29. Zheng X, Yang R, Tang X and Zheng L. Part I: Characterization <strong>of</strong> Solid Dispersions <strong>of</strong>Nimodipine Prepared by Hot-<strong>melt</strong> Extrusion. Drug Deve Ind Pharm 2007; 33:791–802.30. Jana S, Miloslava R. Hot-<strong>melt</strong> <strong>extrusion</strong>, Cesk Slov Farm 2012; 61(3): 87-92.31. Cilurzo F, Cupone I, Minghetti P, Selmin F, Montanari L. F<strong>as</strong>t dissolving films made <strong>of</strong>maltodextrins, Eur J Pharm Biopharm 2008; 70: 895-900.32. De Brabander C, Vervaet C, Fiermans L, Remon JP. Matrix mini-tablets b<strong>as</strong>ed onstarch/microcrystalline wax mixtures. Int J Pharm 2000; 199: 195-203.33. De Brabander C, Vervaet C, Remon JP. <strong>Development</strong> and evaluation <strong>of</strong> sustained rele<strong>as</strong>emini-matrices prepared via <strong>hot</strong> <strong>melt</strong> <strong>extrusion</strong>. J Cont Rel 2003; 89: 235–247.34. Zhang F, McGinity JW. Properties <strong>of</strong> sustained-rele<strong>as</strong>e tablets prepared by <strong>hot</strong>-<strong>melt</strong><strong>extrusion</strong>. Pharm Dev Tech 1999; 4(2): 241–250.35. Crowley MM, Zhang F, Koleng JJ, McGinity JW. Stability <strong>of</strong> polyethylene oxide inmatrix tablets prepared by <strong>hot</strong>-<strong>melt</strong> <strong>extrusion</strong>. Biomater 2002; 23: 4241-4248.36. Roblegg E, Jäger E, Hodzic A, Koscher G, Mohr S, Zimmer A, Khin<strong>as</strong>t J. <strong>Development</strong><strong>of</strong> sustained-rele<strong>as</strong>e lipophilic calcium stearate pellets via <strong>hot</strong> <strong>melt</strong> <strong>extrusion</strong>. Eur J PharmBiopharm 2011; 79: 635–645.37. Clark MR, Johnson TJ, McCabe RT, Clark JT, Tuitupou A, Elgendy H, Friend DR, KiserPF. A <strong>hot</strong>-<strong>melt</strong> extruded intravaginal ring <strong>for</strong> <strong>the</strong> sustained delivery <strong>of</strong> <strong>the</strong> antiretroviralmicrobicide UC781.J Pharm Sci 2012; 101(2):576-87.38. Li L, AbuBaker O, Shao Z, (2006). Characterization <strong>of</strong> poly (ethylene oxide) <strong>as</strong> a drugcarrier in <strong>hot</strong>-<strong>melt</strong> <strong>extrusion</strong>. Drug Dev Ind Pharm 2006; 32: 991–1002.39. Rambali B, Verreck G, Baert L, M<strong>as</strong>sart DL. Itraconazole <strong>for</strong>mulation studies <strong>of</strong> <strong>the</strong> <strong>melt</strong><strong>extrusion</strong>process with mixture design. Drug Dev Pharm 2003; 29(6): 641–652.40. Six K, Berghmans H, Leuner C, Dressman J, Van Werde K, Mullens J, Benoist L,Thimon M, Meublat L, Verreck G, Peeters J, Brewster M, Van den Mooter G.Characterization <strong>of</strong> solid dispersions <strong>of</strong> itraconazole and hydroxypropylmethylcelluloseprepared by <strong>melt</strong> <strong>extrusion</strong>, Part II. Pharm Res 2003; 20(7): 1047–1054.41. Six K, Daems T, de Hoon J, Van Hecken A, Depre M, Bouche MP, Prinsen P, Verreck G,Peeters J, Brewster ME, Van den Mooter G. Clinical study <strong>of</strong> solid dispersions <strong>of</strong>itraconazole prepared by <strong>hot</strong>-stage <strong>extrusion</strong>. Eur J Pharm Sci 2005; 24(2–3): 179–186.42. Gryckze A, Schminke GS, Maniruzzaman M, Beck J, Douroumis D. <strong>Development</strong> andevaluation <strong>of</strong> orally disintegrating tablets (ODTs) containing ibupr<strong>of</strong>en granules preparedby <strong>hot</strong> <strong>melt</strong> <strong>extrusion</strong>. Colloids Surf B Bio 2011; 86: 275-84.15 | P a g e
