Isothermal microcalorimetry for quantifying amorphous content in processed pharmaceuticals

Advanced Drug Delivery Reviews

Volumn 64, Issue 5, 2012, Pages 431-439

  Gaisford, Simon ^a,b  

^a UNIVERSITY OF LONDON   (United Kingdom)

^b MONASH UNIVERSITY   (Australia)

Author keywords

Amorphous content quantification assay; Gas perfusion; Isothermal microcalorimetry; Pharmaceutical

Indexed keywords

AMORPHOUS CONTENT; CRITICAL FACTORS; DATA INTERPRETATION; ISOTHERMAL MICROCALORIMETRY; PARTICLE SURFACE; PHARMACEUTICAL APPLICATIONS; PHARMACEUTICAL POWDER; POWDER FLOW; PROCESSING STEPS; VAPOUR PRESSURES;

ADHESION; DATA PROCESSING; DESIGN; DRUG PRODUCTS; ISOTHERMS; MAGNESIUM PRINTING PLATES; PRODUCT DEVELOPMENT; SELF ASSEMBLY;

AMORPHOUS MATERIALS;

ACETONE; ACETONITRILE; ALCOHOL; ERYTHROMYCIN; GRISEOFULVIN; LACTOSE; PLASTICIZER; PROPANOL; WATER;

ADSORPTION; AMPOULE; CALIBRATION; CHEMICAL PROCEDURES; CRYSTALLIZATION; DIFFERENTIAL SCANNING CALORIMETRY; DYNAMIC VAPOR SORPTION; ENTHALPY; EXPERIMENTAL DESIGN; GAS PERFUSION; HUMIDITY; ISOTHERMAL MICROCALORIMETRY; LIMIT OF DETECTION; LIMIT OF QUANTITATION; MICROCALORIMETRY; NUCLEAR MAGNETIC RESONANCE; PERFUSION; POWDER; PRIORITY JOURNAL; QUANTITATIVE ANALYSIS; REVIEW; THERMODYNAMICS; VAPOR PRESSURE; WATER ABSORPTION; X RAY POWDER DIFFRACTION;

CALORIMETRY; CHEMISTRY, PHARMACEUTICAL; PLASTICIZERS;

EID: 84858798826     PISSN: 0169409X     EISSN: 18728294     Source Type: Journal    
DOI: 10.1016/j.addr.2011.11.001     Document Type: Review

References (64)

