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

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3.7 In vitro drug release profiles ...............................................................................1014.0 Conclusions .....................................................................................................................1035.0 References .......................................................................................................................103CHAPTER 6: DRUG-POLYMER INTERMOLECULAR INTERACTIONS IN HOT-MELT EXTRUDED SOLID DISPERSIONS1.0 Introduction .....................................................................................................................1062.0 Experimental sections .....................................................................................................1072.1 Materials .............................................................................................................1072.2 Determination of drug-polymer miscibility by Hansen solubility parameters()...........................................................................................................................1072.3 Hot-melt extrusion process .................................................................................1072.4 Scanning electron microscopy (SEM) ................................................................1082.5 Thermal analysis by differential scanning calorimetry (DSC)............................1082.6 X-ray powder diffraction (XRPD)......................................................................1082.7 Molecular modelling............................................................................................1082.8 X-ray photoelectron spectroscopy (XPS) analysis...............................................1092.9 Nuclear magnetic resonance (NMR) studies ......................................................1093.0 Results and discussion ...................................................................................................1093.1 Determination of drug-polymer miscibility by Hansen solubility parameters….1093.2 Scanning electron microscopy (SEM) ................................................................1103.3 Differential scanning calorimetry (DSC).............................................................1113.4 X-ray powder diffraction (XRPD).......................................................................1123.5 Intermolecular interactions of hot-melt extrudates.............................................1143.5.1 Molecular modelling.................................................................................114xi | P a g e
3.5.2 X-ray photoelectron spectroscopy (XPS)...................................................1143.5.3 Nuclear magnetic resonance (NMR) studies .............................................1214.0 Conclusions .....................................................................................................................1245.0 References ...................................................................................................................... 124CHAPTER 7: EVALUATION OF THE INTER-RELATION BETWEENINTERMOLECULAR INTERACTIONS AND TASTE MASKING EFFICIENCY INMELT EXTRUDED SOLID DISPERSIONS1.0 Introduction ....................................................................................................................1282.0 Materials and Methods ...................................................................................................1292.1 Materials .............................................................................................................1292.2 Hansen solubility parameters: prediction of drug/polymer miscibility...............1292.3 Flory-Huggins (F-H) theory for the prediction of drug/polymer interactionParameter..............................................................................................................1302.4 Differential scanning calorimetry (DSC) ............................................................1302.5 Preparation of formulation blends and hot-melt extrusion (HME) processing....1312.6 Particle morphology and size distribution ...........................................................1312.7 In vivo taste masking evaluation .........................................................................1312.8 In vitro taste masking evaluation: TS-5000Z sensing system .............................1322.9 Molecular modelling ..........................................................................................1322.10 Fourier Transform Infra-Red (FT-IR) analysis .................................................1322.11 X-ray photoelectron spectroscopy (XPS) analysis ............................................1333.0 Results and discussion......................................................................................................1333.1 Predictions of drug/polymer miscibility: solubility parameters...........................133xii | 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 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
Page 36 and 37: Table 1.1: HME and other convention
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 48 and 49: 29. Zheng X, Yang R, Tang X and Zhe
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
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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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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
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