Back to Search
Start Over
The Influence of Temperature and Viscosity of Polyethylene Glycol on the Rate of Microwave-Induced In Situ Amorphization of Celecoxib
- Source :
- Molecules, Hempel, N-J, Dao, T, Knopp, M M, Berthelsen, R & Lobmann, K 2021, ' The Influence of Temperature and Viscosity of Polyethylene Glycol on the Rate of Microwave-Induced In Situ Amorphization of Celecoxib ', Molecules, vol. 26, no. 1, 110 . https://doi.org/10.3390/molecules26010110, Molecules, Vol 26, Iss 110, p 110 (2021)
- Publication Year :
- 2020
-
Abstract
- Microwaved-induced in situ amorphization of a drug in a polymer has been suggested to follow a dissolution process, with the drug dissolving into the mobile polymer at temperatures above the glass transition temperature (Tg) of the polymer. Thus, based on the Noyes–Whitney and the Stoke–Einstein equations, the temperature and the viscosity are expected to directly impact the rate and degree of drug amorphization. By investigating two different viscosity grades of polyethylene glycol (PEG), i.e., PEG 3000 and PEG 4000, and controlling the temperature of the microwave oven, it was possible to study the influence of both, temperature and viscosity, on the in situ amorphization of the model drug celecoxib (CCX) during exposure to microwave radiation. In this study, compacts containing 30 wt% CCX, 69 wt% PEG 3000 or PEG 4000 and 1 wt% lubricant (magnesium stearate) were exposed to microwave radiation at (i) a target temperature, or (ii) a target viscosity. It was found that at the target temperature, compacts containing PEG 3000 displayed a faster rate of amorphization as compared to compacts containing PEG 4000, due to the lower viscosity of PEG 3000 compared to PEG 4000. Furthermore, at the target viscosity, which was achieved by setting different temperatures for compacts containing PEG 3000 and PEG 4000, respectively, the compacts containing PEG 3000 displayed a slower rate of amorphization, due to a lower target temperature, than compacts containing PEG 4000. In conclusion, with lower viscosity of the polymer, at temperatures above its Tg, and with higher temperatures, both increasing the diffusion coefficient of the drug into the polymer, the rate of amorphization was increased allowing a faster in situ amorphization during exposure to microwave radiation. Hereby, the theory that the microwave-induced in situ amorphization process can be described as a dissolution process of the drug into the polymer, at temperatures above the Tg, is further strengthened.
- Subjects :
- Diffusion
PVP
Pharmaceutical Science
dissolution
02 engineering and technology
030226 pharmacology & pharmacy
Analytical Chemistry
Polyethylene Glycols
Viscosity
chemistry.chemical_compound
0302 clinical medicine
amorphous solid dispersion
Drug Discovery
Transition Temperature
Magnesium stearate
DRUG
Microwaves
Dissolution
chemistry.chemical_classification
RELEVANT
Communication
Anti-Inflammatory Agents, Non-Steroidal
Polymer
021001 nanoscience & nanotechnology
MOLECULAR-WEIGHT
Chemistry (miscellaneous)
polyethylene glycol
Molecular Medicine
DIELECTRIC-PROPERTIES
0210 nano-technology
Glass transition
Crystallization
Materials science
RELAXATION
Polyethylene glycol
lcsh:QD241-441
Excipients
03 medical and health sciences
lcsh:Organic chemistry
PEG ratio
Physical and Theoretical Chemistry
in situ amorphization
Organic Chemistry
technology, industry, and agriculture
temperature
Drug Liberation
microwave radiation
chemistry
Chemical engineering
Solubility
Celecoxib
viscosity
monotecticum
Subjects
Details
- ISSN :
- 14203049
- Volume :
- 26
- Issue :
- 1
- Database :
- OpenAIRE
- Journal :
- Molecules (Basel, Switzerland)
- Accession number :
- edsair.doi.dedup.....a70c6e5c0f2245bedb99d7d88d4de8ce
- Full Text :
- https://doi.org/10.3390/molecules26010110