Compression of amorphous solid dispersions prepared by hot-melt extrusion, spray drying and vacuum drum drying

Autor: Barbara V. Schönfeld, Karl G. Wagner, Ulrich Westedt
Jazyk: angličtina
Rok vydání: 2021
Předmět:
Hot-melt extrusion
Pharmaceutical Science
TS
tensile strength
PSD
particle size distribution
Vacuum drum drying
chemistry.chemical_compound
na
not applicable
w
tablet wall height
Drum drying
Lubricant
Composite material
f2
similarity factor
n.d.
not determined
SE
secondary electron
Tg
glass transition temperature
Spray drying
SSA
specific surface area
FFC
flow function coefficient
HME
hot-melt extrusion
LOD
loss on drying
SF
solid fraction
Downstream processing
SD
spray drying
Extrusion
D
tablet diameter
API
active pharmaceutical ingredient
P
breaking force
medicine.drug
Research Paper
X-ray μCT
X-ray microcomputed tomography
Materials science
f1
difference factor
SEM
scanning electron microscope
CP
compaction pressure
RTV
ritonavir
Die swell
VDD
vacuum drum drying
Pharmacy and materia medica
medicine
Amorphous solid dispersion
t
tablet thickness
Ritonavir
Compression analysis
Sorbitan monolaurate
ASD
amorphous solid dispersion
PSmin
minimal punch separation
V
volume
Amorphous solid
RS1-441
chemistry
Glidant
TER
Total elastic recovery
Zdroj: International Journal of Pharmaceutics: X, Vol 3, Iss, Pp 100102-(2021)
International Journal of Pharmaceutics: X
ISSN: 2590-1567
Popis: The present study explored vacuum drum drying (VDD) as an alternative technology for amorphous solid dispersions (ASDs) manufacture compared to hot-melt extrusion (HME) and spray drying (SD) focusing on downstream processability (powder properties, compression behavior and tablet performance). Ritonavir (15% w/w) in a copovidone/sorbitan monolaurate matrix was used as ASD model system. The pure ASDs and respective tablet blends (TB) (addition of filler, glidant, lubricant) were investigated. Milled extrudate showed superior powder properties (e.g., flowability, bulk density) compared to VDD and SD, which could be compensated by the addition of 12.9% outer phase. Advantageously, the VDD intermediate was directly compressible, whereas the SD material was not, resulting in tablets with defects based on a high degree of elastic recovery. Compared to HME, the VDD material showed superior tabletability when formulated as TB, resulting in stronger compacts at even lower solid fraction values. Despite the differences in tablet processing, tablets showed similar tablet performance in terms of disintegration and dissolution independent of the ASD origin. In conclusion, VDD is a valid alternative to manufacture ASDs. VDD offered advantageous downstream processability compared to SD: less solvents and process steps required (no second drying), improved powder properties and suitable for direct compression.
Graphical abstract Unlabelled Image
Highlights • ASD technology has influence on particle morphology • Compression behavior dominated by particle morphology • Vacuum drum dried intermediate direct compressible into tablets • Vacuum drum dried material shows better tabletability as milled extrudate • ASD technology: no impact on tablet disintegration/dissolution
Databáze: OpenAIRE
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