Abstract
Thermal analysis methods are well-established techniques in research laboratories of pharmaceutical industry. The robustness and sensitivity of instrumentation, the introduction of automation and of reliable software according to the industrial needs widened considerably the areas of applications inthe last decade. Calibration of instruments and validation of results follow the state of the art of cGMP as for other analytical techniques. Thermal analysis techniques are especially useful for the study of the behavior of the poly-phasic systems drug substances and excipients and find a unique place for new delivery systems. Since change of temperature and moisture occur by processing and storage, changes of the solid state may have a considerable effect on activity, toxicity and stability of compounds. Current requirements of the International Conference of Harmonisation for the characterization and the quantitation of polymorphism in new entities re-enforce the position of thermal analysis techniques. This challenging task needs the use of complementary methods. Combined techniques and microcalorimetry demonstrate their advantages. This article reviews the current use of thermal analysis and combined techniques in research and development and in production. The advantage of commercially coupled techniques to thermogravimetry is emphasized with some examples.
Similar content being viewed by others
References
W. W. Wendlandt, Thermal Analysis, 3rd Ed. In Chemical Analysis, Vol. 19., P. J. Elving, J. D. Winefordner and I. M Kolthoff, Eds; John Wiley, New York 1986.
B. Wunderlich, Thermal Analysis, Academic Press, New York 1990.
P. J. Haines, Thermal Methods of Analysis, Principles, Applications and Problems, Blackie, Academic Professional 1995.
E. A. Turi, Thermal Characterization on Polymeric Materials, 2nd Ed., Academic Press, New York 1997.
J. L. Ford and P. Timmins, Pharmaceutical Thermal Analysis Techniques and Applications, Ellis Horwood Books in Biological Sciences, Series in Pharmaceutical Technology, M. Rubinstein, Ed., John Wiley&Sons 1989.
P. A. Barnes, Thermochim. Acta, 114 (1987) 1.
D. Giron, J. Pharm. Biochem. Anal., 40 (1986) 755.
D. Giron, Acta Pharm. Jugosl., 40 (1990) 95.
G. Bettinetti, Farmaco, 47 (1992) 681.
A. F. Barnes, M. J. Hardy and T. J. Lever, J. Thermal Anal., 40 (1993) 499.
D. Giron, Thermal Analysis of Drugs and Drug Products, in Encyclopedia of Pharmaceutical Technology, 1995, vol. 15, p. 1, J. Swarbrick and J. C. Boylan, Eds, Marcel Dekker.
P. H. Willcoks, Thermochim. Acta, 256 (1995) 1.
T. Wadsten, J. Thermal Anal., 47 (1996) 525.
D. Giron, J. Therm. Anal. Cal., 56 (1999) 1285.
D. Giron, P.S.S.T., 1 (1998) 191 and 262.
D. Giron, Am. Pharm. Rev., 3 (2000) 3 and 43.
T. Ozawa, Thermochim. Acta, 355 (2000) 35.
S. Z. D. Cheng, C. Y. Li, B. H. Calhoun, L. Zhu and W. W. Zhou, Thermochim. Acta, 355 (2000) 59.
K. C. Thompson, Thermochim. Acta, 366 (2000) 83.
J. Han, S. Gupte and R. Suryanarayanan, Int. J. Pharm., 170 (2000) 63.
S. L. Simon, Thermochim. Acta, 374 (2001) 55.
G. Buckton, Thermochim. Acta, 248 (1995) 117.
I. Wadsö, Thermochim. Acta, 294 (1999) 1.
H. Nyqvist, Int. J. Pharm. Techn. Prod. Mfr., 4 (1983) 47.
X. M. Zeug, G. P. Martin and C. Marriott, Int. J. Pharm., 218 (2001) 63.
Dynamic Vapour Sorption instrument (DVS), Surface Measurement Systems Ltd, UK.
