Characterization of carbamazepine-Gelucire 50/13 microparticles prepared by a spray-congealing process using ultrasounds.
In this work, the utilization of a spray-congealing technique using a new ultrasonic atomizer to prepare enhanced-release, solvent-free microspheres of carbamazepine (CBZ)-Gelucire 50/13 in different drug-to-polymer ratios was considered. Scanning electron microscopy analysis showed that it was possible to obtain spherically shaped and nonaggregated microparticles; the prevalent particle size was in the range 150-250 microm and the microspheres had a good encapsulation efficiency (> 90% in the prevalent size fraction). The in vitro dissolution tests displayed a significant increase of the CBZ dissolution rate from microspheres compared with pure drug and to drug-Gelucire 50/13 physical mixture. Differential scanning calorimetry, hot stage microscopy, X-ray powder diffractometry, and diffuse reflectance Fourier transform infrared spectroscopy demonstrated phase stability of the original polymorph of CBZ in all the systems; moreover, no interactions between the drug and Gelucire 50/13 were found. The results of this study suggested that the spray-congealing technique using the ultrasonic atomizer could be considered as a new and interesting method to enhance the dissolution rate of a poorly water-soluble drug as CBZ.
Passerini
Nadia
N
Department of Pharmaceutical Sciences, University of Bologna, Via S. Donato 19/2, 40127 Bologna, Italy. passerin@biocfarm.unibo.it
Perissutti
Beatrice
B
Moneghini
Mariarosa
M
Voinovich
Dario
D
Albertini
Beatrice
B
Cavallari
Cristina
C
Rodriguez
Lorenzo
L
D002152:Calorimetry, Differential Scanning; D002220:Carbamazepine / Q000008:administration & dosage / Q000737:chemistry*; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D005079:Excipients; D005223:Fats / Q000008:administration & dosage / Q000737:chemistry*; D007202:Indicators and Reagents; D008855:Microscopy, Electron, Scanning; D008863:Microspheres; D009821:Oils / Q000008:administration & dosage / Q000737:chemistry*; D010316:Particle Size; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D014465:Ultrasonics; D014961:X-Ray Diffraction
D005079:Excipients; D005223:Fats; D007202:Indicators and Reagents; D009821:Oils; C071184:Gelucire 50-13; D002220:Carbamazepine