1. Newell H.E., Buckton G., Butler G.D.A., Thielmann F., Williams D.R. The use of inverse phase gas chromatography to measure the surface energy of crystalline, amorphous and recently milled lactose. Pharm. Res. 2001, 18:662-666.
2. Giron D., Monnier S., Mutz M., Piechon P., Buser T., Stowasser F., Schulze K., Bellus M. Comparison of quantitative methods for analysis of polyphasic pharmaceuticals. J. Therm. Anal. Cal. 2007, 89:729-743.
3. Chen X., Bates S., Morris K.R. Quantifying amorphous content of lactose using parallel beam X-ray powder diffraction and whole pattern fitting. J. Pharm. Biomed. Anal. 2001, 26:63-72.
4. Taylor L.S., Zografi G. The quantitative analysis of crystallinity using FT-Raman spectroscopy. Pharm. Res. 1998, 15:755-761.
5. Gombás A., Antal I., Szabó-Révész P., Marton S., Erõs I. Quantitative determination of crystallinity of alpha-lactose monohydrate by near infrared spectroscopy (NIRS). Int. J. Pharm. 2003, 256:25-32.
6. Lefort R., De Gusseme A., Willart J.-F., Danède F., Descamps M. Solid state NMR and DSC methods for quantifying the amorphous content in solid dosage forms: an application to ball-milling of trehalose. Int. J. Pharm. 2004, 280:209-219.
7. Vollenbroek J., Hebbink G.A., Ziffels S., Steckel H. Determination of low levels of amorphous content in inhalation grade lactose by moisture sorption isotherms. Int. J. Pharm. 2010, 395:62-70.
8. Saklatvala R., Royall P.G., Craig D.Q.M. The detection of amorphous material in a nominally crystalline drug using modulated temperature DSC - a case study. Int. J. Pharm. 1999, 192:55-62.
9. Gabbott P., Clarke P., Mann T., Royall P., Shergill S. A high-sensitivity, high-speed DSC technique: measurement of amorphous lactose. Am. Lab. 2003, 35:17-22.
10. Lappalainen M., Karppinen M. Techniques of differential scanning calorimetry for quantification of low contents of amorphous phases. J. Therm. Anal. Cal. 2010, 102:171-180.
11. Lappalainen M., Pitkänen I., Harjunen P. Quantification of low levels of amorphous content in sucrose by hyperDSC. Int. J. Pharm. 2006, 307:150-155.
12. Pikal M.J., Lukes A.L., Lang J.E., Gaines K. Quantitative crystallinity determinations for β-lactam antibiotics by solution calorimetry: correlations with stability. J. Pharm. Sci. 1978, 67:767-772.
13. Guillory J.K., Erb D.M. Using solution calorimetry to quantitate binary mixtures of three crystalline forms of sulfamethoxazole. Pharm. Manuf. Sep 1985, 28-33.
14. Gao D., Rytting J.H. Use of solution calorimetry to determine the extent of crystallinity of drugs and excipients. Int. J. Pharm. 1997, 151:183-192.
15. Hogan S.E., Buckton G. The quantification of small degrees of disorder in lactose using solution calorimetry. Int. J. Pharm. 2000, 207:57-64.
16. Harjunen P., Lehto V.-P., Koivisto M., Levonen E., Paronen P., Järvinen K. Determination of amorphous content of lactose samples by solution calorimetry. Drug Dev. Ind. Pharm. 2004, 30:809-815.
17. Royall P.G., Gaisford S. Application of solution calorimetry in pharmaceutical and biopharmaceutical research. Curr. Pharm. Biotech. 2005, 6:215-222.
18. Byström K. Microcalorimetric testing of physical stability of drugs in the solid state. Application note M22004 1990, http://www.tainstruments.com.
19. Bakri A. Design, testing and pharmaceutical applications of a gas pressure controller device for solid-gas microcalorimetric titration, Application Note M22021 1993, http://www.tainstruments.com.
20. Bakri A. Novel calorimetric approach to the study of interactions between gases and materials. Proc. 25th North American Thermal Analysis Society (NATAS) conference 1997.
21. Lechuga-Ballesteros D., Bakri A., Miller D.P. Microcalorimetric measurement of the interactions between water vapour and amorphous pharmaceutical solids. Pharm. Res. 2003, 20:308-318.
22. Buckton G., Darcy P. Water mobility in amorphous lactose below and close to the glass transition temperature. Int. J. Pharm. 1996, 136:141-146.
