Formulation and delivery of improved amorphous fenofibrate solid dispersions prepared by thin film freezing

European Journal of Pharmaceutics and Biopharmaceutics

Volumn 82, Issue 3, 2012, Pages 534-544

  Zhang, Meimei ^a,b   Li, Houli ^b   Lang, Bo ^b   O'Donnell, Kevin ^b   Zhang, Haohao ^a   Wang, Zhouhua ^a   Dong, Yixuan ^a   Wu, Chuanbin ^a   Williams III, Robert O ^b  

^a SUN YAT SEN UNIVERSITY   (China)

^b UNIVERSITY OF TEXAS AT AUSTIN   (United States)

Author keywords

Amorphous solid dispersion; Dosage form development; Fenofibrate; Supersaturation dissolution; Thin film freezing

Indexed keywords

FENOFIBRATE; HYDROXYPROPYLMETHYLCELLULOSE ACETATE SUCCINATE; ORGANIC SOLVENT;

ABSORPTION; ANIMAL EXPERIMENT; AQUEOUS SOLUTION; ARTICLE; CRYSTALLIZATION; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG DELIVERY SYSTEM; DRUG FORMULATION; DRUG SOLUBILITY; DRUG STABILITY; FILM COATING; FREEZING; HYDROGEN BOND; IN VITRO STUDY; IN VIVO STUDY; INTESTINE ABSORPTION; MALE; MEAN RESIDENCE TIME; NONHUMAN; PHYSICAL CHEMISTRY; RAT; SINGLE DRUG DOSE;

ADMINISTRATION, ORAL; ANIMALS; BIOLOGICAL AVAILABILITY; CALORIMETRY, DIFFERENTIAL SCANNING; DRUG DELIVERY SYSTEMS; FENOFIBRATE; FREEZING; HYPOLIPIDEMIC AGENTS; MALE; MICROSCOPY, ELECTRON, SCANNING; POROSITY; RATS; RATS, WISTAR; SOLUBILITY; SPECTROSCOPY, FOURIER TRANSFORM INFRARED; X-RAY DIFFRACTION;

EID: 84870573102     PISSN: 09396411     EISSN: 18733441     Source Type: Journal    
DOI: 10.1016/j.ejpb.2012.06.016     Document Type: Article

References (55)

