Evaluation of solid carvedilol-loaded SMEDDS produced by the spray drying method and a study of related substances.
In this study, various formulations of solidified carvedilol-loaded SMEDDS with high SMEDDS loading (up to 67% w/w) were produced with the spray drying process using various porous silica-based carriers. The process yield was improved with higher atomization gas flow rate during the spray drying process and with prolonged mixing time of dispersion of liquid SMEDDS and solid porous carriers prior to the spray drying process. Depending on the choice of the carrier and the SMEDDS:carrier ratio in solid SMEDDS, different drug loading, self-microemulsifying properties, drug release rates, and released drug fractions were obtained. The products exhibited fast drug release due to preserved self-microemulsifying properties and the absence of crystalline carvedilol, which was confirmed with XRD and Raman mapping. A decrease in drug content during the stability study was observed and investigated. This was at least partially attributed to the chemical degradation of the drug. Key degradation products determined by the LC-MS method were amides formed by in situ reaction of carvedilol with fatty acids present in the oily phase of SMEDDS.
['Mandić|J|J|', 'Kosmač|I|I|', 'Kovačević|M|M|', 'Hodnik|B|B|', 'Hodnik|Ž|Ž|', 'Vrečer|F|F|', 'Gašperlin|M|M|', 'Perissutti|B|B|', 'Zvonar Pobirk|A|A|']
D001682:Biological Availability D000077261:Carvedilol D004339:Drug Compounding D016503:Drug Delivery Systems D065546:Drug Liberation D004655:Emulsions D012995:Solubility D000085642:Spray Drying
SMEDDS Spray drying Related substances Porous carriers Carvedilol Stability