Preparation and pharmaceutical characterization of amorphous cefdinir using spray-drying and SAS-process.
The aim of this study was to investigate the effects of micronization and amorphorization of cefdinir on solubility and dissolution rate. The amorphous samples were prepared by spray-drying (SD) and supercritical anti-solvent (SAS) process, respectively and their amorphous natures were confirmed by DSC, PXRD and FT-IR. Thermal gravimetric analysis was performed by TGA. SEM was used to investigate the morphology of particles and the processed particle had a spherical shape, while the unprocessed crystalline particle had a needle-like shape. The mean particle size and specific surface area were measured by dynamic light scattering (DLS) and BET, respectively. The DLS result showed that the SAS-processed particle was the smallest, followed by SD and the unprocessed cefdinir. The BET result was the same as DLS result in that the SAS-processed particle had the largest surface area. Therefore, the processed cefdinir, especially the SAS-processed particle, appeared to have enhanced apparent solubility, improved intrinsic dissolution rate and better drug release when compared with SD-processed and unprocessed crystalline cefdinir due not only to its amorphous nature, but also its reduced particle size. Conclusions were that the solubility and dissolution rate of crystalline cefdinir could be improved by physically modifying the particles using SD and SAS-process. Furthermore, SAS-process was a powerful methodology for improving the solubility and dissolution rate of cefdinir.
Park
Junsung
J
Center for Nanotechnology-based New Drug Dosage Form, College of Pharmacy, Chungnam National University, 220 Gung-dong, Yuseung-gu, Daejeon 305-764, Republic of Korea.
Park
Hee Jun
HJ
Cho
Wonkyung
W
Cha
Kwang-Ho
KH
Kang
Young-Shin
YS
Hwang
Sung-Joo
SJ
D000900:Anti-Bacterial Agents / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D000077525:Cefdinir; D002511:Cephalosporins / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical; D025924:Chromatography, Supercritical Fluid; D018360:Crystallography, X-Ray; D007700:Kinetics; D008855:Microscopy, Electron, Scanning; D036103:Nanotechnology; D010316:Particle Size; D033362:Powder Diffraction; D012995:Solubility; D012997:Solvents / Q000737:chemistry*; D017550:Spectroscopy, Fourier Transform Infrared; D013499:Surface Properties; D013678:Technology, Pharmaceutical / Q000379:methods*; D013818:Thermogravimetry
D000900:Anti-Bacterial Agents; D002511:Cephalosporins; D012997:Solvents; D000077525:Cefdinir