An investigation into the effect of formulation variables and process parameters on characteristics of granules obtained by in situ fluidized hot melt granulation

International Journal of Pharmaceutics

Volumn 423, Issue 2, 2012, Pages 202-212

  Mašić, Ivana ^a   Ilić, Ilija ^b   Dreu, Rok ^b   Ibrić, Svetlana ^a   Parojčić, Jelena ^a   Durić, Zorica ^a  

^a UNIVERSITY OF BELGRADE   (Serbia)

^b UNIVERSITY OF LJUBLJANA   (Slovenia)

Author keywords

Binder particle size; Fluid bed; Granule shape; In situ melt granulation; Melt agglomeration

Indexed keywords

EXCIPIENT; GLYCEROL PALMITOSTEARATE; MACROGOL 2000; PARACETAMOL;

AIRFLOW; ARTICLE; DIFFERENTIAL SCANNING CALORIMETRY; DRUG FORMULATION; DRUG GRANULATION; DRUG RELEASE; DRUG SOLUBILITY; FLOW RATE; IN SITU FLUIDIZED HOT MELT GRANULATION; INFRARED SPECTROSCOPY; MORPHOLOGY; PARTICLE SIZE; PRIORITY JOURNAL; TABLET; TABLET COMPRESSION; VISCOSITY; X RAY POWDER DIFFRACTION;

ACETAMINOPHEN; ADMINISTRATION, ORAL; ADULT; CHEMISTRY, PHARMACEUTICAL; DIGLYCERIDES; DRUG COMPOUNDING; EXCIPIENTS; FEMALE; HOT TEMPERATURE; HUMANS; KINETICS; MALE; PARTICLE SIZE; PHASE TRANSITION; POLYETHYLENE GLYCOLS; POWDERS; RHEOLOGY; SOLUBILITY; SURFACE PROPERTIES; TASTE; TECHNOLOGY, PHARMACEUTICAL; VISCOSITY;

EID: 84856547104     PISSN: 03785173     EISSN: 18733476     Source Type: Journal    
DOI: 10.1016/j.ijpharm.2011.12.013     Document Type: Article

References (45)