1. D.T. Friesen, R. Shanker, M. Crew, D.T. Smithey, W.J. Curatolo, and J.A.S. Nightingale Hydroxypropyl methylcellulose acetate succinate-based spray-dried dispersions: an overview Mol. Pharm. 5 2008 1003 1019
2. D.B. Warren, H. Benameur, C.J.H. Porter, and C.W. Pouton Using polymeric precipitation inhibitors to improve the absorption of poorly water-soluble drugs: a mechanistic basis for utility J. Drug Target. 18 2010 704 731
3. V.J. Stella, and K.W. Nti-Addae Prodrug strategies to overcome poor water solubility Adv. Drug Deliv. Rev. 59 2007 677 694
4. A.T.M. Serajuddin Salt formation to improve drug solubility Adv. Drug Deliv. Rev. 59 2007 603 616
5. H.G. Brittain Effects of mechanical processing on phase composition J. Pharm. Sci. 91 2002 1573 1580
6. N. Qiao, M.Z. Li, W. Schlindwein, N. Malek, A. Davies, and G. Trappitt Pharmaceutical cocrystals: an overview Int. J. Pharm. 419 2011 1 11
7. M.D. Moya-Ortega, M. Messner, P. Jansook, T.T. Nielsen, V. Wintgens, K.L. Larsen, C. Amiel, H.H. Sigurdsson, and T. Loftsson Drug loading in cyclodextrin polymers: dexamethasone model drug J. Inclus. Phenom. Macro. Chem. 69 2010 377 382
8. M.A. Rahman, R. Harwansh, M.A. Mirza, S. Hussain, and A. Hussain Oral lipid based drug delivery system (LBDDS): formulation, characterization and application: a review Curr. Drug Deliv. 8 2011 330 345
9. R.H. Muller, S. Gohla, and C.M. Keck State of the art of nanocrystals - special features, production, nanotoxicology aspects and intracellular delivery Eur. J. Pharm. Biopharm. 78 2011 1 9
10. J.K. Lee, M.H. Lee, and K.B. Kim Synthesis of bulk amorphous composites with three amorphous phases by consolidation of milled amorphous powders Intermetallics 18 2010 2019 2023
11. A. Singh, Z.A. Worku, and G. Van den Mooter Oral formulation strategies to improve solubility of poorly water-soluble drugs Exp. Opin. Drug Deliv. 8 2011 1361 1378
12. L. Peltonen, and J. Hirvonen Pharmaceutical nanocrystals by nanomilling: critical process parameters, particle fracturing and stabilization methods J. Pharm. Pharmacol. 62 2010 1569 1579
13. J.C. DiNunzio, C. Brough, J.R. Hughey, D.A. Miller, R.O. Williams Iii, and J.W. McGinity Fusion production of solid dispersions containing a heat-sensitive active ingredient by hot melt extrusion and Kinetisol® dispersing Eur. J. Pharm. Biopharm. 74 2010 340 351
14. J.P. Lalkshman, Y. Cao, J. Kowalski, and A.T.M. Serajuddin Application of melt extrusion in the development of a physically and chemically stable high-energy amorphous solid dispersion of a poorly water-soluble drug Mol. Pharm. 5 2008 994 1002
15. A. Alhalaweh, S. Andersson, and S.P. Velaga Preparation of zolmitriptan-chitosan microparticles by spray drying for nasal delivery Eur. J. Pharm. Sci. 38 2009 206 214
16. W. Yang, J. Tam, D.A. Miller, J. Zhou, J.T. McConville, K.P. Johnston, and R.O. Williams High bioavailability from nebulized itraconazole nanoparticle dispersions with biocompatible stabilizers Int. J. Pharm. 361 2008 177 188
17. A. Bouchard Supercritical fluid drying of carbohydrates: selection of suitable excipients and process conditions Eur. J. Pharm. Biopharm. 68 2008 781 794
18. K.A. Overhoff, J.D. Engstrom, B. Chen, B.D. Scherzer, T.E. Milner, K.P. Johnston, and R.O. Williams Novel ultra-rapid freezing particle engineering process for enhancement of dissolution rates of poorly water-soluble drugs Eur. J. Pharm. Biopharm. 65 2007 57 67
19. K.A. Overhoff, J.T. McConville, W. Yang, K.P. Johnston, J.I. Peters, and R.O. Williams Effect of stabilizer on the maximum degree and extent of supersaturation and oral absorption of tacrolimus made by ultra-rapid freezing Pharm. Res. 25 2008 167 175
20. K.A. Overhoff, K.P. Johnston, J. Tam, J. Engstrom, and R.O. Williams Use of thin film freezing to enable drug delivery: a review J. Drug Deliv. Sci. Technol. 19 2009 89 98
21. L. Yu Amorphous pharmaceutical solids: preparation, characterization and stabilization Adv. Drug Deliv. Rev. 48 2001 27 42
22. M. Vogt, K. Kunath, and J.B. Dressman Dissolution improvement of four poorly water soluble drugs by cogrinding with commonly used excipients Eur. J. Pharm. Biopharm. 68 2008 330 337
23. Y.P. Chen, Y. Lu, J.M. Chen, J. Lai, J. Sun, F.Q. Hu, and W. Wu Enhanced bioavailability of the poorly water-soluble drug fenofibrate by using liposomes containing a bile salt Int. J. Pharm. 376 2009 153 160
24. J.D. Wei, H.O. Ho, C.H. Chen, W.T. Ke, E.T.H. Chen, and M.T. Sheu Characterisation of fenofibrate dissolution delivered by a self-microemulsifying drug-delivery system J. Pharm. Pharmacol. 62 2010 1685 1696
25. X. Li, L. Gu, Y. Xu, and Y. Wang Preparation of fenofibrate nanosuspension and study of its pharmacokinetic behavior in rats Drug Dev. Ind. Pharm. 35 2009 827 833
26. Z. Jia, P. Lin, Y. Xiang, X. Wang, J. Wang, X. Zhang, and Q. Zhang A novel nanomatrix system consisted of colloidal silica and pH-sensitive polymethylacrylate improves the oral bioavailability of fenofibrate Eur. J. Pharm. Biopharm. 79 2011 126 134
27. K. Tziomalos, and V.G. Athyros Fenofibrate: a novel formulation (Triglide (TM)) in the treatment of lipid disorders: a review Int. J. Nanomed. 1 2006 129 147
28. F. Kesisoglou, S. Panmai, and Y. Wu Nanosizing - Oral formulation development and biopharmaceutical evaluation Adv. Drug Deliv. Rev. 59 2007 631 644
