Spray granulation: Importance of process parameters on in vitro and in vivo behavior of dried nanosuspensions

European Journal of Pharmaceutics and Biopharmaceutics

Volumn 85, Issue 3 PART B, 2013, Pages 1046-1055

  Figueroa, Carlos E ^a   Bose, Sonali ^b  

^a Princeton University   (United States)

^b NOVARTIS PHARMA AG   (Switzerland)

Author keywords

Atomizing pressure; Fluid bed granulation; Naproxen; Spray mode; Spray rate; Wet media milling

Indexed keywords

MANNITOL; NANOCRYSTAL; NANOPARTICLE; NANOSUSPENSION; NAPROXEN; UNCLASSIFIED DRUG;

AEROSOL; ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; ATMOSPHERIC PRESSURE; DISPERSION; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG FORMULATION; DRUG GRANULATION; DRUG GRANULE; DRUG PENETRATION; DRUG RELEASE; DRUG SOLUBILITY; DRUG STABILITY; DRY POWDER; EXPERIMENTAL DOG; IN VITRO STUDY; IN VIVO STUDY; MALE; MATERIALS HANDLING; MAXIMUM PLASMA CONCENTRATION; NEBULIZATION; NONHUMAN; PARTICLE SIZE; PROCESSING; SPRAY DRYING; SUSPENSION; TIME TO MAXIMUM PLASMA CONCENTRATION;

ANALYSIS OF VARIANCE; ANOVA; ATOMIZING PRESSURE; CMC; CRITICAL MICELLE CONCENTRATION; DESIGN OF EXPERIMENT; DOE; FASSGF; FASTED STATE SIMULATED GASTRIC FLUID; FF(C); FLOW RATE INDEX; FLUID BED GRANULATION; FRI; HPC-EXF; HYDROXYPROPYLCELLULOSE-EXF GRADE; JENIKE FLOW FUNCTION; LOD; LOSS ON DRYING; NAPROXEN; PDI; POLYDISPERSITY INDEX; SLS; SODIUM LAURYL SULFATE; SPRAY MODE; SPRAY RATE; WET MEDIA MILLING; X-RAY DIFFRACTION; XRD;

ANIMALS; AREA UNDER CURVE; CHEMISTRY, PHARMACEUTICAL; DESICCATION; DOGS; DRUG STABILITY; MALE; MANNITOL; MICROSCOPY, ELECTRON, SCANNING; NANOPARTICLES; NANOTECHNOLOGY; NAPROXEN; PARTICLE SIZE; POWDERS; SOLUBILITY; SURFACE PROPERTIES; TECHNOLOGY, PHARMACEUTICAL; X-RAY DIFFRACTION;

EID: 84889099394     PISSN: 09396411     EISSN: 18733441     Source Type: Journal    
DOI: 10.1016/j.ejpb.2013.07.015     Document Type: Article

References (54)

