6) Bonferoni, M.C.; Rossi, S.; Ferrari, F.; Bettinetti, G.P.; Caramella, C.Characterization <strong>of</strong> a diltiazem–lambda carrageenan complex. Int. J. Pharm.2000,200, 207–216.7) Lelham, N.C.; Sundel<strong>of</strong>, L.O. Some <strong>as</strong>pects on characterization and properties <strong>of</strong>charged polysaccharides. An investigation <strong>of</strong> <strong>the</strong> system carrageenan/amitriptyline/water with relation to amphiphile adsorption and charge density. Int. J.Pharm. 1995, 115, 103–111.8) Takka, S. Propranolol hydrochloride/anionic polymer binding interaction. Il Farmaco.2003, 58, 1051-1056.9) Puttipipatkhachorna, S.; Nunthanidb, J.; Yamamotoc, K.; Peckd, G. E. Drug physicalstate and drug–polymer interaction on drug rele<strong>as</strong>e from chitosan matrix films. J <strong>of</strong>Controlled Rele<strong>as</strong>e. 201, 75,143–153.10) Baer, D. R.; Engelhard, M.H. XPS analysis <strong>of</strong> nanostructured materials and biologicalsurfaces Journal <strong>of</strong> Electron Spectroscopy and Related Phenomena. 2010, 178, 415–432.11) Li, J.; M<strong>as</strong>so, J. J.; Guertin, J. A. Prediction <strong>of</strong> drug solubility in an acrylate adhesiveb<strong>as</strong>ed on <strong>the</strong> drug–polymer interaction parameter and drug solubility in acetonitrile.Journal <strong>of</strong> Controlled Rele<strong>as</strong>e. 2003, 83, 211–221.12) Davies, M. C.; Wilding, I. R.; Short, R. D.; Khan,M. A.; Watts, J. F.; Melia, C. D. Ananalysis <strong>of</strong> <strong>the</strong> surface chemical structure <strong>of</strong> polymethacrylate (Eudragit) film coatingpolymers by XPS. International Journal <strong>of</strong> Pharmaceutics.1989, 57, 183-187.13) Takka, S.; Rajbhandari, S.; Sakr, A. Effcet <strong>of</strong> anionic polymers on <strong>the</strong> rele<strong>as</strong>e <strong>of</strong>propranolol hydrochloride from matrix tablets. Eur. J. Pharm. Biopharm. 2001, 52,75-82.14) Maniruzzaman, M.; Boateng, J. S.; Bonnefille, M.; Aranyos, A.; Mitchell, J. C.;Douroumis, D. T<strong>as</strong>te m<strong>as</strong>king <strong>of</strong> paracetamol by <strong>hot</strong>-<strong>melt</strong> <strong>extrusion</strong>: an in vitro and invivo evaluation. Eur J Pharm Biopharm. 2012, 80(2), 433-42.15) Gauss View, Version 5, Roy Dennington, Todd Keith and John Millam, SemichemInc., Shawnee Mission KS, 2009.16) Beamson, G.; Briggs, D. High resolution XPS <strong>of</strong> organic polymers: The ScientaESCA 300 Datab<strong>as</strong>e. J. Chem. Educ. 1993, 70, PA25.17) Wang, L.; Cui, F. D.; Hay<strong>as</strong>e, T.; Sunada, H. Preparation and evaluation <strong>of</strong> soliddispersion <strong>for</strong> nitrendipine-carbopol and nitrendipine-HPMCP systems using a twinscrew extruder. Chem. Pharm. Bull. 2005, 53(10), 1240–1245.125 | P a g e
18) Forster, A.; Hempenstall, J.; Tucker, I.; Rades, T. Selection <strong>of</strong> excipients <strong>for</strong> <strong>melt</strong><strong>extrusion</strong> with two poorly water-soluble drugs by solubility parameter calculation and<strong>the</strong>rmal analysis. Int J Pharm 2001, 226(1–2), 147–161.19) Zheng, X.; Yang, R.; Tang, X.; Zheng, L. Part I: Characterization <strong>of</strong> Solid Dispersions<strong>of</strong> Nimodipine Prepared by Hot-<strong>melt</strong> Extrusion. Drug Dev Ind Pharm 2007, 33, 791–802.20) Gryczke, A.; Schminke, S.; Maniruzzaman, M.; Beck, J.; Douroumis D. <strong>Development</strong>and evaluation <strong>of</strong> orally disintegrating tablets (ODTs) containing Ibupr<strong>of</strong>en granulesprepared by <strong>hot</strong> <strong>melt</strong> <strong>extrusion</strong>. Colloids Surf B. Biointerfaces. 2011, 86(2),275-84.21) Tabary, N.; Mahieu, A.; Willart, J-F.; Dudognon, E.; Danède, F.; Descamps, M.;Bacquet, M.; Martel, B. Characterization <strong>of</strong> <strong>the</strong> hidden gl<strong>as</strong>s transition <strong>of</strong> amorphouscyclomaltoheptaose. Carbohydrate Res. 2011, 346, 2193–2199.22) Delplacea, C.; Kreyea, F. Klosea, D.; Danedec, F.; Descampsc, M.; Siepmanna, J.;Siepmanna, F. Impact <strong>of</strong> <strong>the</strong> experimental conditions on drug rele<strong>as</strong>e from parenteraldepot systems: From negligible to significant. Int. J. <strong>of</strong> Pharm. 2012, 432, 11– 22.23) Frisch, M. J.; Trucks, G. W.; Schlegel, H. B.; Scuseria, G. E.; Robb, M. A.;Cheeseman, J. R.; Scalmani, G.; Barone, V.; Mennucci, B.; Petersson, G. A.;Nakatsuji, H.; Caricato, M.; Li, X.; Hratchian, H. P.; Izmaylov, A. F.; Bloino, J.;Zheng, G.; Sonnenberg, J. L.; Hada, M.; Ehara, M.; Toyota, K.; Fukuda, R.;H<strong>as</strong>egawa, J.; Ishida, M.; Nakajima, T.; Honda, Y.; Kitao, O.; Nakai, H.; Vreven, T.;Montgomery, J., J. A. ; Peralta, J. E.; Ogliaro, F.; Bearpark, M.; Heyd, J. J.; Bro<strong>the</strong>rs,E.; Kudin, K. N.; Staroverov, V. N.; Kobay<strong>as</strong>hi, R.; Normand, J.; Raghavachari, K.;Rendell, A.; Burant, J. C.; Iyengar, S. S.; Tom<strong>as</strong>i, J.; Cossi, M.; Rega, N.; Millam, N.J.; Klene, M.; Knox, J. E.; Cross, J. B.; Bakken, V.; Adamo, C.; Jaramillo, J.;Gomperts, R.; Stratmann, R. E.; Yazyev, O.; Austin, A. J.; Cammi, R.; Pomelli, C.;Ochterski, J. W.; Martin, R. L.; Morokuma, K.; Zakrzewski, V. G.; Voth, G. A.;Salvador, P.; Dannenberg, J. J.; Dapprich, S.; Daniels, A. D.; Fark<strong>as</strong>, Ö.; Foresman, J.B.; Ortiz, J. V.; Cioslowski, J.; Fox, D. J. Gaussian 