Improving the physical stability of freeze-dried amorphous sugar matrices by compression at several hundreds MPa

Journal of Pharmaceutical Sciences

Volumn 102, Issue 7, 2013, Pages 2187-2197

  Kagotani, Ryo ^a   Kinugawa, Kohshi ^a   Nomura, Mayo ^a   Imanaka, Hiroyuki ^a   Ishida, Naoyuki ^a   Imamura, Koreyoshi ^a  

^a OKAYAMA UNIVERSITY   (Japan)

Author keywords

Amorphous sugar; Calorimetry (DSC); Compression; Freeze drying; FTIR; Glass transition temperature; Water sorption

Indexed keywords

AMORPHOUS SUGAR; SUGAR; UNCLASSIFIED DRUG;

ARTICLE; FREEZE DRYING; HUMIDIFIER; PHYSICAL PARAMETERS;

EID: 84879030527     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.23568     Document Type: Article

References (37)

1. Manning MC, Patel K, Borchardt RT. 1989. Stability of protein pharmaceuticals. Pharm Res 6:903-918.
2. Pikal MJ. 1994. Freeze-drying of proteins. Process, formulation and stability. In Formulation and Delivery of Proteins and Peptides; Cleland JL, Langer R, Eds. Washington, DC: ACS Symposium Series, Vol. 567, pp 120-133.
3. Slade L, Levine H. 1993. The glassy state phenomenon in food molecules. In The Glassy State in Foods; Blanshard JMV, Lillford PJ, Eds. Nottingham, UK: Nottingham University Press, pp 35-102.
4. White GW, Cakebread SH. 1996. The glassy state in certain sugar-containing food products. J Food Technol 1:73-82.
5. Hancock BC, Shamblin SL. 1998. Water vapour sorption by pharmaceutical sugars. Pharm Sci Technol Today 1:345-351.
6. Roos Y, Karel M. 1991. Plasticizing effect of water on thermal behavior and crystallization of amorphous food model. J Food Sci 56:38-43.
7. Saleki-Gerhardt A, Zografi G. 1994. Non-isothermal and isothermal crystallization of sucrose from the amorphous state. Pharm Res 11:1166-1173.
8. Kedward CJ, MacNaughtan W, Blanshard JMV, Mitchell JR. 2000. Crystallization kinetics of lactose and sucrose based on isothermal differential scanning calorimetry. Carbohydr Res 329:423-430.
9. Harnkarnsujarit N, Charoenrein S. 2011. Effect of water activity on sugar crystallization and ß-carotene stability of freeze-dried mango powder. J Food Eng 105:592-598.
10. Flores-Fernandez GM, Sola RJ, Griebenow K. 2009. The relation between moisture-induced aggregation and structural changes in lyophilized insulin. J Pharm Pharmacol 61:1555-1561.
11. Lai MC, Topp EM. 1999. Solid-state chemical stability of proteins and peptides. J Pharm Sci 88:489-500.
12. Hageman MJ. 1992. Water sorption and solid-state stability of proteins. In Stability of Protein Pharmaceuticals, Part A: Chemical and Physical Pathways of Protein Degradation; Ahern TJ, Manning MC, Eds. New York: Plenum Press, pp 273-309.
13. Oliyai C, Patel JP, Carr L, Borchardt RT. 1994. Chemical pathways of peptide degradation. VII. Solid-state chemical instability of an aspartyl residue in a model hexapeptide. Pharm Res 11:901-908.
14. Jivraj M, Martini LG, Thomson CM. 2000. An overview of the different excipients useful for the direct compression of tablets. Pharm Sci Technol Today 3:58-63.
15. Martinez-Bustos F, Lopez-Soto M, San Martin-Martinez E, Zazueta-Morales JJ, Velez-Medina JJ. 2007. Effects of high energy milling on some functional properties of jicama starch (Pachyrrhizus erosus L. Urban) and cassava starch (Manihot esculenta Crantz). J Food Eng 78:1212-1220.
16. Thanatuksorn P, Kawai K, Kajiwara K, Suzuki T. 2009. Effects of ball-milling on the glass transition of wheat flour constituents. J Sci Food Agric 89:430-435.
17. Imamura K, Kagotani R, Nomura M, Tanaka K, Kinugawa K, Nakanishi K. 2011. Influence of compression on water sorption, glass transition, and enthalpy relaxation behavior of freeze-dried amorphous sugar matrices. Int J Pharm 405:76-83.
