures that can lead to decomposition and poor solubility of poorly water-soluble drugs, requiring a suitable plasticizer to lower melting points and viscosity.
Innovation Solution
The use of spray-dried sorbitol, such as Parteck® SI, as a plasticizer in polymer-containing compositions during hot melt extrusion, which reduces the glass transition and melting temperatures, stabilizes thermally unstable active ingredients, and enhances solubility and mechanical strength of the extrudate.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Temperature
If high temperature is used in hot melt extrusion to process polyvinyl alcohol carrier, then the polymer can be melted and processed, but the thermally unstable active ingredients decompose
Solution Approach 1:
The invention changes the plasticizer parameter from traditional liquid plasticizers to spray-dried sorbitol with specific particle size (5-50 μm), which fundamentally alters the thermal behavior of the system. This parameter change enables processing at lower temperatures (below 150°C) while maintaining polymer processability, thus protecting thermally unstable active ingredients from decomposition
Solution Approach 2:
The invention creates a composite system combining polyvinyl alcohol carrier, spray-dried sorbitol plasticizer, and active ingredients. The spray-dried sorbitol particles form a composite structure that provides both plasticizing function and thermal protection, allowing the mixture to be processed at reduced temperatures while maintaining structural integrity and ingredient stability
2Ease of manufacture
If traditional liquid plasticizers are used to lower melting point and viscosity, then processability improves, but the mechanical strength of extrudate decreases and long-term stability is compromised
Solution Approach 1:
The invention changes the physical state parameter of the plasticizer from liquid to fine solid particles (5-50 μm). This parameter transformation allows the plasticizer to be incorporated into the polymer matrix without compromising the mechanical strength of the final extrudate, while still providing the necessary plasticizing effect for processability
Solution Approach 2:
The spray-dried sorbitol particles act as temporary processing aids that facilitate extrusion but do not permanently weaken the structure. Their fine particle size allows them to be distributed uniformly and provide plasticizing function during processing, while the resulting extrudate maintains adequate mechanical strength for downstream operations
3Stability of the object's composition
If high temperature processing is applied to achieve complete melting, then homogeneity improves, but energy consumption increases and thermal degradation occurs
Solution Approach 1:
The invention changes the temperature parameter from high temperature processing to low temperature processing (below 150°C) by incorporating spray-dried sorbitol particles. This parameter change reduces energy consumption significantly while the fine particle distribution ensures homogeneous mixing through enhanced interfacial contact and reduced melting viscosity
Solution Approach 2:
The spray-dried sorbitol particles create a porous-like structure in the melt that enhances mixing efficiency. The fine particles (5-50 μm) distribute throughout the polymer matrix, creating numerous interfaces that facilitate heat transfer and mass mixing, achieving homogeneity without requiring high temperatures
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 results in a stable amorphous solid dispersion of active pharmaceutical ingredients within a thermoplastic polymer matrix, improving bioavailability and solubility while maintaining long-term stability and ease of milling, overcoming the limitations of traditional crystalline sorbitol.
Implementation Method 1
the applied polyol reduces the glass transition temperature Tg and the melting temperature Tm of said polymer containing compositions
Implementation Method 2
the applied polyol reduces the glass transition temperature Tg and the melting temperature Tm of said polymer containing compositions
Implementation Method 3
Advantageously the applied sorbitol additionally reduces the melting viscosity of the polymer containing thermoplastic composition
Implementation Method 4
Plasticizers are capable to reduce the glass transition temperature and melt point (crystalline or semi-crystalline polymer) of polymer using for (hot) melt extrusion, during reducing the interaction of polymer chain secondary bonding and provide for more mobility
Data Source
AI summary
The present invention relates to the use of spray-dried sorbitol, such as Parteck® SI, as plasticizer for polymer containing compositions processed by (hot) melt extrusion. Due to its improved properties, achieved by its special manufacturing process (spray drying), this direct compressible excipient shows more additional benefits than the same substance in crystalline state.