N. Markova and L. Wadsö, Thermochim. Acta, 574 (2001) 93.
H. Utschick and M. Dohn, J. Therm. Anal. Cal., 52 (1998) 235.
R. Sabbah, A. Xu-Wu, J. S. Chickos, M. L. Leita and M. V. Roux, Thermochim. Acta, 331 (1999) 93.
International Conference on Harmonization (ICH). ICHQ2: Note for guidance on validation of analytical procedures. Methodology (1996).
D. Giron and C. Goldbronn, J. Thermal Anal., 44 (1995) 217.
K. Sato, J. Pharm. Pharmacol, B77-B83 (1993).
S. R. Chemburkar, J. Bauer, K. Deming, H. Spiwek, K. Patel, J. Morris, R. Henry, S. Spanton, W. Dziki, W. Porter, J. Quick, P. Bauer, J. Donaubauer, B. A. Narayanan, M. Soldani, D. Riley and K. McFarland, Organic Process Res., 4 (2000) 413.
D. Giron, C. Goldbronn and P. Piechon, J. Pharm. Biochem. Anal., 7 (1989) 1421.
D. Giron, Thermochim. Acta, 248 (1995) 1.
D. Giron, S.T.P. Pharma (Hors serie), 6 (1990) 87.
Y. Wada and H. Matsubyara, Thermochim. Acta, 196 (1992) 63.
M. Anberg, C. Nyström and S. Castensson, Int. J. Pharm., 81 (1992) 153.
M. Koenigbauer, J. Pharm. Res., 11 (1994) 777.
H. J. W. Ward and G. A. Holdgate, Prog. Med. Chem., 38 (2001) 309.
International Conference on Harmonization (ICH) Guideline Specification Q6A, Decision Tree 4: Investigating the need to set acceptance criteria for polymorphism in drug substances and drug products, 1999.
S. R. Byrn, Solid State Chemistry of Drugs, Academic Press, New York 1982.
H. K. Cammenga, Mater. Sci. Monogr., 28A (1985) 131.
J. Bernstein, R. J. Davey and J. O. Henck, Concomittant Polymorphs, Angew. Chem. Int. Ed., 38 (1999) 3340.
H. G. Brittain, Polymorphism in Pharmaceutical Solids, Marcel Dekker, New York 1999.
E. Doelker, S.T.P. Pharma Prat., 9 (1999) 399.
S. R. Byrn, R. R. Pfeiffer, M. Ganey, C. Hoiberg and G. Poochikian, Pharm. Res., 12 (1995) 945.
G. R. Dersiraju, I. C. Paul and D. Y. Curtin, Amer. Chem. Soc., 99 (1977) 1594.
J. T. Carstensen, Drug Stability, Principles and Practices, Marcel Dekker, New York 1995.
S. R. Vippagunta, H. G. Brittain and D. J. W. Grant, Crystalline solids, Adv. Drug Deliv. Rev., 48 (2001) 3.
N. Garti and K. Sato, Crystallization and polymorphism of fats and fatty acids. Surfactant Science Series, Vol. 31, Marcel Dekker, New York 1988.
A. Burger and J. O. Henck, Biopharm. Pharm. Technol., 1 (1995) 10.
D. Giron, J. Therm. Anal. Cal., 64 (2001) 37.
L. Borka, Spectroscopy, 5 (1990) 12.
M. Kuhnert-Brandstätter, Thermomicroscopy in the analysis of pharmaceuticals, Intern. Ser. Monog. Anal. Chem., Vol. 45 (R. Belcher and M. Freiser, Eds), Pergamon Press, Oxford and Thermomicroscopy of organic compounds in comprehensive Analytical Chemistry, Vol XVI G. Svehla Ed., Elsevier Publisher, Amsterdam 1982, p. 329.