1. T. Abberger Influence of binder properties, method of addition, powder type and operating conditions on fluid-bed melt granulation and resulting tablet properties Pharmazie 56 2001 949 952 (Pubitemid 34016825)
2. T. Abberger, A. Seo, and T. Schaefer The effect of droplet size and powder particle size on the mechanisms of nucleation and growth in fluid bed melt agglomeration Int. J. Pharm. 249 2002 185 197 (Pubitemid 35333445)
3. AnalySIS User's Guide Soft Imaging System GmbH 1998 Germany
4. G.P. Andrews Advances in solid dosage form manufacturing technology Philos. Trans. R. Soc. Lond. A 365 2007 2935 2949
5. M.A. Ansari, and F. Stepanek Formation of hollow core granules by fluid bed in situ melt granulation: modelling and experiments Int. J. Pharm. 32 2006 108 116 (Pubitemid 44247418)
6. G.B. Borini, T.C. Andrade, and L.A.P. Freitas Hot melt granulation of coarse pharmaceutical powders in a spouted bed Powder Technol. 189 2009 520 527
7. A.M. Bouwman, J.C. Bosma, P. Vonk, J.A. Wesselingh, and H.W. Frijlink Which shape factor(s) best describe granules? Powder Technol. 146 2004 66 72 (Pubitemid 39314572)
8. F. Damian, N. Blaton, L. Naesens, J. Balzarini, R. Kinget, P. Augustijns, and G. Van Der Mooter Physicochemical characterisation of solid dispersions of the antiviral agent UC-781 with polyethylene glycol 6000 and Gelucire 44/14 Eur. J. Pharm. Sci. 10 2000 311 322 (Pubitemid 30317467)
9. B. Evrard, K. Amighi, D. Beten, L. Delattre, and A.J. Moës Influence of melting and rheological properties of fatty binders on the melt granulation process in a high-shear mixer Drug Dev. Ind. Pharm. 25 1999 1177 1184
10. B. Evrard, and L. Delattre In vitro evaluation of lipid matries for the development of a sustained-release sulfamethazine bolus for lambs Drug Dev. Ind. Pharm. 22 1996 111 118 (Pubitemid 26075515)
11. J. Hamdani, A.J. Moës, and K. Amighi Physical and thermal characterisation of Precirol® and Compritol® as lipophilic glycerides used for the preparation of controlled-release matrix pellets Int. J. Pharm. 260 2003 47 57 (Pubitemid 36724860)
12. J. Hamdani, A.J. Moës, and K. Amighi Development and evaluation of prolonged release pellets obtained by the melt pelletization process Int. J. Pharm. 245 2002 167 177 (Pubitemid 35299902)
13. P.W.S. Heng, and T.W. Wong Melt process for oral solid dosage forms J. Swabrick, Encyclopedia of Pharmaceutical Technology 3rd ed. 2006 Informa Healthcare New York 2257 2261
14. I. Ilić, P. Kása jr., R. Dreu, K. Pintye-Hódi, and S. Srčič The compressibility and compactibility of different types of lactose Drug Dev. Ind. Pharm. 35 2009 1271 1280
15. M. Kidokoro, Y. Haramiishi, S. Sagasaki, and Y. Yamamoto Application of fluidised hot-melt granulation (FHMG) for the preparation of granules for tableting Drug Dev. Ind. Pharm. 28 2002 67 76
16. J.H. Kirk, S.E. Dann, and C.G. Blatchford Lactose: a definitive guide to polymorph determination Int. J. Pharm. 334 2007 103 114 (Pubitemid 46402962)
17. M. Kojima, and H. Nakagami Preparation of the controlled release matrix tablets of theophylline with micronized low-substituted hydroxypropyl cellulose by a fluidised hot-melt granulation method S. T. P. Pharma Sci. 11 2001 145 150 (Pubitemid 32274921)
18. H.S. Mansur, R.L. Oréfice, and A.A.P. Mansur Characterization of poly(vinyl alcohol)/poly(ethylene glycol) hydrogels and pva-derived hybrids by small-angle X-ray scattering and FTIR spectroscopy Polymer 45 2004 7193 7202 (Pubitemid 39286074)
19. N. Passerini, B. Albertini, M.L. Gonzalez-Rodriguez, C. Cavallari, and L. Rodiguez Preparation and characterization of ibuprofen-poloxamer 188 granules obtained by melt granulation Eur. J. Pharm. Sci. 15 2002 71 78 (Pubitemid 34136970)
20. N. Passerini, B. Albertini, B. Perissutti, and L. Rodriguez Evaluation of melt granulation and ultrasonic spray congealing as techniques to enhance the dissolution of praziquantel Int. J. Pharm. 318 2006 92 102 (Pubitemid 43963306)
21. N. Passerini, G. Calogerà, B. Albertini, and L. Rodriguez Melt granulation of pharmaceutical powders: a comparison of high-shear mixer and fluidised bed processes Int. J. Pharm. 391 2010 177 186
22. A. Pauli-Bruns, K. Knop, and B.C. Lippold Preparation of sustained release matrix pellets by melt agglomeration in the fluidized bed: influence of formulation variables and modeling of agglomerate growth Eur. J. Pharm. Biopharm. 74 2010 503 512
