화학공학소재연구정보센터
Powder Technology, Vol.326, 370-378, 2018
Mechanistic investigation on the performance of Huperzine A loaded microparticles based on ultra-fine particle processing system
Ultra-fine particle processing system (UPPS) was more advantageous in producing microparticles (MPs) than the conventional technologies since it was applicable for a wide range of drugs and the MPs could be manufactured in a successive and controllable way under mild conditions. The MPs based on this technology showed small uniform particle size, proper surface roughness, and dense structure, which were anticipated to benefit tablet compaction. Therefore, ethyl cellulose (EC) was selected as the matrix material to confirm the superiorities of UPPS produced MPs for compaction due to its rigidity and inflexibility. To improve the encapsulation efficiency (EE%) of EC based MPs, hydrophilic/hydrophobic plasticizers and polymers were added, and the effect was mechanistically investigated regarding to the polymer properties and particle size of MPs. The results revealed that the EE% of MPs was significantly improved in the presence of hydrophilic polymers, which was mainly related to the reduced drug leakage as a result of modified polymer properties and decreased particle size of MPs. The forming mechanism of MPs determined by X-ray photoelectron spectroscopy (XPS) revealed that the MPs were enriched with low molecular weight polymers on the surface due to the unevenly migration driven by the centrifugal force. The topography of MPs determined by atomic force microscopy showed that the MPs had considerable rough surface to the commercial excipient, which benefited for further compaction. Consequently, the dissolution profile of MPs after compaction was approachable to that of original MPs and the tablets showed optimal content uniformity. (C) 2017 Elsevier B.V. All rights reserved.