Compression-induced crystallization of amorphous indomethacin in tablets: Characterization of spatial heterogeneity by two-dimensional X-ray diffractometry

Molecular Pharmaceutics

Volumn 12, Issue 1, 2015, Pages 253-263

  Thakral, Naveen K ^a,b   Mohapatra, Sarat ^b   Stephenson, Gregory A ^a   Suryanarayanan, Raj ^b  

^a ELI LILLY AND COMPANY   (United States)

^b UNIVERSITY OF MINNESOTA   (United States)

Author keywords

amorphous; compression; crystallization; depth profiling; indomethacin; synchrotron; tablet; two dimensional X ray diffractometry

Indexed keywords

INDOMETACIN; LUBRICATING AGENT; MAGNESIUM STEARATE; POLYETHYLENE TEREPHTHALATE; EXCIPIENT; STEARIC ACID; STEARIC ACID DERIVATIVE; TABLET;

ANALYTIC METHOD; ARTICLE; CHEMICAL COMPOSITION; COMPRESSION; COMPRESSION PRESSURE; CRYSTALLIZATION; DIE WALL FRICTION; DRUG BIOAVAILABILITY; DRUG DESIGN; DRUG MANUFACTURE; FRICTION; PRESSURE; SYNCHROTRON RADIATION; TABLET; X RAY DIFFRACTION; CHEMISTRY; COMPRESSIVE STRENGTH; SCANNING ELECTRON MICROSCOPY; SURFACE PROPERTY; SYNCHROTRON;

COMPRESSIVE STRENGTH; CRYSTALLIZATION; EXCIPIENTS; INDOMETHACIN; MICROSCOPY, ELECTRON, SCANNING; PRESSURE; STEARIC ACIDS; SURFACE PROPERTIES; SYNCHROTRONS; TABLETS; X-RAY DIFFRACTION;

EID: 84920440109     PISSN: 15438384     EISSN: 15438392     Source Type: Journal    
DOI: 10.1021/mp5005788     Document Type: Article

References (32)

