Predicting physical stability of ternary amorphous solid dispersions using specific mechanical energy in a hot melt extrusion process

2018 ◽  
Vol 548 (1) ◽  
pp. 571-585 ◽  
Author(s):  
Masataka Hanada ◽  
Scott V. Jermain ◽  
Xingyu Lu ◽  
Yongchao Su ◽  
Robert O. Williams
Keyword(s):  
Mechanical Energy ◽  
Solid Dispersions ◽  
Physical Stability ◽  
Amorphous Solid ◽  
Hot Melt Extrusion ◽  
Extrusion Process ◽  
Melt Extrusion ◽  
Amorphous Solid Dispersions ◽  
Specific Mechanical Energy ◽  
Hot Melt

scholarly journals Processing of Polyvinyl Acetate Phthalate in Hot-Melt Extrusion—Preparation of Amorphous Solid Dispersions

Pharmaceutics ◽  
2020 ◽  
Vol 12 (4) ◽  
pp. 337 ◽  
Author(s):  
Marius Monschke ◽  
Kevin Kayser ◽  
Karl G. Wagner
Keyword(s):  
Polyvinyl Acetate ◽  
Solid Dispersions ◽  
Amorphous Solid ◽  
Hot Melt Extrusion ◽  
Extrusion Process ◽  
Dissolution Time ◽  
Melt Extrusion ◽  
Amorphous Solid Dispersions ◽  
Ph Dependent ◽  
Hot Melt

The preparation of amorphous solid dispersions (ASDs) is a suitable approach to overcome solubility-limited absorption of poorly soluble drugs. In particular, pH-dependent soluble polymers have proven to be an excellently suitable carrier material for ASDs. Polyvinyl acetate phthalate (PVAP) is a polymer with a pH-dependent solubility, which is as yet not thoroughly characterized regarding its suitability for a hot-melt extrusion process. The objective of this study was to assess the processability of PVAP within a hot-melt extrusion process with the aim of preparing an ASD. Therefore, the influence of different process parameters (temperature, feed-rate) on the degree of degradation, solid-state and dissolution time of the neat polymer was studied. Subsequently, drug-containing ASDs with indomethacin (IND) and dipyridamole (DPD) were prepared, respectively, and analyzed regarding drug content, solid-state, non-sink dissolution performance and storage stability. PVAP was extrudable in combination with 10% (w/w) PEG 3000 as plasticizer. The dissolution time of PVAP was only slightly influenced by different process parameters. For IND no degradation occurred in combination with PVAP and single phased ASDs could be generated. The dissolution performance of the IND-PVAP ASD at pH 5.5 was superior and at pH 6.8 equivalent compared to commonly used polymers hydroxypropylmethylcellulose acetate succinate (HPMCAS) and Eudragit L100-55.

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 A Miniaturized Extruder to Prototype Amorphous Solid Dispersions: Selection of Plasticizers for Hot Melt Extrusion

Pharmaceutics ◽  
2018 ◽  
Vol 10 (2) ◽  
pp. 58 ◽  
Author(s):  
Matthias E. Lauer ◽  
Reto Maurer ◽  
Anne T. De Paepe ◽  
Cordula Stillhart ◽  
Laurence Jacob ◽  
...  
Keyword(s):  
Solid Dispersions ◽  
Amorphous Solid ◽  
Hot Melt Extrusion ◽  
Melt Extrusion ◽  
Amorphous Solid Dispersions ◽  
Hot Melt ◽  
Selection Of

scholarly journals Drug–Smectite Clay Amorphous Solid Dispersions Processed by Hot Melt Extrusion

2020 ◽  
Vol 21 (7) ◽  
Author(s):  
Uttom Nandi ◽  
Md. S.H. Mithu ◽  
Andrew P. Hurt ◽  
Vivek Trivedi ◽  
Dennis Douroumis
Keyword(s):  
Solid Dispersions ◽  
Amorphous Solid ◽  
Hot Melt Extrusion ◽  
Melt Extrusion ◽  
Amorphous Solid Dispersions ◽  
Smectite Clay ◽  
Hot Melt
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