23. Buckton G., Darcy P. Assessment of disorder in crystalline powders - a review of analytical techniques and their application. Int. J. Pharm. 1999, 179:141-158.
24. Greenspan L. Humidity fixed of binary saturated aqueous solutions. J. Res. Nat. Bur. Stand. 1977, 81A:89-96.
25. Hogan S.E., Buckton G. Water sorption/desorption - near IR and calorimetric study of crystalline and amorphous raffinose. Int. J. Pharm. 2001, 227:57-69.
26. Khalef N., Pinal R., Bakri A. Limitations of amorphous content quantification by isothermal calorimetry using saturated salt solutions to control relative humidity: alternative methods. J. Pharm. Sci. 2010, 99:2080-2089.
27. Briggner L.E., Buckton G., Byström K., Darcy P. The use of isothermal microcalorimetry in the study of changes in crystallinity induced during the processing of powders. Int. J. Pharm. 1994, 105:125-135.
28. Aso Y., Yoshioka S., Otsuka T., Kojima S. The physical stability of amorphous nifedipine determined by isothermal microcalorimetry. Chem. Pharm. Bull. 1995, 43:300-303.
29. Buckton G., Darcy P., Greenleaf D., Holbrook P. The use of isothermal microcalorimetry in the study of changes in crystallinity of spray-dried salbutamol sulphate. Int. J. Pharm. 1995, 116:113-118.
30. O'Neill M.A.A., Gaisford S. Application and use of isothermal calorimetry in pharmaceutical development. Int. J. Pharm. 2011, 417:83-93.
31. A. Sunkara, S. Gaisford, Use of powder-pockets to improve amorphous detection and quantification limits by isothermal microcalorimetry, J. Pharm. Biomed. Anal. submitted for publication.
32. Baronsky J., Bonaerts S., Traeubel M., Urbanetz N. Isothermal microcalorimetry perfusion experiments: a method to verify the relative vapour pressure of organic liquids inside the sample vessel. Thermochimica Acta 2009, 493:37-41.
33. Phillips E.M. An approach to estimate the amorphous content of pharmaceutical powders using calorimetry with no calibration standards. Int. J. Pharm. 1997, 149:267-271.
34. Hancock B.C. Comments on "An approach to estimate the amorphous content of pharmaceutical powders using calorimetry with no calibration standards". Int. J. Pharm. 1998, 160:131-133.
35. Ramos R., Gaisford S., Buckton G. Calorimetric determination of amorphous content in lactose: a note on the preparation of calibration curves. Int. J. Pharm. 2005, 300:13-21.
36. Brodka-Pfeiffer K., Langguth P., Graβ P., Häusler H. Influence of mechanical activation on the physical stability of salbutamol sulphate. Eur. J. Pharm. Biopharm. 2003, 56:393-400.
37. Angberg M., Nyström C., Castensson S. Evaluation of heat-conduction microcalorimetry in pharmaceutical stability studies. III. Crystallographic changes due to water vapour uptake in anhydrous lactose powder. Int. J. Pharm. 1991, 73:209-220.
38. Angberg M., Nyström C., Castensson S. Evaluation of heat conduction microcalorimetry in pharmaceutical stability studies. V. A new approach for continuous measurements in abundant water vapour. Int. J. Pharm. 1992, 81:153-167.
39. Angberg M., Nyström C., Castensson S. Evaluation of heat-conduction microcalorimetry in pharmaceutical stability studies. VI. Continuous monitoring of the interaction of water vapour with powders and powder mixtures at various relative humidities. Int. J. Pharm. 1992, 83:11-23.
40. Sebhatu T., Angberg M., Ahlneck C. Assessment of the degree of disorder in crystalline solids by isothermal microcalorimetry. Int. J. Pharm. 1994, 104:135-144.
41. Timmermann I.-L., Steckel H., Trunk M. Assessing the re-crystallization behaviour of amorphous lactose using the RH-perfusion cell. Eur. J. Pharm. Biopharm. 2006, 64:107-114.
42. Chidavaenzi O.C., Buckton G., Koosha F., Pathak R. The use of thermal techniques to assess the impact of feed concentration on the amorphous content and polymorphic forms present in spray dried lactose. Int. J. Pharm. 1997, 159:67-74.
43. Chidavaenzi O.C., Buckton G., Koosha F. The effect of co-spray drying with polyethylene glycol 4000 on the crystallinity and physical form of lactose. Int. J. Pharm. 2001, 216:43-49.