18. Shotton E, Obiorah BA. 1975. Effect of physical properties on compression characteristics. J Pharm Sci 64:1213-1216.
19. Sebhatu T, Ahlneck C, Alderborn G. 1997. The effect of moisture content on the compression and bond-formation properties of amorphous lactose particles. Int J Pharm 146:101-114.
20. Inghelbrecht S, Remon JP. 1998. The roller compaction of different types of lactose. Int J Pharm 166:135-144.
21. Sebhatu T, Alderborn G. 1999. Relationships between the effective interparticulate contact area and the tensile strength of tablets of amorphous and crystalline lactose of varying particle size. Eur J Pharm Sci 8:235-242.
22. Ndindayino F, Vervaet C, Van den Mooter G, Remon JP. 2002. Direct compression and moulding properties of co-extruded isomalt/drug mixtures. Int J Pharm 235:159-168.
23. Berggren J, Frenning G, Alderborn G. 2004. Compression behavior and tablet-forming ability of spray-dried amorphous composite particles. Eur J Pharm Sci 22:191-200.
24. Kawakami K, Miyoshi K, Tamura N, Yamaguchi T, Ida Y. 2006. Crystallization of sucrose glass under ambient conditions: Evaluation of crystallization rate and unusual melting behavior of resultant crystals. J Pharm Sci 95:1354-1363.
25. Imamura K, Nomura M, Tanaka K, Kataoka N, Oshitani J, Imanaka H, Nakanishi, K. 2010. Impacts of compression on crystallization behavior of freeze-dried amorphous sucrose. J Pharm Sci 99:1452-1463.
26. Imamura K, Kinugawa K, Kagotani R, Nomura M, Nakanishi K. 2012. Impact of compression, physical aging, and freezing rate on the crystallization characteristics of an amorphous sugar matrix. J Food Eng 112:313-318.
27. Imamura K, Kagotani R, Nomura M, Kinugawa K, Nakanishi, K. 2012. Heterogeneity of the state and functionality of water molecules sorbed in an amorphous sugar matrix. Carbohydr Res 351:108-113.
28. Imamura K, Yokoyama T, Fukushima A, Kinuhata M, Nakanishi K. 2010. Water sorption, glass transition, and protein-stabilizing behavior of an amorphous sucrose matrix combined with various materials. J Pharm Sci 99:4669-4677.
29. Greenspan L. 1977. Humidity fixed points of binary saturated aqueous solutions. J Res of NDS A Phys Chem 81A:89-96.
30. Byler DM, Susi H. 1986. Examination of the secondary structure on proteins by deconvolved FTIR spectra. Biopolymers 25:469-487.
31. Imamura K, Maruyama Y, Tanaka K, Yokoyama T, Imanaka H, Nakanishi K. 2008. True density analysis of a freeze-dried amorphous sugar matrix. J Pharm Sci 97:2789-2797.
32. Alavi SH, Rizvi SSH, Harriott P. 2003. Process dynamics of starch-based microcellular foams produced by supercritical fluid extrusion. II: Numerical simulation and experimental evaluation. Food Res Int 36:321-330.
33. Liu L, Rigsbee DR, Stotz C, Pikal MJ. 2002. Dynamics of pharmaceutical amorphous solids: The study of enthalpy relaxation by isothermal microcalorimetry. J Pharm Sci 91:1853-1862.
34. Kaminski K, Kaminska E, Hensel-Bielowka S, Pawlus S, Paluch M, Ziolo J. 2008. High pressure study on molecular mobility of leucrose. J Chem Phys 129:084501.
35. Grzybowska K, Paluch M, Grzybowski A, Pawlus S, Ancherbak S, Prevosto D, Capaccioli S. 2010. Dynamic crossover of water relaxation in aqueous mixtures: Effect of pressure. J Phys Chem Lett 1:1170-1175.
36. Abdul-Fattah AM, Truong-Le V, Yee L, Nguyen L, Kalonia DS, Cicerone MT, Pikal MJ. 2007. Drying-induced variations in physico-chemical properties of amorphous pharmaceuticals and their impact on stability (I): Stability of a monoclonal antibody. J Pharm Sci 96:1983-2008.
37. Kilbrun D, Claude J, Schweizer T, Alam A, Ubbink J. 2005. Carbohydrate polymers in amorphous states: An integrated thermodynamic and nanostructural investigation. Biomacromolecules 6:864-879.