1. C. Lipinski Poor aqueous solubility - an industry wide problem in drug discovery Am. Pharm. Rev. 5 2002 82 85
2. G.L. Amidon, H. Lennernas, V.P. Shah, and J.R. Crison A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability Pharm. Res. 12 1995 413 420
3. J.M. Butler, and J.B. Dressman The developability classification system: application of biopharmaceutics concepts to formulation development J. Pharm. Sci. 99 2010 4940 4954
4. A.A. Noyes, and W.R. Whitney The rate of solution of solid substances in their own solutions J. Am. Chem. Soc. 19 1897 930 934
5. 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
6. L. Peltonen, and J. Hirvonen Pharmaceutical nanocrystals by nanomilling: critical process parameters, particle fracturing and stabilization methods J. Pharm. Pharmacol. 62 2010 1569 1579
7. B. Van Eerdenbrugh, J. Vermant, J.A. Martens, L. Froyen, H.J. Van, P. Augustijns, and G. Van den Mooter A screening study of surface stabilization during the production of drug nanocrystals J. Pharm. Sci. 98 2009 2091 2103
8. B. Van Eerdenbrugh, L. Froyen, H.J. Van, J.A. Martens, P. Augustijns, and G. Van den Mooter Drying of crystalline drug nanosuspensions - the importance of surface hydrophobicity on dissolution behavior upon redispersion Eur. J. Pharm. Sci. 35 2008 127 135
9. B. Van Eerdenbrugh, G. Van den Mooter, and P. Augustijns Top-down production of drug nanocrystals: nanosuspension stabilization, miniaturization and transformation into solid products Int. J. Pharm. 364 2008 64 75
10. P. Sharma, W.A. Denny, and S. Garg Effect of wet milling process on the solid state of indomethacin and simvastatin Int. J. Pharm. 380 2009 40 48
11. P. Kayaert, and G. Van den Mooter Is the amorphous fraction of a dried nanosuspension caused by milling or by drying? A case study with Naproxen and Cinnarizine Eur. J. of Pharm. Biopharm. 81 2012 650 656
12. J. Beirowski, S. Inghelbrecht, A. Arien, and H. Gieseler Freeze-drying of nanosuspensions, 1: freezing rate versus formulation design as critical factors to preserve the original particle size distribution J. Pharm. Sci. 100 2011 1958 1968
13. B. Van Eerdenbrugh, L. Froyen, J.A. Martens, N. Blaton, P. Augustijns, M. Brewster, and G. Van den Mooter Characterization of physico-chemical properties and pharmaceutical performance of sucrose co-freeze-dried solid nanoparticulate powders of the anti-HIV agent loviride prepared by media milling Int. J. Pharm. 338 2007 198 206
14. M.V. Chaubal, and C. Popescu Conversion of nanosuspensions into dry powders by spray drying: a case study Pharm. Res. 25 2008 2302 2308
15. D. Mou, H. Chen, J. Wan, H. Xu, and X. Yang Potent dried drug nanosuspensions for oral bioavailability enhancement of poorly soluble drugs with pH-dependent solubility Int. J. Pharm. 413 2011 237 244
16. V. Nekkanti, R. Pillai, V. Venkateshwarlu, and T. Harisudhan Development and characterization of solid oral dosage form incorporating candesartan nanoparticles Pharm. Dev. Technol. 14 2009 290 298
17. S. Basa, T. Muniyappan, P. Karatgi, R. Prabhu, and R. Pillai Production and in vitro characterization of solid dosage form incorporating drug nanoparticles Drug Dev. Ind. Pharm. 34 2008 1209 1218
18. P. Kayaert, M. Anne, and G. Van den Mooter Bead layering as a process to stabilize nanosuspensions: influence of drug hydrophobicity on nanocrystal reagglomeration following in-vitro release from sugar beads J. Pharm. Pharmacol. 63 2011 1446 1453
19. S. Bose, D. Schenck, I. Ghosh, A. Hollywood, E. Maulit, and C. Ruegger Application of spray granulation for conversion of a nanosuspension into a dry powder form Eur. J. Pharm. Sci. 47 2012 35 43
20. A. Monteiro, A. Afolabi, and E. Bilgili Continuous production of drug nanoparticle suspensions via wet stirred media milling: a fresh look at the Rehbinder effect Drug Dev. Ind. Pharm. 2012 1 18
21. L. Sievens-Figueroa, A. Bhakay, J.I. Jerez-Rozo, N. Pandya, R.J. Romanach, B. Michniak-Kohn, Z. Iqbal, E. Bilgili, and R.N. Dave Preparation and characterization of hydroxypropyl methyl cellulose films containing stable BCS Class II drug nanoparticles for pharmaceutical applications Int. J. Pharm. 423 2012 496 508
22. C.P. Mora, and F. Martinez Thermodynamic quantities relative to solution processes of Naproxen in aqueous media at pH 1.2 and 7.4 Phys. Chem. Liq. 44 2006 585 596
23. S.M. Iveson, P.A.L. Wauters, S. Forrest, J.D. Litster, G.M.H. Meesters, and B. Scarlett Growth regime map for liquid-bound granules: further development and experimental validation Powder Technol. 117 2001 83 97
24. F.N. Christensen, and P. Bertelsen Qualitative description of the Wurster-based fluid-bed coating process Drug Dev. Ind. Pharm. 23 1997 451 463
25. R. Freeman Measuring the flow properties of consolidated, conditioned and aerated powders - a comparative study using a powder rheometer and a rotational shear cell Powder Technol. 174 2007 25 33
