3. K. Woertz, C. Tissen, P. Kleinebudde, J. Breitkreutz, Rational development <strong>of</strong> t<strong>as</strong>tem<strong>as</strong>ked oral liquids guided by an electronic tongue. Int. J. Pharm., 400 (2010), pp.114-23.4. T. Sato, K. Nishishita, Y. Okada, K. Toda, Effect <strong>of</strong> gap junction blocker -glycyrrhetinic acid on t<strong>as</strong>te disk cells in frog. Cell. Mol. Neurobiol., 29 (2009), pp.503–512.5. V. Lyall, T. –H. T. Phan, Z. Ren, S. Mummalaneni, P. Melone, S. Mahavadi, K. S.Murthy, J.A. DeSimone, Regulation <strong>of</strong> <strong>the</strong> putative TRPV 1t salt t<strong>as</strong>te receptor byphosphatidylinositol 4, 5-bisphosphate. J. Neurophysiol., 103 (2010), pp. 1337–1349.6. M.A. Repka, S.K. Battu, S.B. Upadhye, S. Thumma, M.M. Crowley, F. Zhang, C.Martin, J.W. McGinity, Pharmaceutical applications <strong>of</strong> <strong>hot</strong>-<strong>melt</strong> <strong>extrusion</strong>: Part II.Drug Dev Ind Pharm., 33 (2007), pp. 1043-57.7. M.M. Crowley, F. Zhang, M.A. Repka, S. Thumma, S.B. Upadhye, S.K. Battu, J.W.McGinity, C.Martin, Pharmaceutical applications <strong>of</strong> <strong>hot</strong>-<strong>melt</strong> <strong>extrusion</strong>: part I. DrugDev. Ind. Pharm., 33 (2007), pp. 909-26.8. A. Almeida, S. PossemiersS, M.N. Boone, T. De Beer, T. Quinten, L. VanHoorebeke, J.P. Remon, C. Vervaet. Ethylene vinyl acetate <strong>as</strong> matrix <strong>for</strong> oralsustained rele<strong>as</strong>e dosage <strong>for</strong>ms produced via <strong>hot</strong>-<strong>melt</strong> <strong>extrusion</strong>. Eur. J. Pharm.Biopharm.,77 (2011), pp. 297-305.9. E. Verhoeven, T.R. De Beer, E. Schacht, G. Van den Mooter, J.P. Remon, C. Vervaet.Influence <strong>of</strong> polyethylene glycol/polyethylene oxide on <strong>the</strong> rele<strong>as</strong>e characteristics <strong>of</strong>sustained-rele<strong>as</strong>e ethylcellulose mini-matrices produced by <strong>hot</strong>-<strong>melt</strong> <strong>extrusion</strong>: Invitro and in vivo evaluation. Eur J Pharm. Biopharm.72 (2009), pp. 463 - 470.10. E. Verhoeven, T.R.M. De Beer, G. Van den Mooter, J.P. Remon, C. Vervaet.Influence <strong>of</strong> <strong>for</strong>mulation and process parameters on <strong>the</strong> rele<strong>as</strong>e characteristics <strong>of</strong>ethylcellulose sustained-rele<strong>as</strong>e mini-matrices produced by <strong>hot</strong>-<strong>melt</strong> <strong>extrusion</strong>. Eur. J.Pharm. Biopharm., 69 (2008), pp. 312-31911. J. Liu, F. Zhang, J.W. McGinity. Properties <strong>of</strong> lipophilic matrix tablets containingphenylpropanolamine hydrochloride prepared by <strong>hot</strong>-<strong>melt</strong> <strong>extrusion</strong>. Eur. J. Pharm.Biopharm., 52 (2001), pp. 181-190.12. A. Gryczke, S. Schminke, M. Maniruzzaman, J. Beck, D. Douroumis, <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>. Coll Surf B Biointerfaces., 86 (2011), pp. 275-84.81 | P a g e