P. M. Cooke, Anal. Chem., 68 (1996) 333R.
K. Pommerenke, Am. Lab., 32 (2000) 30.
J. Bernstein and J. O. Henck, Cryst. Eng., 1 (1998) 119.
P. Ghetti, A. Ghidini and R. Stradi, Boll. Chim. Farm., 133 (1994) 689.
U. J. Griesser, M. E. Auer and A. Burger, Microchem. J., 65 (2000) 283.
R. J. Clark, Chem. Society Reviews, (1995) 187.
P. Valisa, Lab. 2000, 11 (1997) 26.
M. Szelagiewicz, C. Marcolli, S. Cianferani, A. P. Hard, A. Vit, A. Burkhard, M. von Raumer, Ch. Hofmeier, A. Zilian, E. Francotte and R. Schenker, J. Therm. Anal. Cal., 57 (1999) 23.
R. Guerin, B. Coutois, A. Rezzouk and A. Le Roy, C. R. Acad. Sci., Ser. II, 316 (1993) 441.
M. Takeuchi, S. Ueno, J. Yano, E. Floter and K. Sato, J. Am. Oil Chem. Soc., 77 (2000) 1243.
M. Sonoyama, H. Yajima, T. Nakano, M. Matsumoto, I. Tsukushi and T. Ishii, Chem. Lett., 5 (2000) 558.
E. Husson, Key Eng. Mater., 155 (1999) 1.
P. Tandon, R. Neubert and S. Wartewig, J. Mol. Struct., 526 (2000) 49.
H. Chang, R. Murugan and A. Ghule, Thermochim. Acta, 374 (2001) 45.
M. Epple and H. K. Cammenga, J. Thermal Anal., 38 (1992) 619.
P. Conflant and A. M. Guyot-Hermann, Eur. J. Pharm. Biopharm., 40 (1994) 388.
L. O. Figura and M. Epple, J. Thermal Anal., 44 (1995) 45.
M. Epple, J. Thermal Anal., 45 (1996) 1265.
D. Giron, M. Draghi, C. Goldbronn, S. Pfeffer and P. Piechon, J. Thermal Anal., 49 (1997) 913.
R. Suneel, Z. Marek and R. Suryanarayanan, Pharm. Res., 18 (2001) 267.
G. Keller, F. Lavigne, L. Forte, K. Andrieux, M. Dahim, C. Loisel, M. Ollivon, C. Bourgaux and P. Lesieur, J. Therm. Anal. Cal., 51 (1998) 783.
M. Ollivon, C. Loisel, C. Lopez, P. Lesieur, F. Artzner and G. Keller, Cryst. Solidif. Prop. Lipids, N. Widlak, R. Hartel and S. Narine, AOCS Press, 2001 p. 34.