26. J. Tomas Fundamentals of cohesive powder consolidation and flow Granular Matter 6 2004 75 86
27. M. Efentakis, and J.B. Dressman Gastric juice as a dissolution medium: surface tension and pH Eur. J. Drug Metab. Pharmacokinet. 23 1998 97 102
28. J.B. Dressman, G.L. Amidon, C. Reppas, and V.P. Shah Dissolution testing as a prognostic tool for oral drug absorption: immediate release dosage forms Pharm. Res. 15 1998 11 22
29. A. Aburub, D.S. Risley, and D. Mishra A critical evaluation of fasted state simulating gastric fluid (FaSSGF) that contains sodium lauryl sulfate and proposal of a modified recipe Int. J. Pharm. 347 2008 16 22
30. A. Bhakay, R. Dave, and E. Bilgili Recovery of BCS Class II drugs during aqueous redispersion of core-shell type nanocomposite particles produced via fluidized bed coating Powder Technol. 2012
31. D. Junemann, and J. Dressman Analytical methods for dissolution testing of nanosized drugs J. Pharm. Pharmacol. 64 2012 931 943
32. D. Juenemann, E. Jantratid, C. Wagner, C. Reppas, M. Vertzoni, and J.B. Dressman Biorelevant in vitro dissolution testing of products containing micronized or nanosized fenofibrate with a view to predicting plasma profiles Eur. J. Pharm. Biopharm. 77 2011 257 264
33. J.J. Guo, P.F. Yue, J.L. Lv, J. Han, S.S. Fu, S.X. Jin, S.Y. Jin, and H.L. Yuan Development and in vivo/in vitro evaluation of novel herpetrione nanosuspension Int. J. Pharm. 441 2013 227 233
34. Q. Ma, H. Sun, E. Che, X. Zheng, T. Jiang, C. Sun, and S. Wang Uniform nano-sized valsartan for dissolution and bioavailability enhancement: influence of particle size and crystalline state Int. J. Pharm. 441 2013 75 81
35. M.K. Gupta, Y.C. Tseng, D. Goldman, and R.H. Bogner Hydrogen bonding with adsorbent during storage governs drug dissolution from solid-dispersion granules Pharm. Res. 19 2002 1663 1672
36. D.B. Shenoy, and G.B. Sukhorukov Engineered microcrystals for direct surface modification with layer-by-layer technique for optimized dissolution Eur. J. Pharm. Biopharm. 58 2004 521 527
37. C. Kindermann, K. Matthee, J. Strohmeyer, F. Sievert, and J. Breitkreutz Tailor-made release triggering from hot-melt extruded complexes of basic polyelectrolyte and poorly water-soluble drugs Eur. J. Pharm. Biopharm. 79 2011 372 381
38. F.J. Otero-Espinar, S. Anguiano-Igea, N. Garcia-Gonzalez, J.L. Vila-Jato, and J. Blanco-Mendez Interaction of naproxen with β-cyclodextrin in solution and in the solid state Int. J. Pharm. 79 1992 149 157
39. D.M. Jones Factors to consider in fluid bed processing Pharm. Technol. 9 1985 50 62
40. S. Flogel, and H. Egermann Fluid bed granulation of lactose using bottom spray method Eur. J. Pharm. Sci. 4 Supplement 1 1996 S185
41. Z.H. Loh, D.Z. Er, L.W. Chan, C.V. Liew, and P.W. Heng Spray granulation for drug formulation Expert Opin. Drug Deliv. 8 2011 1645 1661
42. K. Dewettinck, L. Deroo, W. Messens, and A. Huyghebaert Agglomeration tendency during top-spray fluidized bed coating with gums LWT - Food Sci. Technol. 31 1998 576 584
43. M. Hemati, R. Cherif, K. Saleh, and V. Pont Fluidized bed coating and granulation: influence of process-related variables and physicochemical properties on the growth kinetics Powder Technol. 130 2003 18 34
44. X. Hu, J.C. Cunningham, and D. Winstead Study growth kinetics in fluidized bed granulation with at-line FBRM Int. J. Pharm. 347 2008 54 61
45. K. Dewettinck, W. Messens, L. Deroo, and A. Huyghebaert Agglomeration tendency during top-spray fluidized bed coating with gelatin and starch hydrolysate LWT - Food Sci. Technol. 32 1999 102 106
46. M. Tzika, S. Alexandridou, and C. Kiparissides Evaluation of the morphological and release characteristics of coated fertilizer granules produced in a Wurster fluidized bed Powder Technol. 132 2003 16 24
47. J.Z. Gao, A. Jain, R. Motheram, D.B. Gray, and M.A. Hussain Fluid bed granulation of a poorly water soluble, low density, micronized drug: comparison with high shear granulation Int. J. Pharm. 237 2002 1 14
48. X. Wang, F. Cui, Y. Yonezawa, and H. Sunada Preparation and evaluation of high drug content particles Drug Dev. Ind. Pharm. 29 2003 1109 1118
49. E. Teunou, and D. Poncelet Batch and continuous fluid bed coating - review and state of the art J. Food Eng. 53 2002 325 340
50. P. Bertelsen, F.N. Christensen, P. Holm, and K. Jorgensen Comparison of organic solvent-based ethylcellulose coatings of KCl crystals applied by top and bottom spraying in fluidized-bed equipment Int. J. Pharm. 111 1994 117 125
51. A.M. Mehta, and D.M. Jones Coated pellets under the microscope Pharm. Technol. 9 1985 52 60
52. K. Dewettinck, and A. Huyghebaert Fluidized bed coating in food technology Trends Food Sci. Technol. 10 1999 163 168
53. H.H. Frey, and B. Rieh Pharmacokinetics of naproxen in the dog Am. J. Vet. Res. 42 1981 1615 1617
54. E. Samara, D. Avnir, D. Ladkani, and M. Bialer Pharmacokinetic analysis of diethylcarbonate prodrugs of ibuprofen and naproxen Biopharm. Drug Dispos. 16 1995 201 210