Original Study of the Bioavailability Enhancement of Itraconazole-Based Solid Dispersions Produced by Hot Melt Extrusion in the Framework of the Three Rs Rule

2016 ◽  
Author(s):  
Justine Thiry
Keyword(s):  
Solid Dispersions ◽  
Hot Melt Extrusion ◽  
Original Study ◽  
Melt Extrusion ◽  
Bioavailability Enhancement ◽  
Hot Melt ◽  
The Three Rs

Bioavailability enhancement of itraconazole-based solid dispersions produced by hot melt extrusion in the framework of the Three Rs rule

2017 ◽  
Vol 99 ◽  
pp. 1-8 ◽  
Author(s):  
Justine Thiry ◽  
Miranda G.M. Kok ◽  
Laurence Collard ◽  
Antoine Frère ◽  
Fabrice Krier ◽  
...  
Keyword(s):  
Solid Dispersions ◽  
Hot Melt Extrusion ◽  
Melt Extrusion ◽  
Bioavailability Enhancement ◽  
Hot Melt ◽  
The Three Rs

Preparation of osthole-polymer solid dispersions by hot-melt extrusion for dissolution and bioavailability enhancement

2014 ◽  
Vol 465 (1-2) ◽  
pp. 436-443 ◽  
Author(s):  
Fei Yun ◽  
An Kang ◽  
Jinjun Shan ◽  
Xiaoli Zhao ◽  
Xiaolin Bi ◽  
...  
Keyword(s):  
Solid Dispersions ◽  
Hot Melt Extrusion ◽  
Melt Extrusion ◽  
Bioavailability Enhancement ◽  
Hot Melt

Hot Melt Extrusion for Amorphous Solid Dispersions: Temperature and Moisture Activated Drug–Polymer Interactions for Enhanced Stability

2013 ◽  
Vol 10 (10) ◽  
pp. 3665-3675 ◽  
Author(s):  
Ashish L. Sarode ◽  
Harpreet Sandhu ◽  
Navnit Shah ◽  
Waseem Malick ◽  
Hossein Zia
Keyword(s):  
Solid Dispersions ◽  
Amorphous Solid ◽  
Hot Melt Extrusion ◽  
Melt Extrusion ◽  
Amorphous Solid Dispersions ◽  
Polymer Interactions ◽  
Hot Melt ◽  
Enhanced Stability

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.

scholarly journals Polyelectrolytes in Hot Melt Extrusion: A Combined Solvent-Based and Interacting Additive Technique for Solid Dispersions

Pharmaceutics ◽  
2019 ◽  
Vol 11 (4) ◽  
pp. 174 ◽  
Author(s):  
Felix Ditzinger ◽  
Catherine Dejoie ◽  
Dubravka Sisak Jung ◽  
Martin Kuentz
Keyword(s):  
Solid Dispersions ◽  
Hot Melt Extrusion ◽  
Water Soluble ◽  
Quality Data ◽  
Homogeneous Distribution ◽  
Melt Extrusion ◽  
Synchrotron Source ◽  
Process Step ◽  
X Ray ◽  
Hot Melt

Solid dispersions are important supersaturating formulations to orally deliver poorly water-soluble drugs. A most important process technique is hot melt extrusion but process requirements limit the choice of suitable polymers. One way around this limitation is to synthesize new polymers. However, their disadvantage is that they require toxicological qualification and present regulatory hurdles for their market authorization. Therefore, this study follows an alternative approach, where new polymeric matrices are created by combining a known polymer, small molecular additives, and an initial solvent-based process step. The polyelectrolyte, carboxymethylcellulose sodium (NaCMC), was tested in combination with different additives such as amino acids, meglumine, trometamol, and urea. It was possible to obtain a new polyelectrolyte matrix that was viable for manufacturing by hot melt extrusion. The amount of additives had to be carefully tuned to obtain an amorphous polymer matrix. This was achieved by probing the matrix using several analytical techniques, such as Fourier transform infrared spectroscopy, differential scanning calorimetry, hot stage microscopy, and X-ray powder diffraction. Next, the obtained matrices had to be examined to ensure the homogeneous distribution of the components and the possible residual crystallinity. As this analysis requires probing a sample on several points and relies on high quality data, X-ray diffraction and starring techniques at a synchrotron source had to be used. Particularly promising with NaCMC was the addition of lysine as well as meglumine. Further research is needed to harness the novel matrix with drugs in amorphous formulations.

scholarly journals Hot-melt extrusion process impact on polymer choice of glyburide solid dispersions: The effect of wettability and dissolution

2019 ◽  
Vol 559 ◽  
pp. 245-254 ◽  
Author(s):  
Maen Alshafiee ◽  
Mohammad K. Aljammal ◽  
Daniel Markl ◽  
Adam Ward ◽  
Karl Walton ◽  
...  
Keyword(s):  
Solid Dispersions ◽  
Hot Melt Extrusion ◽  
Extrusion Process ◽  
Melt Extrusion ◽  
Hot Melt
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