23. B. Perissutti, F. Rubessa, M. Moneghini, and D. Voinovich Formulation design of carbamazepine fast release tablets prepared by melt granulation technique Int. J. Pharm. 256 2003 53 63 (Pubitemid 36412139)
24. F. Podczeck, S.R. Rahman, and J.M. Newton Evaluation of a standardised procedure to assess the shape of pellets using image analysis Int. J. Pharm. 192 1999 123 138 (Pubitemid 29531547)
25. S. Qi, P. Avalle, R. Saklatvala, and D.Q.M. Craig An investigation into the effects of thermal history on the crystallization behaviour of amorphous paracetamol Eur. J. Pharm. Biopharm. 69 2008 364 371 (Pubitemid 351471777)
26. M.H. Rubinstein, and P. Musikabhuma Formulation and evaluation of paracetamol 500 mg tablets produced by a new direct granulation method Drug Dev. Ind. Pharm. 6 1980 451 473 (Pubitemid 11177096)
27. T. Schæfer, P. Holm, and H.G. Kristensen Melt granulation in a laboratory scale high shear mixer Drug Dev. Ind. Pharm. 16 1990 1249 1277 (Pubitemid 20170821)
28. T. Schæfer, and C. Mathiesen Melt pelletization in a high shear mixer. IX. Effects of binder particle size Int. J. Pharm. 139 1996 139 148 (Pubitemid 26276276)
29. T. Schæfer, B. Taagegaard, L.J. Thomsen, and H.G. Kristensen Melt pelletization in a high shear mixer. IV. Effects of process variables in a laboratory scale mixer Eur. J. Pharm. Sci. 1 1993 125 131 (Pubitemid 24055797)
30. T. Schæfer, B. Taagegaard, L.J. Thomsen, and H.G. Kristensen Melt pelletization in a high shear mixer. V. Effects of apparatus variables Eur. J. Pharm. Sci. 1 1993 133 141 (Pubitemid 24055798)
31. A. Seo, P. Holm, and T. Schaefer Effects of droplet size and type of binder on the agglomerate growth mechanisms by melt agglomeration in a fluidised bed Eur. J. Pharm. Sci. 16 2002 95 105 (Pubitemid 34786444)
32. R. Thies, and P. Kleinebudde Melt pelletisation of a hygroscopic drug in high shear mixer. Part 1. Influence of process variables Int. J. Pharm. 188 1999 131 143 (Pubitemid 29486716)
33. T. Vilhelmsen, H. Eliasen, and T. Schæfer Effect of a melt agglomeration process on agglomerates containing solid dispersions Int. J. Pharm. 303 2005 132 142 (Pubitemid 41318030)
34. T. Vilhelmsen, J. Kristensen, and T. Schæfer Melt pelletization with polyethylene glycol in a rotary processor Int. J. Pharm. 275 2004 141 153 (Pubitemid 38481527)
35. D. Voinovich, M. Moneghini, B. Perissutti, J. Filipovic-Grcic, and I. Grabnar Preparation in high-shear mixer of sustained-release pellets by melt pelletisation Int. J. Pharm. 203 2000 235 244 (Pubitemid 30627643)
36. G.M. Walker, C.R. Holland, M.M.N. Ahmad, and D.Q.M. Craig Influence of process parameters on fluidised hot-melt granulation and tablet pressing of pharmaceutical powders Chem. Eng. Sci. 60 2005 3867 3877 (Pubitemid 40665416)
37. G.M. Walker, G. Andrews, and D.S. Jones Effect of process parameters on the melt granulation of pharmaceutical powders Powder Technol. 165 2006 161 166 (Pubitemid 43928028)
38. G.M. Walker, S.E.J. Bell, G. Andrews, and D.S. Jones Co-melt fluidised bed granulation of pharmaceutical powders: improvements in drug bioavailability Chem. Eng. Sci. 62 2007 451 462 (Pubitemid 44750899)
39. G.M. Walker, S.E.J. Bell, M. Vann, H. Zhai, D.S. Jones, and G.P. Andrews Pharmaceutically engineering powders using FHMG: the effects of process parameters and formulation variables Chem. Eng. Res. Des. 85 2007 981 986 (Pubitemid 47241492)
40. G.M. Walker, S.E.J. Bell, M. Vann, D.S. Jones, and G.P. Andrews Fluidised bed characterisation using Raman spectroscopy: applications to pharmaceutical processing Chem. Eng. Sci. 62 2007 3832 3838 (Pubitemid 46891458)
41. G.M. Walker, S.E.J. Bell, K. Greene, D.S. Jones, and G.P. Andrews Characterisation of fluidised bed granulation processes using in situ Raman spectroscopy Chem. Eng. Sci. 64 2009 91 98
42. T.W. Wong, W.S. Cheong, and W.S. Heng Melt granulation and pelletization D.M. Parikh, Handbook of Pharmaceutical Granulation Technology 2005 Synthon Pharmaceutical Inc. North Carolina 385 406
43. D. Yang, R. Kulkarni, R.J. Behme, and P.N. Kotiyan Effect of the melt granulation technique on the dissolution characteristics of griseofulvin Int. J. Pharm. 329 2007 72 80 (Pubitemid 44940845)
44. H. Zhai, S. Li, G.P. Andrews, D.S. Jones, S.E.J. Bell, and G.M. Walker Nucleation and growth in fluidised hot melt granulation Powder Technol. 189 2009 230 237
45. F. Zhou, C. Vervaet, and J.P. Remon Matrix pellets based on the combination of waxes, starches and maltodextrins Int. J. Pharm. 133 1996 155 160 (Pubitemid 26163331)