09, Revision B.1, Gaussian, Inc.,Walling<strong>for</strong>d CT, 2009.24) R. Dennington, T. Keith, J. Millam. Gauss View, Version 5, Semichem Inc., ShawneeMission KS. 2009.25) Choong, C.; Griffiths, J-P.; Moloney, M. G.; Triffitt, J.; Swallow, D. Directintroduction <strong>of</strong> phosphonate by <strong>the</strong> surface modification <strong>of</strong> polymers enhancesbiocompatibility. Reactive & Functional Polymers. 2009, 69, 77–85.126 | P a g e
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DECLARATION“I certify that this w
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taste masking effect of the process
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CHAPTER 2: DISSOLUTION ENHANCEMENT
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3.2 Powder and ODT characterization
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3.7 In vitro drug release profiles
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3.1 Solubility parameters and extru
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polymers.7.2 DSC findings of all AP
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2.4b Diffractograms of FMT formulat
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4.3 Schematic representation of the
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55 exrudates (b) DPD/L100-55 PM (c)
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8.5d A plot of the logarithm of HCS
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L100Eudragit L100L100-55 Eudragit L
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Maniruzzaman M, Rai D, Boateng JS.
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Maniruzzaman M, Boateng JS, Bonnefi
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CHAPTER 1: INTRODUCTION1.0 Backgrou
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Table 1.1: HME and other convention
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homogenize but also compress the ex
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properties of polymers and excipien
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particles‘ wettability [46] . A v
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Table 1.2: Different hot-melt extru
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1.8 Aims and objectivesThe purpose
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29. Zheng X, Yang R, Tang X and Zhe
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56. International Conference on Har
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CHAPTER 2: DISSOLUTION ENHANCEMENT
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Fdid ,Vi F2pip , p( Ehi/ ViVi )i =
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used. Each sample was scanned from
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Furthermore, by means of thermodyna
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3.2 Particle size morphology and pa
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Fig. 2.4a: Diffractograms of INM fo
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However, the DSC thermograms of the
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Fig. 2.5b: DSC thermograms of INM a
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Fig. 2.5e: DSC thermograms of FMT a
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Nevertheless, more than 80% FMT was
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6. Caron V, Tajber L, Corrigan OI,
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CHAPTER 3: DEVELOPMENT AND EVALUATI
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2.2 Hot-Melt extrusionHot-melt extr
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Committee of the University of Gree
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The PM of formulation II (40% IBU)
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Fig. 3.3: DSC thermograms of pure I
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As a general rule, the powder compr
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Fig. 3.4: Schematic diagram of ODT
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Fig. 3.5: Schematic diagram of ODTs
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Fig. 3.7: Schematic diagram of ODTs
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F2 0 0.5 0 1 0 1F6 0 0.5 0 1 0 2F7
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6. M.F. Al-Omran, S.A. Al-Suwayeh,
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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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- Page 140 and 141: scale or lower. XPS is more accurat
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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