29. P. Srinarong, J.H. Faber, M.R. Visser, W.L.J. Hinrichs, and H.W. Frijlink Strongly enhanced dissolution rate of fenofibrate solid dispersion tablets by incorporation of superdisintegrants Eur. J. Pharm. Biopharm. 73 2009 154 161
30. S. Wang Ordered mesoporous materials for drug delivery Micropor. Mesopor. Mater. 117 2009 1 9
31. G.P. Sanganwar, and R.B. Gupta Dissolution-rate enhancement of fenofibrate by adsorption onto silica using supercritical carbon dioxide Int. J. Pharm. 360 2008 213 218
32. S. Lee, H.-S. Yun, and S.-H. Kim The comparative effects of mesoporous silica nanoparticles and colloidal silica on inflammation and apoptosis Biomaterials 32 2011 9434 9443
33. J.H. Hu, T.L. Rogers, J. Brown, T. Young, K.P. Johnston, and R.O. Williams Improvement of dissolution rates of poorly water soluble APIs using novel spray freezing into liquid technology Pharm. Res. 19 2002 1278 1284
34. J.C. DiNunzio, D.A. Miller, W. Yang, J.W. McGinity, and R.O. Williams Amorphous compositions using concentration enhancing polymers for improved bioavailability of itraconazole Mol. Pharm. 5 2008 968 980
35. A. Heinz, K. Gordon, C. McGoverin, T. Rades, and C. Strachan Understanding the solid-state forms of fenofibrate - a spectroscopic and computational study Eur. J. Pharm. Biopharm. 71 2009 100 108
36. H. de Waard, W.L.J. Hinrichs, and H.W. Frijlink A novel bottom-up process to produce drug nanocrystals: controlled crystallization during freeze-drying J. Control. Release 128 2008 179 183
37. H. Hardung, and D. Djuric Soluplus (R) a novel excipient for hot melt extrusion Chim. Oggi - Chem. Today 28 2010 XIV XV
38. R. Wang, C. Pellerin, and O. Lebel Role of hydrogen bonding in the formation of glasses by small molecules: a triazine case study J. Mater. Chem. 19 2009 2747 2753
39. Q.-P. Huang, J.-X. Wang, Z.-B. Zhang, Z.-G. Shen, J.-F. Chen, and J. Yun Preparation of ultrafine fenofibrate powder by solidification process from emulsion Int. J. Pharm. 368 2009 160 164
40. H. Konno, and L.S. Taylor Influence of different polymers on the crystallization tendency of molecularly dispersed amorphous felodipine J. Pharm. Sci. 95 2006 2692 2705
41. G. Van den Mooter, M. Wuyts, N. Blaton, R. Busson, P. Grobet, P. Augustijns, and R. Kinget Physical stabilisation of amorphous ketoconazole in solid dispersions with polyvinylpyrrolidone K25 Eur. J. Pharm. Sci. 12 2001 261 269
42. W. Curatolo, J.A. Nightingale, and S.M. Herbig Utility of hydroxypropylmethylcellulose acetate succinate (HPMCAS) for initiation and maintenance of drug supersaturation in the GI Milieu Pharm. Res. 26 2009 1419 1431
43. M.E. Brewster, R. Vandecruys, G. Verreck, and J. Peeters Supersaturating drug delivery systems: effect of hydrophilic cyclodextrins and other excipients on the formation and stabilization of supersaturated drug solutions Pharmazie 63 2008 217 220
44. C. Goddeeris, T. Willems, and G. Van den Mooter Formulation of fast disintegrating tablets of ternary solid dispersions consisting of TPGS 1000 and HPMC 2910 or PVPVA 64 to improve the dissolution of the anti-HIV drug UC 781 Eur. J. Pharm. Sci. 34 2008 293 302
45. S. Ozaki, T. Minamisono, T. Yamashita, T. Kato, and I. Kushida Supersaturation-nucleation behavior of poorly soluble drugs and its impact on the oral absorption of drugs in thermodynamically high-energy forms J. Pharm. Sci. 101 2012 214 222
46. A. Newman, G. Knipp, and G. Zografi Assessing the performance of amorphous solid dispersions J. Pharm. Sci. 101 2012 1355 1377
47. D.A. Miller, J.C. DiNunzio, W. Yang, J.W. McGinity, and R.O. Williams Enhanced in vivo absorption of itraconazole via stabilization of supersaturation following acidic-to-neutral pH transition Drug Dev. Ind. Pharm. 34 2008 890 902
48. A. Riedel, and C.S. Leopold Degradation of omeprazole induced by enteric polymer solutions and aqueous dispersions: HPLC investigations Drug Dev. Ind. Pharm. 31 2005 151 160
49. H. Al-Obaidi, and G. Buckton Evaluation of griseofulvin binary and ternary solid dispersions with HPMCAS AAPS PharmSciTech 10 2009 1172 1177
50. D.E. Alonzo, Y. Gao, D. Zhou, H. Mo, G.G.Z. Zhang, and L.S. Taylor Dissolution and precipitation behavior of amorphous solid dispersions J. Pharm. Sci. 100 2011 3316 3331
51. D.J. van Drooge, W.L.J. Hinrichs, and H.W. Frijlink Anomalous dissolution behaviour of tablets prepared from sugar glass-based solid dispersions J. Control. Release 97 2004 441 452
52. M.M. Al-Tabakha HPMC capsules: current status and future prospects J. Pharm. Pharm. Sci. 13 2010 428 442
53. P.J. Marsac, A.C.F. Rumondor, D.E. Nivens, U.S. Kestur, L. Stanciu, and L.S. Taylor Effect of temperature and moisture on the miscibility of amorphous dispersions of felodipine and poly(vinyl pyrrolidone) J. Pharm. Sci. 99 2010 169 185
54. T. Zhu, J.C. Ansquer, M.T. Kelly, D.J. Sleep, and R.S. Pradhan Comparison of the gastrointestinal absorption and bioavailability of fenofibrate and fenofibric acid in humans J. Clin. Pharmacol. 50 2010 914 921
55. M. Van Speybroeck, R. Mellaerts, R. Mols, T. Do Thi, J.A. Martens, J. Van Humbeeck, P. Annaert, G. Van den Mooter, and P. Augustijns Enhanced absorption of the poorly soluble drug fenofibrate by tuning its release rate from ordered mesoporous silica Eur. J. Pharm. Sci. 41 2010 623 630