scholarly journals The Influence of Drug Physical State on the Dissolution Enhancement of Solid Dispersions Prepared Via Hot-Melt Extrusion: A Case Study Using Olanzapine

2014 ◽  
Vol 103 (4) ◽  
pp. 1214-1223 ◽  
Author(s):  
Maria Fátima Pina ◽  
Min Zhao ◽  
João F. Pinto ◽  
João J. Sousa ◽  
Duncan Q.M. Craig
Keyword(s):  
Physical State ◽  
Solid Dispersions ◽  
Hot Melt Extrusion ◽  
Dissolution Enhancement ◽  
Melt Extrusion ◽  
Hot Melt

scholarly journals An investigation into the formations of the internal microstructures of solid dispersions prepared by hot melt extrusion

2020 ◽  
Vol 155 ◽  
pp. 147-161
Author(s):  
Fahad Alqahtani ◽  
Peter Belton ◽  
Bin Zhang ◽  
Mohammed Al-Sharabi ◽  
Steven Ross ◽  
...  
Keyword(s):  
Solid Dispersions ◽  
Hot Melt Extrusion ◽  
Melt Extrusion ◽  
Hot Melt

scholarly journals Influence of Carbamazepine Dihydrate on the Preparation of Amorphous Solid Dispersions by Hot Melt Extrusion

Pharmaceutics ◽  
2020 ◽  
Vol 12 (4) ◽  
pp. 379 ◽  
Author(s):  
Xiangyu Ma ◽  
Felix Müller ◽  
Siyuan Huang ◽  
Michael Lowinger ◽  
Xu Liu ◽  
...  
Keyword(s):  
Energy State ◽  
Solid Dispersions ◽  
Amorphous Solid ◽  
Hot Melt Extrusion ◽  
Water Soluble ◽  
Melt Extrusion ◽  
Amorphous Solid Dispersions ◽  
Water Soluble Drugs ◽  
The Impact ◽  
Hot Melt

Amorphous solid dispersions (ASDs) are commonly used in the pharmaceutical industry to improve the dissolution and bioavailability of poorly water-soluble drugs. Hot melt extrusion (HME) has been employed to prepare ASD based products. However, due to the narrow processing window of HME, ASDs are normally obtained with high processing temperatures and mechanical stress. Interestingly, one-third of pharmaceutical compounds reportedly exist in hydrate forms. In this study, we selected carbamazepine (CBZ) dihydrate to investigate its solid-state changes during the dehydration process and the impact of the dehydration on the preparation of CBZ ASDs using a Leistritz micro-18 extruder. Various characterization techniques were used to study the dehydration kinetics of CBZ dihydrate under different conditions. We designed the extrusion runs and demonstrated that: 1) the dehydration of CBZ dihydrate resulted in a disordered state of the drug molecule; 2) the resulted higher energy state CBZ facilitated the drug solubilization and mixing with the polymer matrix during the HME process, which significantly decreased the required extrusion temperature from 140 to 60 °C for CBZ ASDs manufacturing compared to directly processing anhydrous crystalline CBZ. This work illustrated that the proper utilization of drug hydrates can significantly improve the processability of HME for preparing ASDs.

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