Abstract:
:Previous studies have shown that protein storage stability in freeze-dried l-arginine-based systems improved in the presence of chloride ions. However, chloride ions reduced the glass transition temperature of the freeze concentrate (Tg') and made freeze drying more challenging. In this study, l-arginine was freeze dried with mannitol to obtain partially crystalline solids that can be freeze dried in a fast process and result in elegant cakes. We characterized the effect of different l-arginine counter ions on physicochemical properties of mannitol compared with mannitol/sucrose systems. Thermal properties of formulations with different compositions were correlated to thermal history during freeze drying and to physicochemical properties (cake appearance, residual moisture, reconstitution time, crystallinity). Partially crystalline solids were obtained even at the highest l-arginine level (mannitol:l-arginine of 2:1) used in this study. All l-arginine-containing formulations yielded elegant cakes. Only cakes containing l-arginine chloride and succinate showed a surface "crust" formed by phase separation. X-ray powder diffraction showed that inhibition of mannitol crystallization was stronger for l-arginine compared with sucrose and varied with the type of l-arginine counter ion. The counter ion affected mannitol polymorphism and higher levels of mannitol hemi-hydrate were obtained at high levels of l-arginine chloride.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Stärtzel P,Gieseler H,Gieseler M,Abdul-Fattah AM,Adler M,Mahler HC,Goldbach Pdoi
10.1016/j.xphs.2016.07.001subject
Has Abstractpub_date
2016-10-01 00:00:00pages
3123-3135issue
10eissn
0022-3549issn
1520-6017pii
S0022-3549(16)41524-8journal_volume
105pub_type
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