Development of hot-melt extrusion as a novel technique for the ...

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20. Davies MC, Wilding IR, Short RD, Khan MA, Watts JF, Melia CD. An analysis ofthe surface chemical structure of polymethacrylate (Eudragit) film coating polymersby XPS. Int. J Pharm.1989; 57: 183-187.21. Flory PJ. Principles of polymer chemistry. Ithaca, New York: Cornell UniversityPress. 195322. Marsac PJ, Shamblin SL, Taylor LS. Theoretical and practical approaches forprediction of drug–polymer miscibility and solubility. Pharm Res. 2006; 23:2417–2426.23. Friesen DT, Shanker R, Crew M, Smithey DT, Curatolo WJ, Nightingale JAS. 2008.Hydroxypropyl methylcellulose acetate succinate-based spray-dried dispersions: Anoverview. Mol. Pharm. 2008; 5:1003–1019.24. Nishi T, Wang TT. Melting point depression and kinetic effects of cooling oncrystallization in poly (vinylidene fluride)-poly (methyl methacrylate) mixtures.Macromolecules. 1975; 8:909–915.25. Hildebrand J, Scott R. Solubility of non-electrolytes. 3 rd ed. New York:Reinhold.1950.26. Maniruzzaman M, Rana MM, Boateng JS, Mitchell JC, Douroumis D. Dissolutionenhancement of poorly water-soluble APIs processed by hot-melt extrusion usinghydrophilic polymers. Drug Dev. Ind. Pharm. 2012. In press.27. Bagley EB, Nelson TP & Scigliano JM. Three-dimensional solubility parameters andtheir relationship to internal pressure measurements in polar and hydrogen bondingsolvents. J Paint. Technol. 1971; 43: 35-42.28. WMA Declaration of Helsinki - Ethical Principles for Medical Research InvolvingHuman Subjects. 59 th WMA General Assembly, Seoul, Korea, October 2008.29. Gauss View, Version 5, Roy Dennington, Todd Keith and John Millam, SemichemInc. Shawnee Mission KS, 2009.30. Frisch MJ, Trucks GW, Schlegel HB, Scuseria GE, Robb MA, Cheeseman JR et al.Gaussian 09, Revision B.1, Gaussian, Inc., Wallingford CT, 2009.31. Zhao Y, Truhlar DG. The M06 suite of density functionals for main groupthermochemistry, thermochemical kinetics, noncovalent interactions, excited states,and transition elements: two new functionals and systematic testing of four M06-classfunctionals and 12 other functional. Chem. Acc. 2008; 120: 215– 241.149 | P a g e
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Page 3 and 4:
DECLARATION“I certify that this w
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taste masking effect of the process
Page 8 and 9:
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
Page 22 and 23:
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
Page 34 and 35:
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
Page 44 and 45:
Table 1.2: Different hot-melt extru
Page 46 and 47:
1.8 Aims and objectivesThe purpose
Page 48 and 49:
29. Zheng X, Yang R, Tang X and Zhe
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56. International Conference on Har
Page 52 and 53:
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
Page 64 and 65:
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,
Page 74 and 75:
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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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
Page 132 and 133: Fig. 5.5b: Distance and discriminat
Page 134 and 135: Table 5.4: Mean standard deviation
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
Page 142 and 143: patterns were identified after ener
Page 144 and 145: 3.3 Differential scanning calorimet
Page 146 and 147: Fig. 6.3a: Diffractograms of PRP fo
Page 148 and 149: good agreement with the anticipated
Page 150 and 151: Since L100 contained higher proport
Page 152 and 153: at ~533.01 eV is the combination of
Page 154 and 155: Finally, the XPS analysis confirmed
Page 156 and 157: Fig. 6.6b: 1 H NMR spectra of all P
Page 158 and 159: 6) Bonferoni, M.C.; Rossi, S.; Ferr
Page 160 and 161: 26) Vandencasteele, N.; Reniers, F.
Page 162 and 163: Gibbs free energy change before and
Page 164 and 165: 2.5 Hot-melt extrusion (HME) proces
Page 166 and 167: 2.11 X-ray photoelectron spectrosco
Page 168 and 169: Table 7.2: DSC findings of all APIs
Page 170 and 171: 3.4 In vivo and in vitro taste mask
Page 172 and 173: Fig. 7.3c: Normalised DI (%) of all
Page 174 and 175: Table 7.4: Binding energy calculati
Page 176 and 177: PRP/ polymers extruded in compariso
Page 178 and 179: atom as NH + 4 . This observed N 1s
Page 180 and 181: 8.0 ConclusionsThe presence of inte
Page 184 and 185: CHAPTER 8: SUSTAINED RELEASE HYDROC
Page 186 and 187: 2.3 Preparation of formulation blen
Page 188 and 189: medium pH was maintained as 1.2 by
Page 190 and 191: Fig. 8.1: SEM images of [(a), (b)]
Page 192 and 193: Fig. 8.2b: DSC transitions of HCS/E
Page 194 and 195: in the range of 10-12 kP. However,
Page 196 and 197: ate and time on the basis of Eq. (8
Page 198 and 199: Fig. 8.5c: A plot of the cubic root
Page 200 and 201: when n > 0.89. From the results of
Page 202 and 203: 14. Lam PL, Lee KKH,Wong RSM, Cheng
Page 204 and 205: Furthermore, HME has successfully b
Page 206 and 207: Supp. Fig. 2: XPS O 1s peaks for PR
Page 208 and 209: Supp. Fig. 4: O 1s BE peaks for L10
Page 210 and 211: 8.2 s 6.2 s 3.8 s 1.8 s 200 msS
Page 212 and 213: 12.2 s 9.0 s 6.2 s 3.8 s 1.8 s
Page 214 and 215: Supplementary table 1: Solubility p
Page 216 and 217: N = 55000/ 219.2 = 250.912Density:
Page 218 and 219: (4) Eudragit L100, N = (125000/202
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