K. Crowley, R. T. Forbes, P. York, D. C. Apperley, H. Nyqvist and O. Camber, J. Pharm. Sci., 89 (2000), 1286.
M. Guo and H. R. Kricheldorf, Polym. Prep., 37 (1996) 366.
D. Giron, C. Goldbronn, M. Mutz, S. Pfeffer, P. Piechon and P. Schwab, J. Therm. Anal. Cal., 68 (2002) 453.
K. Byström, Thermometric company, Application Note 22004, 1990.
G. Buckton, P. Darcy, D. Greenleaf and P. Holbrook, Int. J.Pharm., 16 (1995) 113.
D. Giron, P. Remy, S. Thomas and E. Vilette, J. Thermal Anal., 48 (1997) 465.
D. Giron, P. Piechon, C. Goldbronn and S. Pfeffer, J. Therm. Anal. Cal., 57 (1999) 61.
C. Gustafsson, T. Lennholm and C. Nystrom, Int. J. Pharm., 174 (1998) 243.
S. Guinot and F. Leveiller, Int. J. Pharm., 192 (1999) 63.
B. C. Hancock and G. Zografi, Pharm. Res., 11 (1994) 471.
B. C. Hancock and G. Zografi, J. Pharm. Sci., 86 (1997) 1.
B. C. Hancok, C. R. Dalton, M. J. Pikal and S. L. Shamblin, Pharm. Res., 15 (1998) 762.
X. Chen, S. Bates and K. R. Morris, J. Pharm. Biomed. Anal., 26 (2001) 63.
J. Jacques, A. Collet and S. H. Wilen, Enantiomers, racemates and resolutions, J. Wiley, 1981.
G. Coquerel, Enantiomer, 5 (2000) 481.
A. Bakri, L. H. M. Janssen and J. Wilting, J. Thermal Anal., 33 (1988) 1193.
F. Zaman, A. E. Beezer, J. C. Mitchell, O. Clarkson, J. Elliot, M. Nishet and A. F. Davis, Int. J. Pharm., 225 (2001) 135.
J. L. Ford, Drug Dev. Ind. Pharm., 13 (1987) 1741.
A. T. M. Serajuddin, J. Pharm. Sci., 88 (1999) 1058.
R. Ficarra, P. Ficarra, M. R. Di Bella, D. Raneri, S. Tommasini, M. L. Calabro, M. C. Gamberini and C. Rustichelli, J. Pharm. Biomed., 23 (2000) 33.
C. Dubernet, Thermochim. Acta, 248 (1995) 259.
K. M. G. Taylor and R. M. Morris, Thermochim. Acta, 248 (1995) 289.
E. C. A. Van Winden, W. Zhang and D. J. A. Crommelin, Pharm. Res., 14 (1997) 1151.
P. Garidel, C. Johan and A. Blume, J. Liposome Res., 10 (2000) 131.
E. C. A. van Winden, H. Talsma and D. J. A. Crommelin, J. Pharm. Sci., 87 (1998) 231.
L. Forte, K. Andrieux, G. Keller, C. Madelmont, S. Lesieur, M. Paternostre, M. Ollivon, C. Bourgaux and R. Lesieur, J. Therm. Anal. Cal., 51 (1998) 773.
F. Franks, Dev. Biol. Stand., 74 (1992) 9.
H. Ross and F. Franks, Drug Stab., 1 (1996) 73.
A. I. Liapiz, M. J. Pikala and R. Bruttini, Drying Technol., 14 (1996) 1265.
W. Regenass, Chimia, 51 (1997) 189.
F. Stoessel, Chem. Eng. Sci., 43 (1993) 68.
J. L. Gustin, J. Loss Prevention in the Process Industries, 6 (1993) 275.
T. Arii, A. Kishi and Y. Kobayashi, Thermochim. Acta, 325 (1999) 151. and Rigaku application note presented at the 48th annual Denver X-ray conference, 1999.
M. R. Caira, Top. Curr. Chem., 198 (1998) 163.
S. Materazzi and R. Curini, Appl. Spectrosc. Rev., 36 (2001) 1.
F. Hoffmann, R. Riesen and J. Foreman, Proc. NATAS Annu. Conf. Therm. Anal. Appl., 27 (1999) 401.
T. Ozawa, Mass Spectrom. Soc., 11 (1998) 52.
C. Breen, P. M. Last, S. Taylor and P. Komadel, Thermochim. Acta, 363 (2000) 93.
E. Kaisersberger and E. Post, Thermochim. Acta, 295 (1997) 73.
O. Persenaire, M. Alexandre, P. Degee and P. Dubois, Biomacromolecules, 2 (2001) 288.
M. Maciejewski and A. Baiker, Thermochim. Acta, 295 (1997) 95.
H. M. Pollock and A. Hammiche, J. Phys. D. Appl. Phys., 34 (2001) R23.
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Giron, D. Applications of Thermal Analysis and Coupled Techniques in Pharmaceutical Industry. Journal of Thermal Analysis and Calorimetry 68, 335–357 (2002). https://doi.org/10.1023/A:1016015113795
Issue Date:
DOI: https://doi.org/10.1023/A:1016015113795