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

More documents

Recommendations

Info

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
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
Page 98 and 99:
leading to significant variations w
Page 100 and 101:
2.6. In vitro drug release studiesI
Page 102 and 103:
v2d 2p(4.1)Table 4.1: Calculated so
Page 104 and 105:
The observed melting peaks are shif
Page 106 and 107:
Fig. 4.2a: Powder XRPD patterns of
Page 108 and 109:
Interestingly, no difference was ob
Page 110 and 111:
7 Astree sensors Taste masking effi
Page 112 and 113:
The in vitro e-tongue evaluation wa
Page 114 and 115:
3. K. Woertz, C. Tissen, P. Kleineb
Page 116 and 117:
25. B.C. Hancock, P. York, R.C. Row
Page 118 and 119:
CHAPTER 5: AN IN VIVO AND IN VITRO
Page 120 and 121:
(dispersion forces and polarization
Page 122 and 123:
Table 5.1: Sample preparation for t
Page 124 and 125:
Table 5.2: Solubility parameters ca
Page 126 and 127:
Physical mixtures (PM) and extruded
Page 128 and 129:
Fig. 5.2c: Thermograms of CTZ and V
Page 130 and 131:
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 182 and 183:
20. Davies MC, Wilding IR, Short RD
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
show all

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

You also want an ePaper? Increase the reach of your titles

Delete template?

Save as template?