A slow cooling rate of indomethacin melt spatially confined in microcontainers increases the physical stability of the amorphous drug without influencing its biorelevant dissolution behaviour

Drug Delivery and Translational Research

Volumn 4, Issue 3, 2014, Pages 268-274

  Nielsen, Line Hagner ^a   Keller, Stephan Sylvest ^b   Boisen, Anja ^b   Müllertz, Anette ^a,c   Rades, Thomas ^a  

^a UNIVERSITY OF COPENHAGEN   (Denmark)

^b TECHNICAL UNIVERSITY OF DENMARK   (Denmark)

^c BIONEER A S   (Denmark)

Author keywords

Amorphous form preparation; Amorphous indomethacin; Biorelevant dissolution; Physical stability; Raman microscopy

Indexed keywords

ICE; INDOMETACIN; LIQUID NITROGEN;

ARTICLE; COOLING; DISSOLUTION; DRUG DELIVERY SYSTEM; DRUG DOSAGE FORM; DRUG STABILITY; DRUG STORAGE; MORPHOLOGY; PH; PRIORITY JOURNAL; ROOM TEMPERATURE; SCANNING ELECTRON MICROSCOPY;

EID: 84900005336     PISSN: 2190393X     EISSN: 21903948     Source Type: Journal    
DOI: 10.1007/s13346-013-0166-7     Document Type: Article

References (27)

1. Ainslie KM, Lowe RD, Beaudette TT, Petty L, Bachelder EM, Desai TA. Microfabricated devices for enhanced bioadhesive drug delivery: attachment to and small-molecule release through a cell monolayer under flow. Small. 2009;5: 2857-63.
2. Ahmed A, Bonner C, Desai TA. Bioadhesive microdevices with multiple reservoirs: a new platform for oral drug delivery. J Control Release. 2002;81(3): 291-306.
3. Tao SL, Lubeley MW, Desai TA. Bioadhesive poly(methyl methacrylate) microdevices for controlled drug delivery. J Control Release. 2003;88(2): 215-28.
4. Lipinski CA, Lombardo F, Dominy BW, Feeney PJ. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv Drug Deliv Rev. 2001;46(1-3): 3-26.
5. Hancock BC, Zografi G. Characteristics and significance of the amorphous state in pharmaceutical systems. J Pharm Sci. 1997;86(1): 1-12.
6. Yu L. Amorphous pharmaceutical solids: preparation, characterization and stabilization. Adv Drug Deliv Rev. 2001;48(1): 27-42.
7. Bates S, Zografi G, Engers D, Morris K, Crowley K, Newman A. Analysis of amorphous and nanocrystalline solids from their X-ray diffraction patterns. Pharm Res. 2006;23(10): 2333-49.
8. Ambike AA, Mahadik KR, Paradkar A. Stability study of amorphous valdecoxib. Int J Pharm. 2004;282(1-2): 151-62.
9. Chieng N, Rades T, Saville D. Formation and physical stability of the amorphous phase of ranitidine hydrochloride polymorphs prepared by cryo-milling. Eur J Pharm Biopharm. 2008;68(3): 771-80.
10. Wu T, Sun Y, Li N, de Villiers MM, Yu L. Inhibiting surface crystallization of amorphous indomethacin by nanocoating. Langmuir. 2007;23(9): 5148-53.
11. Crowley KJ, Zografi G. The effect of low concentrations of molecularly dispersed poly(vinylpyrrolidone) on indomethacin crystallization from the amorphous state. Pharm Res. 2003;20(9): 1417-22.
12. Nielsen LH, Keller SS, Gordon KC, Boisen A, Rades T, Mullertz A. Spatial confinement can lead to increased stability of amorphous indomethacin. Eur J Pharm Biopharm. 2012;81(2): 418-25.
13. Strachan CJ, Rades T, Gordon KC, Rantanen J. Raman spectroscopy for quantitative analysis of pharmaceutical solids. J Pharm Pharmacol. 2007;59(2): 179-92.
14. Winter CA, Risley EA, Nuss GW. Anti-inflammatory and antipyretic activities of indomethacin, 1-(P-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetic acid. J Pharmacol Exp Ther. 1963;141: 369-76.
15. Aceves-Hernandez JM, Nicolas-Vazquez I, Aceves FJ, Hinojosa-Torres J, Paz M, Castano VM. Indomethacin polymorphs: experimental and conformational analysis. J Pharm Sci. 2009;98(7): 2448-63.
16. Andronis V, Yoshioka M, Zografi G. Effects of sorbed water on the crystallization of indomethacin from the amorphous state. J Pharm Sci. 1997;86(3): 346-51.
17. Karmwar P, Graeser K, Gordon KC, Strachan CJ, Rades T. Investigation of properties and recrystallisation behaviour of amorphous indomethacin samples prepared by different methods. Int J Pharm. 2011;417: 94-100.
18. Graeser KA, Strachan CJ, Patterson JE, Gordon KC, Rades T. Physicochemical properties and stability of two differently prepared amorphous forms of simvastatin. Crystal Growth Des. 2008;8(1): 128-35.
19. Bhugra C, Shmeis R, Pikal MJ. Role of mechanical stress in crystallization and relaxation behavior of amorphous indomethacin. J Pharm Sci. 2008;97(10): 4446-58.
20. Karmwar P, Boetker JP, Graeser KA, Strachan CJ, Rantanen J, Rades T. Investigations on the effect of different cooling rates on the stability of amorphous indomethacin. Eur J Pharm Sci. 2011;44(3): 341-50.
21. Yoshioka M, Hancock BC, Zografi G. Crystallization of indomethacin from the amorphous state below and above its glass transition temperature. J Pharm Sci. 1994;83(12): 1700-5.
22. Ayenew Z, Paudel A, Rombaut P, van den Mooter G. Effect of compression on non-isothermal crystallization behaviour of amorphous indomethacin. Pharm Res. 2012;29(9): 2489-98.
23. Fukuoka E, Makita M, Yamamura S. Some physicochemical properties of glassy indomethacin. Chem Pharm Bull (Tokyo). 1986;34(10): 4314-21.
24. Forster A, Hempenstall J, Rades T. Characterization of glass solutions of poorly water-soluble drugs produced by melt extrusion with hydrophilic amorphous polymers. J Pharm Pharmacol. 2001;53(3): 303-15.
25. Karmwar P, Graeser K, Gordon KC, Strachan CJ, Rades T. Effect of different preparation methods on the dissolution behaviour of amorphous indomethacin. Eur J Pharm Biopharm. 2012;80(2): 459-64.
26. Tao SL, Popat K, Desai TA. Off-wafer fabrication and surface modification of asymmetric 3D SU-8 microparticles. Nat Protoc. 2007;1(6): 3153-8.
27. Carpentier L, Decressain R, Desprez S, Descamps M. Dynamics of the amorphous and crystalline alpha-, gamma-phases of indomethacin. J Phys Chem B. 2006;110(1): 457-64.