43. Chokshi RJ, Shah NHS, Sandhu KH, Malick AW, Zia H. Stabilization <strong>of</strong> Low Gl<strong>as</strong>sTransition Temperature Indomethacin Formulations: Impact <strong>of</strong> Polymer-Type and ItsConcentration. J Pharm Sci 2008; 97(6):2286-98.44. Andrews GP, Jones DS, Abu Diak O, McCoy CP, Watts AB, McGinity JW. Themanufacture and characterization <strong>of</strong> <strong>hot</strong> <strong>melt</strong> extruded enteric tablets. Eur J PharmBiopharm 2008; 69(1):264-73.45. Mehuys E, Remon JP, Vervaet C. Production <strong>of</strong> enteric capsules by means <strong>of</strong> <strong>hot</strong>-<strong>melt</strong><strong>extrusion</strong>. Eur J Pharm Sci 2005; 24: 207-212.46. Miller DA, J<strong>as</strong>on TM, Yang W, Robert OW, McGinity JW. Hot-Melt Extrusion <strong>for</strong>Enhanced Delivery <strong>of</strong> Drug Particles. J Pharm Sci 2007; 96(2): 361-376.47. Verreck G, Decorte A, Heymans K, Adriaensen J, Liu D, Tom<strong>as</strong>ko D, Arien A, Peeters J,Van den Mooter G, Brewster ME. Hot stage <strong>extrusion</strong> <strong>of</strong> p-amino salicylic acid with ECusing CO2 <strong>as</strong> a temporary pl<strong>as</strong>ticizer. Int J Pharm 2006; 327: 45-50.48. Breitkreutz J, El-Saleh F, Kiera C, Kleinebudde P, Wiedey W. Pediatric drug<strong>for</strong>mulations <strong>of</strong> sodium benzoate: II. Coated granules with a lipophilic binder. Eur JPharm Biopham 2003; 56: 255-60.49. Douroumis D. Practical approaches <strong>of</strong> t<strong>as</strong>te m<strong>as</strong>king technologies in oral solid <strong>for</strong>ms. ExpOpin Drug Deliv 2007; 4: 417–426.50. Douroumis D. Orally disintegrating dosage <strong>for</strong>ms and t<strong>as</strong>te-m<strong>as</strong>king technologies. ExpOpin Drug Deliv 2010; 8: 665-75.51. Witzleb R, Kanikanti VR, Hamann HJ, Kleinebudde P. Solid lipid <strong>extrusion</strong> with smalldie diameters--electrostatic charging, t<strong>as</strong>te m<strong>as</strong>king and continuous production. Eur JPharm Biopharm 2011; 77: 170-7.52. Va<strong>as</strong>sena J, Bartscherb K, Breitkreutza J. T<strong>as</strong>te m<strong>as</strong>ked lipid pellets with enhancedrele<strong>as</strong>e <strong>of</strong> hydrophobic active Ingredient. Int J Pharm 2012, 429:99– 103.53. Gutierrez-Rocca JC, McGinity JW. Influence <strong>of</strong> aging on <strong>the</strong> physical-mechanicalproperties <strong>of</strong> acrylic resin films c<strong>as</strong>t from aqueous dispersions and organic solutions. DrugDev Ind Pharm 1993; 19:315–332.54. Steuernagel CR. Latex emulsions <strong>for</strong> controlled drug delivery. In McGinity JW. (Ed.),Aqueous polymeric coatings <strong>for</strong> pharmaceutical dosage <strong>for</strong>ms, Marcel Dekker Inc, 1997;79: 582.55. Barnhart S, Thin film oral dosage <strong>for</strong>ms, in Rathbone MJ, Hadgraft J, Roberts MS, LaneME (Eds.), Modified-rele<strong>as</strong>e Drug Delivery Technology, In<strong>for</strong>ma Healthcare, 2008:209–216.16 | P a g e
- Page 3 and 4: DECLARATION“I certify that this w
- Page 6 and 7: taste masking effect of the process
- Page 8 and 9: CHAPTER 2: DISSOLUTION ENHANCEMENT
- Page 10 and 11: 3.2 Powder and ODT characterization
- Page 12 and 13: 3.7 In vitro drug release profiles
- Page 15: 3.1 Solubility parameters and extru
- Page 18 and 19: polymers.7.2 DSC findings of all AP
- Page 20 and 21: 2.4b Diffractograms of FMT formulat
- Page 22 and 23: 4.3 Schematic representation of the
- Page 24 and 25: 55 exrudates (b) DPD/L100-55 PM (c)
- Page 26 and 27: 8.5d A plot of the logarithm of HCS
- Page 28 and 29: L100Eudragit L100L100-55 Eudragit L
- Page 30 and 31: Maniruzzaman M, Rai D, Boateng JS.
