Polymer incorporation method affects the physical stability of amorphous indomethacin in aqueous suspension

European Journal of Pharmaceutics and Biopharmaceutics

Volumn 96, Issue , 2015, Pages 32-43

  Surwase, S A ^a,b   Itkonen, L ^a,b   Aaltonen, J ^b   Saville, D ^a   Rades, T ^c   Peltonen, L ^b   Strachan, C J ^b  

^a UNIVERSITY OF OTAGO   (New Zealand)

^b UNIVERSITY OF HELSINKI   (Finland)

^c UNIVERSITY OF COPENHAGEN   (Denmark)

Author keywords

Amorphous; Crystallisation; Dissolution; Indomethacin; Physical stability; Polymer; Solid dispersion; Solubility; Stabilisation; Suspension

Indexed keywords

INDOMETACIN; HYDROXYPROPYLMETHYLCELLULOSE; MACROGOL DERIVATIVE; POLYVINYL CAPROLACTAM-POLYVINYL ACETATE-POLYETHYLENE GLYCOL GRAFT COPOLYMER; POLYVINYL DERIVATIVE; POVIDONE; SOLUTION AND SOLUBILITY;

ARTICLE; CHEMISTRY; CRYSTALLIZATION; DRUG FORMULATION; DRUG STABILITY; DRUG STORAGE; INFRARED SPECTROSCOPY; PHARMACEUTICS; POWDER DIFFRACTION; PROCEDURES; SOLUBILITY; SOLUTION AND SOLUBILITY;

CRYSTALLIZATION; DRUG COMPOUNDING; DRUG STABILITY; DRUG STORAGE; HYPROMELLOSE DERIVATIVES; INDOMETHACIN; POLYETHYLENE GLYCOLS; POLYVINYLS; POVIDONE; POWDER DIFFRACTION; SOLUBILITY; SOLUTIONS; SPECTROSCOPY, FOURIER TRANSFORM INFRARED; TECHNOLOGY, PHARMACEUTICAL;

EID: 84937597307     PISSN: 09396411     EISSN: 18733441     Source Type: Journal    
DOI: 10.1016/j.ejpb.2015.06.005     Document Type: Article

References (46)

