Preparation of budesonide-poly (ethylene oxide) solid dispersions using supercritical fluid technology.
The purpose of this study was to investigate the possibility of preparing solid dispersions of the poorly soluble budesonide by supercritical fluid (SCF) technique, using poly (ethylene oxide) (PEO) as a hydrophilic carrier. The budesonide-PEO solid dispersions were prepared, using supercritical carbon dioxide (SC CO(2)) as the processing medium, and characterized by scanning electron microscopy (SEM), powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), solubility test and dissolution test in order to understand the influence of the SCF process on the physical status of the drug. The endothermic peak of budesonide in the SCF-treated mixtures was significantly reduced, indicating that budesonide was in amorphous form inside the carrier system. This was further confirmed by SEM and PXRD studies. The enhanced dissolution rates of budesonide were observed from SCF-treated budesonide-PEO mixtures. The amorphous characteristic of the budesonide, the better mixing of drug and PEO powders in the presence of SC CO(2), together with the improved wettability of the drug in PEO, produced a remarkable enhancement of the in vitro drug dissolution rate. Thus, budesonide-PEO solid dispersions with enhanced dissolution rate can be prepared using organic solvent-free SCF process.
Liu
Hui
H
Department of Pharmacy, Wuhan General Hospital, Wuhan, PR China.
Zhou
Li-Li
LL
Wei
Lan-Lan
LL
Hong-Guo
Nie
Shu-Fang
SF
Yang
Xing-Gang
XG
Tang
Ren
R
Pan
Wei-San
WS
D019819:Budesonide / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D002245:Carbon Dioxide; D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers / Q000737:chemistry*; D005938:Glucocorticoids / Q000737:chemistry*; D008855:Microscopy, Electron, Scanning; D008970:Molecular Weight; D011092:Polyethylene Glycols / Q000737:chemistry*; D011208:Powders; D012995:Solubility; D013678:Technology, Pharmaceutical; D013816:Thermodynamics; D017155:Wettability; D014961:X-Ray Diffraction
D004337:Drug Carriers; D005938:Glucocorticoids; D011208:Powders; D002245:Carbon Dioxide; D011092:Polyethylene Glycols; D019819:Budesonide