Pharmaceutical micro-particles give amorphous sucrose higher physical stability
2011 (English)In: Internation Journal of Pharmaceutics, ISSN 0378-5173, E-ISSN 1873-3476, Vol. 409, no 1-2, 96-103 p.Article in journal (Refereed) Published
The aim of this study was to explore how pharmaceutical micro-sized filler particles affect the amorphous stability of sucrose in sucrose/filler particle composites produced by freeze-drying. Focus was put on the filler particles' properties crystallinity, hygroscopicity, hydrophobicity, and surface area, and their influence on physical stability of the amorphous phase. The micro-sized filler particles were examined with Blaine permeametry, gas adsorption, pycnometry, gravimetric vapour sorption, X-ray diffraction, and light microscopy before composites of sucrose and micro-sized filler particles were prepared by freeze-drying. The stability of the composites was examined with X-ray diffraction, differential scanning calorimetry (DSC), and microcalorimetry. All composites were amorphous and showed higher stability compared to pure amorphous sucrose, which was evident from a delay in heat and moisture-induced crystallization. However, calcium carbonate and oxazepam micro-sized filler particles lost their ability to stabilize the amorphous sucrose when exposed to humidity. The dry glass transition temperature (T-g) was higher for the composites, indicating the stabilization was mediated by a reduced molecular mobility of the amorphous phase.
Place, publisher, year, edition, pages
2011. Vol. 409, no 1-2, 96-103 p.
Amorphous, Sucrose, Physical stability, Freeze-drying, Crystallization, Micro-particles
IdentifiersURN: urn:nbn:se:uu:diva-153962DOI: 10.1016/j.ijpharm.2011.02.031ISI: 000290135800012PubMedID: 21356288OAI: oai:DiVA.org:uu-153962DiVA: diva2:418518