Existence of a mannitol hydrate during freeze-drying and practical implications

Journal of Pharmaceutical Sciences

Volumn 88, Issue 2, 1999, Pages 196-198

  Yu, Lian ^a   Milton, Nathaniel ^a   Groleau, Edward G ^a   Mishra, Dinesh S ^a   Vansickle, Ronald E ^a  

^a ELI LILLY AND COMPANY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

MANNITOL; SORBITOL;

ARTICLE; CRYSTALLIZATION; FREEZE DRYING; HEATING; THERMOSTABILITY; X RAY DIFFRACTION;

EID: 0032970823     PISSN: 00223549     EISSN: None     Source Type: Journal    
DOI: 10.1021/js980323h     Document Type: Article

References (27)

1. Marwick, T. C. An X-ray Study of Mannitol, Dulcitol and Mannose. Nature 1931, 127, 11-12.
2. McCrea, G. W. An X-ray Study of Mannitol. Nature 1931, 127, 162-163.
3. Rye, A.; Sorum, H. Crystalline Modifications of D-Mannitol. Acta Chem. Scand. 1952, 6, 1128-1129.
4. Berman, H. M.; Jeffrey, G. A.; Rosentein, R. D. The Crystal Structures of the α′ and β Forms of D-Mannitol. Acta Crystallogr. 1968, B24, 442-449,
5. Kim, H. S.; Jeffrey, G. A.; Rosenstein, R. D. The Crystal Structure of the K Form of D-Mannitol. Acta Crystallogr. 1968, B24, 1449-1455.
6. Walter-Levy, L. Sur les varietes crystallines du D-mannitol. C. R. Acad. Sc. Paris 1968, 267, 1779-1782.
7. Debord, B.; Lefebvre, C.; Guyot-Hermann, A. M.; Hubert, J.; Bouche, R.; Guyot, J. C. Study of Different Crystalline Forms of Mannitol: Comparative Behaviour under Compression. Drug Dev. Ind. Pharm. 1987, 13, 1533-1546.
8. Jones, F. T.; Lee, K. S. The Optical and Crystallographic Properties of Three Phases of Mannitol. Microscope 1970, 18, 279-285.
9. 13C-N.M.R. chemical shifts of Carbohydrates in the Solid State. The Spectra of D-Mannitol Polymorphs and of DL-Mannitol. Carbohydr. Res. 1990, 197, 41-52.
10. Pitkanen, I.; Perkkalainen, P.; Rautiainen, H. Thermoanalytical Studies of Phases of D-Mannitol. Thermochim. Acta 1993, 214, 157-162.
11. Burger, A.; Hetz, S.; Weissnicht, A. On the Polymorphism of Mannitol. Eur. J. Pharm. Biopharm. 1994, 40(Suppl.), 21S.
12. Yu, L.; Mishra, D. S.; Rigsbee, D. R. Determination of the Glass Properties of D-Mannitol Using Sorbitol as an Impurity. J. Pharm. Sci. 1998, 87, 774-777.
13. Willaims, N. A.; Lee, Y.; Polli, G. P.; Jennings, T. A. The Effect of Cooling Rate on Solid-Phase Transitions and Associated Vial Breakage Occurring in Frozen Mannitol Solutions. J. Parenteral Sci. Technol. 1986, 40, 135-141
14. Williams, N. A.; Dean, T. Vial Breakage by Frozen Mannitol Solutions: Correlation with Thermal Characteristics and Effect of Stereoisomerism, Additives and Vial Configuration. J. Parenteral Sci. Technol. 1991, 45, 94-100.
15. Kim, A. I.; Akers, M. J.; Nail, S. L. The Physical State of Mannitol after Freeze-Drying: Effects of Mannitol Concentration, Freezing Rate, and a Noncrystallizing Cosolute. J. Pharm. Sci. 1998, 87, 931-935.
16. Martini, A.; Kume, S.; Crivellente, M.; Artico, R. Use of Subambient Differential Scanning Calorimetry to Monitor the Frozen-State Behavior of Blends of Excipients for Freeze-Drying. PDA J. Pharm. Sci. Technol. 1997, 51, 62-67.
17. Cavatur, R. K.; Suryanarayanan, R. Characterization of Frozen Aqueous Solutions by Low-Temperature X-ray Powder Diffractometry. Pharm. Res. 1998, 15, 194-199.
18. Kovalcik, T.; Guillory, J. K. The Stability of Cyclophosphamide in Lyophilized Cakes. Part I. Mannitol, Lactose, and Sodium Bicarbonate as Excipients. J. Parenteral Sci. Technol. 1988, 42, 29-39.
19. Isutsu, K.; Yoshioka, S.; Terao, T. Effect of Mannitol Crystallinity on the Stabilization of Enzymes during Freeze-Drying. Chem. Pharm. Bull. 1994, 42, 5-8.
20. Pitkanen et al. wrote in 1993, "We took efforts to crystallize hydrous forms, but did not succeed" (ref 10).
21. Stephenson, G. A.; Groleau, E. G.; Kleemann, R. L.; Xu, W.; Rigsbee, D. R. Formation of Isomorphic Desolvates: Creating a Molecular Vacuum. J. Pharm. Sci. 1998, 87, 536-542.
22. The Powder Diffraction File. International Centre for Diffraction Data, 12 Campus Blvd., Newtown Square, PA 19073-3273.
23. Yu, L.; Milton, N. Unpublished result.
24. Cavatur, R. K.; Suryanarayanan, R. Characterization of Phase Transitions During Freeze-Drying by in Situ Powder X-ray Powder Diffractometry, presentation abstract submitted to the AAPS Annual Meeting and Exposition, Nov 15-19, 1998, San Francisco, CA.
25. Wade, A.; Weller, P. J., Eds. Handbook of Pharmaceutical Excipients, 2nd ed.; American Pharmaceutical Association: Washington, D.C., 1994.
26. Herman, B. D.; Sinclair, B. D.; Milton, N.; Nail, S. L. The Effect of bulking Agent on the Solid-State Stability of Freeze-Dried Methylprednisolone Sodium Succinate. Pharm. Res. 1994, 11, 1467-1473.
27. Roos, Y.; Karel, M. Crystallization of Amorphous Lactose. J. Food Sci. 1992, 57, 775-777.