A calorimetric investigation of thermodynamic and molecular mobility contributions to the physical stability of two pharmaceutical glasses

Journal of Pharmaceutical Sciences

Volumn 96, Issue 1, 2007, Pages 71-83

  Zhou, Deliang ^a   Grant, David J W ^a   Zhang, Geoff G Z ^b   Law, Devalina ^b   Schmitt, Eric A ^b  

^a UNIVERSITY OF MINNESOTA   (United States)

^b ABBOTT LABORATORIES   (United States)

Author keywords

Adam Gibbs; Annealing; Crystallization; Modulated DSC; Molecular mobility

Indexed keywords

NIFEDIPINE; RITONAVIR;

ARTICLE; CRYSTALLIZATION; DIFFERENTIAL SCANNING CALORIMETRY; DRUG STABILITY; ENTROPY; GLASS TRANSITION TEMPERATURE; HEAT ACCLIMATIZATION; MOLECULAR DYNAMICS; THERMODYNAMICS; THERMOSTABILITY;

EID: 33846143481     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.20633     Document Type: Article

References (41)

1. Pikal MJ, Lukes AL, Lang JE, Gaines K. 1978. Quantitative crystallinity determinations for β-lactam antibiotics by solution calorimetry: Correlations with stability. J Pharm Sci 67:767-772.
2. Aso Y, Yoshioka S, Otsuka T, Kojima S. 1995. The physical stability of amorphous nifedipine determined by isothermal microcalorimetry. Chem Pharm Bull 43:300-303.
3. Hancock BC, Shamblin SL, Zografi G. 1995. Molecular mobility of amorphous pharmaceutical solids below their glass transition temperature. Pharm Res 12:799-806.
4. Hancock BC, Zografi G. 1997. Characteristics and significance of the amorphous state in pharmaceutical systems. J Pharm Sci 86:1-12.
5. Duddu SP, Zhang G, Dal Monte PR. 1997. The relationship between protein aggregation and molecular mobility below the glass transition temperature of lyophilized formulations containing a monclonal antibody. Pharm Res 14:596-600.
6. Shamblin SL, Tang X, Chang L, Hancock BC, Pikal MJ. 1999. Characterization of the time scales of molecular motion in pharmaceutically important glasses. J Phys Chem B 103:4113-4121.
7. 1H NMR relaxation times. J Pharm Sci 89:408-416.
8. Zografi G. 2000. The Amorphous State. The 42nd Annual International Industrial Pharmaceutical Research and Development Conference, Madison, WI.
9. 13C nuclear magnetic resonance relaxation time and the relaxation time obtained from the heating rate dependence of the glass transition temperature. J Pharm Sci 90:798-806.
10. Zhou D, Zhang GGZ, Law D, Grant DJW, Schmitt EA. 2002. Physical stability of amorphous pharmaceuticals: Importance of configurational thermodynamic quantities and molecular mobility. J Pharm Sci 91:1863-1872.
11. Adam G, Gibbs JH. 1965. On the temperature dependence of cooperative relaxation properties in glass-forming liquids. J Chem Phys 43:139-146.
12. Gibbs JH, DiMarzio EA. 1958. Nature of the glass transition and the glassy state. J Chem Phys 28:373-383.
13. Hodge IM. 1995. Physical aging in polymer glasses. Science 267:1945-1947.
14. Hodge IM. 1996. Strong and fragile liquids-a brief critique. J Non-Cryst Solids 202:164-172.
15. Angell CA. 1997. Why C1 = 16-17 in the WLF equation is physical-and the fragility of polymers. Polymer 38:6261-6266.
16. Hodge IM. 1994. Enthalpy relaxation and recovery in amorphous materials. J Non-Cryst Solids 169:211-266.
17. Tool AQ, Eichlin CG. 1931. Variations caused in the heating curves of glass by heat treatment. J Am Ceram Soc 14:276-308.
18. Tool AQ. 1946. Relation between inelastic deformability and thermal expansion of glass in its annealing range. J Am Ceram Soc 29:240-253.