44. Gustafsson C., Lennholm H., Iversen T., Nyström C. Comparison of solid state NMR and isothermal microcalorimetry in the assessment of the amorphous component of lactose. Int. J. Pharm. 1998, 174:243-252.
45. Dilworth S., Buckton G., Gaisford S., Ramos R. Approaches to determine the enthalpy of crystallization, and amorphous content, of lactose from isothermal microcalorimetry data. Int. J. Pharm. 2004, 284:83-94.
46. Lehto V.P., Tenho M., Vaha-Heikkila V.K., Harjunen P., Paallysaho M., Valissaari J., Niemela P., Jarvinen K. The comparison of seven different methods to quantify the amorphous content of spray dried lactose. Powder Tech. 2006, 167:85-93.
47. Steckel H., Bolzen N. Calorimetric study on amorphous lactose during and after recrystallization at different relative humidity. Pharm. Ind. 2005, 67:709-712.
48. Ziffels S., Steckel H. Influence of amorphous content on compaction behaviour of anhydrous α-lactose. Int. J. Pharm. 2010, 387:71-78.
49. Ziffels S., Schwarz E., Hartwig S. Recrystallisation behaviour of partially amorphous lactose during and after compression. Pharm. Ind. 2010, 72:508-521.
50. Cook P.A., Dellman C.I., Horspool K.R., Lukas T.M., Marshall P.V., Nichols G., Smith D., Ticehurst M.D. The characterisation and quantification of amorphous content of micronized drug particles. Eur. J. Pharm. Sci. 1996, 4:S181.
51. Giron D., Remy P., Thomas S., Vilette E. Quantitation of amorphicity by microcalorimetry. J. Therm. Anal. Cal. 1997, 48:465-472.
52. Ahmed H., Buckton G., Rawlins D.A. Crystallisation of partially amorphous griseofulvin in water vapour: determination of kinetic parameters using isothermal heat conduction microcalorimetry. Int. J. Pharm. 1998, 167:139-145.
53. Lehto V.-P., Laine E. Assessment of physical stability of different forms of cefadroxil at high humidities. Int. J. Pharm. 1998, 163:49-62.
54. Fiebich K., Mutz M. Evaluation of calorimetric and gravimetric methods to quantify the amorphous content of desferal. J. Therm. Anal. Cal. 1999, 57:75-85.
55. Kawakami K., Miyoshi K., Tamura N., Yamaguchi T., Ida Y. Crystallisation of sucrose glass under ambient conditions: evaluation of crystallisation rate and unusual melting behaviour of resultant crystals. J. Pharm. Sci. 2006, 95:1354-1363.
56. Brodka-Pfeiffer K., Häusler H., Graβ P., Langguth P. Conditioning following powder micronization: Influence on particle growth of salbutamol sulphate. Drug Dev. Ind. Pharm. 2003, 29:1077-1084.
57. Gaisford S., Dennison M., Tawfik M., Jones M.D. Following mechanical activation of salbutamol sulphate during ball-milling with isothermal calorimetry. Int. J. Pharm. 2010, 393:74-78.
58. Kawakami K., Numa T., Ida Y. Assessment of amorphous content by microcalorimetry. J. Pharm. Sci. 2002, 91:417-423.
59. Vemuri N.M., Chrzan Z., Cavatur R. Use of isothermal microcalorimetry in pharmaceutical preformulation studies, part II. Amorphous phase quantification in a predominantly crystalline phase. J. Therm. Anal. Cal. 2004, 78:55-62.
60. Mackin L., Zanon R., Park J.M., Foster K., Opalenik H., Demonte M. Quantification of low levels (<10%) of amorphous content in micronized active batches using dynamic vapour sorption and isothermal microcalorimetry. Int. J. Pharm. 2002, 231:227-236.
61. Samra R.M., Buckton G. The crystallisation of a model hydrophobic drug (terfenadine) following exposure to humidity and organic vapours. Int. J. Pharm. 2004, 284:53-60.
62. Ahmed H., Buckton G., Rawlins D.A. The use of isothermal microcalorimetry in the study of small degrees of amorphous content of a hydrophobic powder. Int. J. Pharm. 1996, 130:195-201.
63. Al-Hadithi D., Buckton G., Brocchini S. Quantification of amorphous content in mixed systems: amorphous trehalose with lactose. Thermochimica Acta 2004, 417:193-199.
64. Darcy P., Buckton G. Quantitative assessments of powder crystallinity: estimates of heat and mass transfer to interpret isothermal microcalorimetry data. Thermochimica Acta 1998, 316:29-36.