1. Thayer, A. M. Finding Solutions Chem. Eng. News 2010, 88 (22) 13-18
2. Joshi, A. B.; Patel, S.; Kaushal, A. M.; Bansal, A. K. Compaction studies of alternate solid forms of celecoxib Adv. Powder Technol. 2010, 21 (4) 452-460
3. Vyazovkin, S.; Dranca, I. Effect of Physical Aging on Nucleation of Amorphous Indomethacin J. Phys. Chem. B 2007, 111 (25) 7283-7287
4. Wu, C. T.; Luo, H. L. Pressure effect on vapor-deposited amorphous materials J. Non-Cryst. Solids 1975, 18 (1) 21-28
5. Mackenzie, J. D. High-Pressure Effects on Oxide Glasses: I, Densification in Rigid State J. Am. Ceram. Soc. 1963, 46 (10) 461-470
6. Wojnarowska, Z.; Adrjanowicz, K.; Wlodarczyk, P.; Kaminska, E.; Kaminski, K.; Grzybowska, K.; Wrzalik, R.; Paluch, M.; Ngai, K. Broadband dielectric relaxation study at ambient and elevated pressure of molecular dynamics of pharmaceutical: indomethacin J. Phys. Chem. B 2009, 113 (37) 12536-12545
7. Adrjanowicz, K.; Grzybowski, A.; Grzybowska, K.; Pionteck, J.; Paluch, M. Toward Better Understanding Crystallization of Supercooled Liquids under Compression: Isochronal Crystallization Kinetics Approach Cryst. Growth Des. 2013, 13 (11) 4648-4654
8. Macleod, H. M.; Marshall, U. The determination of density distribution in ceramic compacts using autoradiography Powder Technol. 1977, 16 (1) 107-122
9. Sinka, I. C.; Burch, S. F.; Tweed, J. H.; Cunningham, J. C. Measurement of density variations in tablets using X-ray computed tomography Int. J. Pharm. 2004, 271 (1-2) 215-224
10. Henson, M. J.; Zhang, L. Drug Characterization in Low Dosage Pharmaceutical Tablets Using Raman Microscopic Mapping Appl. Spectrosc. 2006, 60 (11) 1247-1255
11. Koradia, V.; Tenho, M.; Lopez de Diego, H.; Ringkjøbing-Elema, M.; Møller-Sonnergaard, J.; Salonen, J.; Lehto, V.-P.; Rantanen, J. Investigation of Solid Phase Composition on Tablet Surfaces by Grazing Incidence X-ray Diffraction Pharm. Res. 2012, 29 (1) 134-144
12. Thakral, N. K.; Ragoonanan, V.; Suryanarayanan, R. Quantification, Mechanism, and Mitigation of Active Ingredient Phase Transformation in Tablets Mol. Pharmaceutics 2013, 10 (8) 3128-3136
13. He, B. B. Two-dimensional X-ray Diffraction; John Wiley & Sons: 2011.
14. Yoshioka, M.; Hancock, B. C.; Zografi, G. Crystallization of indomethacin from the amorphous state below and above its glass transition temperature J. Pharm. Sci. 1994, 83 (12) 1700-1705
15. Bhugra, C.; Shmeis, R.; Pikal, M. J. Role of mechanical stress in crystallization and relaxation behavior of amorphous indomethacin J. Pharm. Sci. 2008, 97 (10) 4446-4458
16. Ayenew, Z.; Paudel, A.; Rombaut, P.; Mooter, G. Effect of Compression on Non-isothermal Crystallization Behaviour of Amorphous Indomethacin Pharm. Res. 2012, 29 (9) 2489-2498
17. Hammersley, A. P. Fit2D: an introduction and overview; ESRF internal report, ESRF97HA02T; 1997.
18. Hammersley, A. P. Two dimensional detector software; from real detector to idealised image or two-theta scan Int. J. High Pressure Res. 1996, 14 (4-6) 235-248
19. Busignies, V.; Leclerc, B.; Porion, P.; Evesque, P.; Couarraze, G.; Tchoreloff, P. Quantitative measurements of localized density variations in cylindrical tablets using X-ray microtomography Eur. J. Pharm. Biopharm. 2006, 64 (1) 38-50
20. Siiriä, S. M.; Antikainen, O.; Heinämäki, J.; Yliruusi, J. 3D simulation of internal tablet strength during tableting AAPS PharmSciTech 2011, 12 (2) 593-603
21. Ellison, C. D.; Ennis, B. J.; Hamad, M. L.; Lyon, R. C. Measuring the distribution of density and tabletting force in pharmaceutical tablets by chemical imaging J. Pharm. Biomed. Anal. 2008, 48 (1) 1-7
22. Briscoe, B. J.; Rough, S. L. The effects of wall friction on the ejection of pressed ceramic parts Powder Technol. 1998, 99 (3) 228-233
23. Wu, C.-Y.; Ruddy, O. H.; Bentham, B. C.; Hancock, B. C.; Best, S. M.; Elliott, J. A. Modelling the mechanical behaviour of pharmaceutical powders during compaction Powder Technol. 2005, 152 (1) 107-117
24. Sinka, I. C.; Cunningham, J. C.; Zavaliangos, A. The effect of wall friction in the compaction of pharmaceutical tablets with curved faces: a validation study of the Drucker-Prager Cap model Powder Technol. 2003, 133 (1) 33-43
25. Nelson, E.; Naqvi, S.; Busse, L.; Higuchi, T. The physics of tablet compression: IV. Relationship of ejection, and upper and lower punch forces during compressional process: Application of measurements to comparison of tablet lubricants J. Am. Pharm. Assoc. 1954, 43 (10) 596-602
26. Moody, G.; Rubinstein, M.; FitzSimmons, R. Tablet lubricants I. Theory and modes of action Int. J. Pharm. 1981, 9 (2) 75-80
27. Wang, J.; Wen, H.; Desai, D. Lubrication in tablet formulations Eur. J. Pharm. Biopharm. 2010, 75 (1) 1-15
28. Wu, T.; Yu, L. Surface crystallization of indomethacin below Tg Pharm. Res. 2006, 23 (10) 2350-2355
29. Zhu, L.; Wong, L.; Yu, L. Surface-enhanced crystallization of amorphous nifedipine Mol. Pharmaceutics 2008, 5 (6) 921-926
30. Wu, T.; Sun, Y.; Li, N.; de Villiers, M. M.; Yu, L. Inhibiting surface crystallization of amorphous indomethacin by nanocoating Langmuir 2007, 23 (9) 5148-5153
31. Zhang, S.-W.; Yu, L.; Huang, J.; Hussain, M. A.; Derdour, L.; Qian, F.; de Villiers, M. M. A Method to Evaluate the Effect of Contact with Excipients on the Surface Crystallization of Amorphous Drugs AAPS PharmSciTech 2014, 1-11
32. Jahn, T.; Steffens, K.-J. Press chamber coating as external lubrication for high speed rotary presses: Lubricant spray rate optimization Drug Dev. Ind. Pharm. 2005, 31 (10) 951-957