Use of a Plasticizer for Physical Stability Prediction of Amorphous Solid Dispersions
- Univ. of Minnesota, Minneapolis, MN (United States)
Utilizing glycerol as a plasticizer, an accelerated physical stability testing method of amorphous solid dispersions (ASDs) was developed. The influence of glycerol concentration on the glass transition temperature and α-relaxation time (a measure of molecular mobility) of amorphous ketoconazole, celecoxib, and the solid dispersions of each prepared with polyvinylpyrrolidone was investigated. By temperature scaling (Tg/T), the effects of glycerol concentration and temperature on the relaxation time were simultaneously evaluated. Glycerol, in a concentration dependent manner, accelerated crystallization in all of the systems without affecting the fragility. In celecoxib-PVP ASDs, the drug crystallization was well coupled to molecular mobility and was essentially unaltered at glycerol concentrations up to 2% w/w. The acceleration in crystallization brought about by glycerol expedited the determination of the coupling between molecular mobility and crystallization. As a result, we were able to predict the physical stability of the unplasticized ASD. Lastly, this approach is especially useful for ASDs with high polymer content where drug crystallization is extremely slow at the relevant storage temperature.
- Research Organization:
- Argonne National Laboratory (ANL), Argonne, IL (United States)
- Sponsoring Organization:
- USDOE Office of Science (SC), Basic Energy Sciences (BES)
- Grant/Contract Number:
- AC02-06CH11357
- OSTI ID:
- 1406627
- Journal Information:
- Crystal Growth and Design, Vol. 17, Issue 8; ISSN 1528-7483
- Publisher:
- American Chemical SocietyCopyright Statement
- Country of Publication:
- United States
- Language:
- ENGLISH
Web of Science
A Miniaturized Extruder to Prototype Amorphous Solid Dispersions: Selection of Plasticizers for Hot Melt Extrusion
|
journal | May 2018 |
Similar Records
Rapid Assessment of the Physical Stability of Amorphous Solid Dispersions
Effect of Polymer Molecular Weight on the Crystallization Behavior of Indomethacin Amorphous Solid Dispersions