13. A. Michalk, V.-R. Kanikanti, H.-J. Hamann, P. Kleinebudde. Controlled rele<strong>as</strong>e <strong>of</strong>active <strong>as</strong> a consequence <strong>of</strong> <strong>the</strong> die diameter in solid lipid <strong>extrusion</strong>. J. ControlRele<strong>as</strong>e., 132 (2008), pp. 35-41.14. R. Witzleb, V.R. Kanikanti, H.J. Hamann, P. Kleinebudde. Solid lipid <strong>extrusion</strong> withsmall die diameters--electrostatic charging, t<strong>as</strong>te m<strong>as</strong>king and continuous production.Eur. J. Pharm. Biopharm., 77 (2011), pp. 170-7.15. J. Breitkreutz, F. El-Saleh, C. Kiera, P. Kleinebudde, W. Wiedey. Pediatric drug<strong>for</strong>mulations <strong>of</strong> sodium benzoate: II. Coated granules with a lipophilic binder. Eur. J.Pharm. Biopharm., 56 (2003), pp. 255-60.16. K. Woertz, C. Tissen, P. Kleinebudde, J. Breitkreutz, A comparative study on twoelectronic tongues <strong>for</strong> pharmaceutical <strong>for</strong>mulation development. J. Pharm. Biomed.Anal., 55 (2011), pp. 272-81.17. T. Harada, T. Uchida, M. Yoshida, Y. Kobay<strong>as</strong>hi, R. Narazaki, T. Ohwaki, A newmethod <strong>for</strong> evaluating <strong>the</strong> bitterness <strong>of</strong> medicines in development using a t<strong>as</strong>te sensorand a disintegration testing apparatus, Chem. Pharm. Bull., 58 (2010), pp. 1009–1014.18. K. Woertz, C. Tissen, P. Kleinebudde, J. Breitkreutz, Per<strong>for</strong>mance qualification <strong>of</strong> anelectronic tongue b<strong>as</strong>ed on ICH guideline Q2, J. Pharm. Biomed. Anal. 51 (2010), pp.497–506.19. H. Liu, P. Wang, X. Zhang, F. Shen, C.G. Gogos Effects <strong>of</strong> <strong>extrusion</strong> processparameters on <strong>the</strong> dissolution behavior <strong>of</strong> indomethacin in Eudragit E PO soliddispersions. Int. J. Pharm., 383 (2010), pp. 161-9.20. H. Suwardie, P. Wang, D.B. Todd, V. Panchal, M. Yang, C.G. Gogos. Rheologicalstudy <strong>of</strong> <strong>the</strong> mixture <strong>of</strong> acetaminophen and polyethylene oxide <strong>for</strong> <strong>hot</strong>-<strong>melt</strong> <strong>extrusion</strong>application. Eur. J. Pharm. Biopharm., (2011) (in press)21. P.J. H<strong>of</strong>tyzer, D.W.V Krevelen, Properties <strong>of</strong> polymers, Elsevier, Amsterdam, 1976.22. S. Khan, P. Kataria, P. Nakhat, Y.P. Pramod, T<strong>as</strong>te M<strong>as</strong>king <strong>of</strong> OndansetronHydrochloride by Polymer Carrier System and Formulation <strong>of</strong> Rapid-DisintegratingTablets, AAPS PharmSciTech., 8 (2007), pp. E1 – E723. H. Goel, N. Vora, V. Rana, A Novel Approach to Optimize and Formulate F<strong>as</strong>tDisintegrating Tablets <strong>for</strong> Nausea and Vomiting, AAPS PharmSciTech., 9 (2008)774–781.24. A. Forster, J. Hempenstall, I. Tucker, T. Rades, 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., 226 (1–2) (2001), pp. 147–161.82 | 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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- 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
- Page 98 and 99: leading to significant variations w
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- Page 102 and 103: v2d 2p(4.1)Table 4.1: Calculated so
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- Page 120 and 121: (dispersion forces and polarization
- Page 122 and 123: Table 5.1: Sample preparation for t
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- Page 126 and 127: Physical mixtures (PM) and extruded
- Page 128 and 129: Fig. 5.2c: Thermograms of CTZ and V
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- Page 136 and 137: Fig. 5.6b: Release profiles of VRP
- Page 138 and 139: 17. Woertz K,Tissen C, Kleinebudde
- Page 140 and 141: scale or lower. XPS is more accurat
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- Page 152 and 153: at ~533.01 eV is the combination of
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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