- Page 32 and 33: Maniruzzaman M, Boateng JS, Bonnefi
- Page 34 and 35: CHAPTER 1: INTRODUCTION1.0 Backgrou
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- Page 38 and 39: homogenize but also compress the ex
- Page 40 and 41: properties of polymers and excipien
- Page 42 and 43: particles‘ wettability [46] . A v
- Page 44 and 45: Table 1.2: Different hot-melt extru
- Page 46 and 47: 1.8 Aims and objectivesThe purpose
- Page 50 and 51: 56. International Conference on Har
- Page 52 and 53: CHAPTER 2: DISSOLUTION ENHANCEMENT
- Page 54 and 55: Fdid ,Vi F2pip , p( Ehi/ ViVi )i =
- Page 56 and 57: used. Each sample was scanned from
- Page 58 and 59: Furthermore, by means of thermodyna
- Page 60 and 61: 3.2 Particle size morphology and pa
- Page 62 and 63: Fig. 2.4a: Diffractograms of INM fo
- Page 64 and 65: However, the DSC thermograms of the
- Page 66 and 67: Fig. 2.5b: DSC thermograms of INM a
- Page 68 and 69: Fig. 2.5e: DSC thermograms of FMT a
- Page 70 and 71: Nevertheless, more than 80% FMT was
- Page 72 and 73: 6. Caron V, Tajber L, Corrigan OI,
- Page 74 and 75: CHAPTER 3: DEVELOPMENT AND EVALUATI
- Page 76 and 77: 2.2 Hot-Melt extrusionHot-melt extr
- Page 78 and 79: Committee of the University of Gree
- Page 80 and 81: The PM of formulation II (40% IBU)
- Page 82 and 83: Fig. 3.3: DSC thermograms of pure I
- Page 84 and 85: As a general rule, the powder compr
- Page 86 and 87: Fig. 3.4: Schematic diagram of ODT
- Page 88 and 89: Fig. 3.5: Schematic diagram of ODTs
- Page 90 and 91: Fig. 3.7: Schematic diagram of ODTs
- Page 92 and 93: F2 0 0.5 0 1 0 1F6 0 0.5 0 1 0 2F7
- Page 94 and 95: 6. M.F. Al-Omran, S.A. Al-Suwayeh,
- Page 96 and 97: 30. L. Saerens, L. Dierickx, B. Len
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leading to significant variations w
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2.6. In vitro drug release studiesI
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v2d 2p(4.1)Table 4.1: Calculated so
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The observed melting peaks are shif
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Fig. 4.2a: Powder XRPD patterns of
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Interestingly, no difference was ob
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7 Astree sensors Taste masking effi
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The in vitro e-tongue evaluation wa
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3. K. Woertz, C. Tissen, P. Kleineb
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25. B.C. Hancock, P. York, R.C. Row
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CHAPTER 5: AN IN VIVO AND IN VITRO
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(dispersion forces and polarization
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Table 5.1: Sample preparation for t
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Table 5.2: Solubility parameters ca
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Physical mixtures (PM) and extruded
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Fig. 5.2c: Thermograms of CTZ and V
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masking effect for active concentra
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Fig. 5.5b: Distance and discriminat
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Table 5.4: Mean standard deviation
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Fig. 5.6b: Release profiles of VRP
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17. Woertz K,Tissen C, Kleinebudde
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scale or lower. XPS is more accurat
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patterns were identified after ener
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3.3 Differential scanning calorimet
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Fig. 6.3a: Diffractograms of PRP fo
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good agreement with the anticipated
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Since L100 contained higher proport
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at ~533.01 eV is the combination of
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Finally, the XPS analysis confirmed
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Fig. 6.6b: 1 H NMR spectra of all P
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6) Bonferoni, M.C.; Rossi, S.; Ferr
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26) Vandencasteele, N.; Reniers, F.
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Gibbs free energy change before and
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2.5 Hot-melt extrusion (HME) proces
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2.11 X-ray photoelectron spectrosco
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Table 7.2: DSC findings of all APIs
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3.4 In vivo and in vitro taste mask
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Fig. 7.3c: Normalised DI (%) of all
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Table 7.4: Binding energy calculati
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PRP/ polymers extruded in compariso
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atom as NH + 4 . This observed N 1s
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8.0 ConclusionsThe presence of inte
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20. Davies MC, Wilding IR, Short RD
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CHAPTER 8: SUSTAINED RELEASE HYDROC
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2.3 Preparation of formulation blen
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medium pH was maintained as 1.2 by
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Fig. 8.1: SEM images of [(a), (b)]
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Fig. 8.2b: DSC transitions of HCS/E
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in the range of 10-12 kP. However,
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ate and time on the basis of Eq. (8
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Fig. 8.5c: A plot of the cubic root
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when n > 0.89. From the results of
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14. Lam PL, Lee KKH,Wong RSM, Cheng
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Furthermore, HME has successfully b
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Supp. Fig. 2: XPS O 1s peaks for PR
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Supp. Fig. 4: O 1s BE peaks for L10
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8.2 s 6.2 s 3.8 s 1.8 s 200 msS
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12.2 s 9.0 s 6.2 s 3.8 s 1.8 s
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Supplementary table 1: Solubility p
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N = 55000/ 219.2 = 250.912Density:
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(4) Eudragit L100, N = (125000/202