1. I. Khanna Drug discovery in pharmaceutical industry: productivity challenges and trends Drug Discov. Today 17 19-20 2012 1088 1102
2. J. Higgins, M.E. Cartwright, and et al. Progressing preclinical drug candidates: strategies on preclinical safety studies and the quest for adequate exposure Drug Discov. Today 17 15-16 2012 828 836
3. S. Gopinathan, E. O'Neill, and et al. In vivo toxicology of excipients commonly employed in drug discovery in rats J. Pharmacol. Toxcol. Methods 68 2 2013 284 295
4. K. Nagapudi, and J. Jona Amorphous active pharmaceutical ingredients in preclinical studies: preparation, characterization, and formulation Curr. Bioact. Compd. 4 4 2008 213 224
5. H.D. Williams, N.L. Trevaskis, and et al. Strategies to address low drug solubility in discovery and development Pharmacol. Rev. 65 1 2013 315 499
6. B.C. Hancock, and M. Parks What is the true solubility advantage for amorphous pharmaceuticals? Pharm. Res. 17 4 2000 397 404
7. J. Brouwers, M.E. Brewster, and et al. Supersaturating drug delivery systems: the answer to solubility-limited oral bioavailability? J. Pharm. Sci. 98 8 2009 2549 2572
8. N.J. Babu, and A. Nangia Solubility advantage of amorphous drugs and pharmaceutical cocrystals Cryst. Growth Des. 11 7 2011 2662 2679
9. S.B. Murdande, M.J. Pikal, and et al. Solubility advantage of amorphous pharmaceuticals, Part 3: Is maximum solubility advantage experimentally attainable and sustainable? J. Pharm. Sci. 100 10 2011 4349 4356
10. N. Boersen, T. Lee, and et al. Development of Preclinical Formulations for Toxicology Studies. A Comprehensive Guide to Toxicology in Preclinical Drug Development 2013 Academic Press pp. 69-86 (Chapter 4)
11. C. Bhugra, and M.J. Pikal Role of thermodynamic, molecular, and kinetic factors in crystallization from the amorphous state J. Pharm. Sci. 97 4 2008 1329 1349
12. M. Savolainen, K. Kogermann, and et al. Better understanding of dissolution behaviour of amorphous drugs by in situ solid-state analysis using Raman spectroscopy Eur. J. Pharm. Biopharm. 71 1 2009 71 79
13. S. Ozaki, I. Kushida, and et al. Evaluation of drug supersaturation by thermodynamic and kinetic approaches for the prediction of oral absorbability in amorphous pharmaceuticals J. Pharm. Sci. 101 11 2012 4220 4230
14. J.A. Baird, and L.S. Taylor Evaluation of amorphous solid dispersion properties using thermal analysis techniques Adv. Drug Deliv. Rev. 64 5 2012 396 421
15. R. Laitinen, K. Löbmann, and et al. Emerging trends in the stabilization of amorphous drugs Int. J. Pharm. 453 1 2013 65 79
16. A. Paudel, E. Nies, and et al. Relating hydrogen-bonding interactions with the phase behavior of Naproxen/PVP K 25 solid dispersions: evaluation of solution-cast and quench-cooled films Mol. Pharm. 9 11 2012 3301 3317
17. H. Sekikawa, M. Nakano, and et al. Inhibitory effect of polyvinylpyrrolidone on the crystallization of drugs Chem. Pharm. Bull. 26 1 1978 118 126
18. S.L. Raghavan, A. Trividic, and et al. Crystallization of hydrocortisone acetate: influence of polymers Int. J. Pharm. 212 2 2001 213 221
19. Y. Yokoi, E. Yonemochi, and et al. Effects of sugar ester and hydroxypropyl methylcellulose on the physicochemical stability of amorphous cefditoren pivoxil in aqueous suspension Int. J. Pharm. 290 1-2 2005 91 99
20. D.B. Warren, H. Benameur, and et al. Using polymeric precipitation inhibitors to improve the absorption of poorly water-soluble drugs: a mechanistic basis for utility J. Drug Target. 18 10 2010 704 731
21. V.G. Kadajji, and G.V. Betageri Water soluble polymers for pharmaceutical applications Polymers 3 4 2011 1972 2009
22. B.C. Hancock, S.L. Shamblin, and et al. Molecular mobility of amorphous pharmaceutical solids below their glass transition temperatures Pharm. Res. 12 6 1995 799 806
23. V. Andronis, M. Yoshioka, and et al. Effects of sorbed water on the crystallization of indomethacin from the amorphous state J. Pharm. Sci. 86 3 1997 346 351
24. V. Andronis, and G. Zografi Crystal nucleation and growth of indomethacin polymorphs from the amorphous state J. Non-Cryst. Solids 271 3 2000 236 248
25. D. Alonzo, G.Z. Zhang, and et al. Understanding the behavior of amorphous pharmaceutical systems during dissolution Pharm. Res. 27 4 2010 608 618
26. K. Greco, and R. Bogner Crystallization of amorphous Indomethacin during dissolution: effect of processing and annealing Mol. Pharm. 7 5 2010 1406 1418
27. C.R. Raymond, P.J. Sheskey, and et al. Handbook of Pharmaceutical Excipients 2006 Pharmaceutical Press and the American Pharmacists Association London
28. S. Ali, Soluplus® - The Solid Solution Opening New Doors in Solubilization. < http://www.pharma-ingredients.basf.com/Documents/ENP/Brochure/EN/RZ-BASF-Broschure-Soluplus.pdf > (retrieved 15.08.12).
29. L.S. Taylor, and G. Zografi Spectroscopic characterization of interactions between PVP and Indomethacin in amorphous molecular dispersions Pharm. Res. 14 12 1997 1691 1698
30. M. Yoshioka, B.C. Hancock, and et al. Inhibition of indomethacin crystallization in poly(vinylpyrrolidone) coprecipitates J. Pharm. Sci. 84 8 1995 983 986
31. M. Savolainen, A. Heinz, and et al. Screening for differences in the amorphous state of indomethacin using multivariate visualization Eur. J. Pharm. Sci. 30 2 2007 113 123
32. S.A. Surwase, J.P. Boetker, and et al. Indomethacin: new polymorphs of an old drug Mol. Pharm. 10 12 2013 4472 4480
33. M. Yoshioka, B.C. Hancock, and et al. Crystallization of indomethacin from the amorphous state below and above its glass transition temperature J. Pharm. Sci. 83 12 1994 1700 1705
34. P. Karmwar, K. Graeser, and et al. Investigation of properties and recrystallisation behaviour of amorphous indomethacin samples prepared by different methods Int. J. Pharm. 417 1-2 2011 94 100
35. A. Forster, J. Hempenstall, and et al. Characterization of glass solutions of poorly water-soluble drugs produced by melt extrusion with hydrophilic amorphous polymers J. Pharm. Pharmacol. 53 3 2001 303 315
36. D. Smithey, J. Fennewald, and et al. Evaluation of Soluplus® Spray Dried Dispersion for Poorly Soluble Compounds 2010 American Association of Pharmaceutical Scientists New Orleans, LA, US
37. K. Gong, I.U. Rehman, and et al. Characterization and drug release investigation of amorphous drug-hydroxypropyl methylcellulose composites made via supercritical carbon dioxide assisted impregnation J. Pharm. Biomed. Anal. 48 4 2008 1112 1119
38. A.C.F. Rumondor, and L.S. Taylor Effect of polymer hygroscopicity on the phase behavior of amorphous solid dispersions in the presence of moisture Mol. Pharm. 7 2 2009 477 490
39. P. Dani, V. Puri, and et al. Solubility advantage from amorphous etoricoxib solid dispersions Drug Dev. Ind. Pharm. 2013 1 10
40. M. Maniruzzaman, D.J. Morgan, and et al. Drug-polymer intermolecular interactions in hot-melt extruded solid dispersions Int. J. Pharm. 443 1-2 2013 199 208
41. L.A. Wegiel, L.J. Mauer, and et al. Crystallization of amorphous solid dispersions of resveratrol during preparation and storage - impact of different polymers J. Pharm. Sci. 102 1 2013 171 184
42. K. Kawakami Modification of physicochemical characteristics of active pharmaceutical ingredients and application of supersaturable dosage forms for improving bioavailability of poorly absorbed drugs Adv. Drug Deliv. Rev. 64 6 2012 480 495
43. J. Gong, M. Chen, and et al. Polymeric micelles drug delivery system in oncology J. Control. Release 159 3 2012 312 323
44. T. Ozeki, H. Yuasa, and et al. Mechanism of medicine release from solid dispersion composed of poly(ethylene oxide)-carboxyvinylpolymer interpolymer complex and pH effect on medicine release Int. J. Pharm. 171 1 1998 123 132
45. P. Tran, T. Tran, and et al. Controlled release systems containing solid dispersions: strategies and mechanisms Pharm. Res. 28 10 2011 2353 2378
46. G. Terife, P. Wang, and et al. Hot melt mixing and foaming of Soluplus® and indomethacin Polym. Eng. Sci. 52 8 2012 1629 1639