19. Ritland HN. 1956. Limitations of the fictive temperature concept. J Am Ceram Soc 39:403-406.
20. Narayanaswamy OS. 1971. Model of structural relaxation in glass. J Am Ceram Soc 54:491-498.
21. Scherer GW. 1984. Use of the Adam-Gibbs equation in the analysis of structural relaxation. J Am Ceram Soc 67:504-511.
22. Hodge IM. 1987. Effects of annealing and prior history on enthalpy relaxation in glassy polymers. 6. Adam-Gibbs formulation of nonlinearity. Macromolecules 20:2897-2908.
23. Williams G, Watts DC. 1970. Non-symmetrical dielectric relaxation behavior arising from a simple empirical decay function. Trans Faraday Soc 66:80-85.
24. Williams G, Watts DC, Dev SB, North AM. 1971. Further considerations of nonsymmetrical dielectric relaxation behavior arising from a simple empirical decay function. Trans Faraday Soc 67:1323-1335.
25. Modulated DSC™ Compendium: Basic Theory and Experimental Considerations. New Castle, Deleware: Published by TA Instruments, Inc.
26. Moynihan CT, Easteal AJ, Wilder J. 1974. Dependence of the glass transition temperature on heating and cooling rate. J Phys Chem 78:2673-2677.
27. Moynihan CT, Lee SK, Tatsumisago M, Minami T. 1996. Estimation of activation energies for structural relaxation and viscous flow from DTA and DSC experiments. Thermochim Acta 280(281):153-162.
28. Kauzmann W. 1948. The nature of the glassy state and the behavior of liquids at low temperatures. Chem Rev 43:219-256.
29. Debenedetti PG, Stillinger FH. 2001. Supercooled liquids and the glass transition. Nature 410:259-267.
30. Casalini R, Capaccioli S, Lucchesi M, Rolla PA, Corezzi S. 2001. Pressure dependence of structural relaxation time in terms of the Adam-Gibbs model. Phys Rev E 63:031207/1-031207/6.
31. Richert R, Angell CA. 1998. Dynamics of glass-forming liquids. V. On the link between molecular dynamics and configurational entropy. J Chem Phys 108:9017-9026.
32. Johari GP. 2000. A resolution for the enigma of a liquid's configurational entropy-molecular kinetics relation. J Chem Phys 112:8958-8969.
33. Johari GP. 2002. The entropy loss on supercooling a liquid and anharmonic contributions. J Chem Phys 116:2043-2046.
34. Martinez L-M, Angell CA. 2000. Vibrational entropy, configurational entropy, and the fragility of glassforming liquids. Los Alamos Natl Lab Preprint Arch Condensed Matter 1-11.
35. Hately RHM. 1997. Glass fragility and stability of pharmaceutical preparations-excipient selection. Pharm Dev Tech 2:257-264.
36. Williams ML. 1955. The temperature dependence of mechanical and electrical relaxations in polymers. J Phys Chem 59:95-96.
37. Williams ML, Landel RF, Ferry JD. 1955. The temperature dependence of relaxation mechanisms in amorphous polymers and other glass-forming liquids. J Am Chem Soc 77:3701-3707.
38. Angell CA. 1985. In: Ngai K, Wright GB, editors. Relaxations in Complex Systems. Springfield, VA: National Technical Information Service, US Department of Commerce. p 345.
39. Vogel H. 1921. Das Temperaturabhängigkeitsgesetz der Viskosität von Flüssigkeiten. Phys Z 22:645-646.
40. Tammann VG, Hesse W. 1926. Die Abhängigkeit der Viscosität von der Temperatur bei unterkühlten Flüssigkeiten. Z Anorg Allg Chem 156:245-257.
41. Fulcher GS. 1925. Analysis of recent measurements of the viscosity of glasses. J Am Ceram Soc 8:339-355.