Back to Search
Start Over
Interdependence of particle properties and bulk powder behavior of indomethacin in quench-cooled molten two-phase solid dispersions
- Source :
- International journal of pharmaceutics. 541(1-2)
- Publication Year :
- 2017
-
Abstract
- Solid dispersions (SDs) hold a proven potential in formulating poorly water-soluble drugs. The present paper investigates the interfacial phenomena associated with the bulk powder flow, water sorption, wetting and dissolution of the SDs prepared by a modified melt and quench-cooling (QC) method. Poorly water-soluble indomethacin (IND) was QC molten with solubilizing graft copolymer (Soluplus (R)) or polyol sugar alcohol (xylitol, XYL). The interfacial interactions of SDs with air/water were found to be reliant on the type (amorphous/crystalline) and amount of the carrier material used. The final SDs were composed of fused agglomerates (SOL) or large jagged particles (XYL) with good wetting and powder flow properties. The initial dissolution of IND was accelerated by both carrier materials studied. The QC molten SDs with amorphous Soluplus (R) significantly improved the dissolution rate of IND at pH 6.8 (79.9 +/- 0.2% at 30 min) compared to that of pure crystalline drug. The substantial improvement in the dissolution rate of IND was in connection with the amorphous state of the drug being stabilized by Soluplus (R) in the QC molten SDs. However, it is evident that a strong H-bond formation between the components in some regions of the QC molten SDs can limit the dissolution of IND. The QC molten two-phase SDs with a polyol carrier (XYL) showed rapid and continuous drug release without reaching a plateau.
- Subjects :
- Materials science
BIOAVAILABILITY
polymer
Chemistry, Pharmaceutical
Drug Compounding
Indomethacin
dissolution
Pharmaceutical Science
02 engineering and technology
030226 pharmacology & pharmacy
Phase Transition
Polyethylene Glycols
Excipients
03 medical and health sciences
0302 clinical medicine
Polyol
Drug Stability
Phase (matter)
particle properties
WATER-SOLUBLE DRUG
Copolymer
HOT-MELT EXTRUSION
FLOWABILITY
FORMULATION
Dissolution
Xylitol
DISSOLUTION RATE
solid dispersion
chemistry.chemical_classification
Drug Carriers
bulk powder behavior
AMORPHOUS INDOMETHACIN
MIXTURES
Polymer
021001 nanoscience & nanotechnology
Amorphous solid
PHYSICAL STABILITY
Drug Liberation
SIZE
Chemical engineering
chemistry
Solubility
317 Pharmacy
Agglomerate
Polyvinyls
Wetting
Powders
0210 nano-technology
Subjects
Details
- ISSN :
- 18733476
- Volume :
- 541
- Issue :
- 1-2
- Database :
- OpenAIRE
- Journal :
- International journal of pharmaceutics
- Accession number :
- edsair.doi.dedup.....08a660ff41391227d7c37c559a098429