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

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4.3 Schematic representation of the taste scores of pure API, bulk polymers75and the extruded formulations.4.4a Electronic tongue ―taste map‖: Global signal comparison (PCA analysis76of the electrode responses) between pure PMOL and extrudedformulations with VA64 polymer after dissolution for 60s.4.4b Electronic tongue ―taste map‖: Global signal comparison (PCA analysis77of the electrode responses) between pure and extruded formulations withEPO polymer after dissolution for 60s.4.5 Distance and discrimination comparison between signal of 100% PMOL78formulation and each polymer‘s formulation on Astree e-tongue (after60s).4.6 Correlation of human sensory data ―Reference‖ with Astree electronic78tongue measurements ―Measured‖.4.7a Dissolution profiles of PMOL in PMOL/EPO extrudates (n=3). 794.7b Dissolution profiles of PMOL in PMOL/VA64 extrudates (n=3). 80CHAPTER 55.1 SEM images (magnification x 500) of (i) CTZ/L100 EXT, (ii) CTZ/EZE92EXT, (iii) VRP/L100 EXT and (iv) VRP/EZE EXT.5.2a DSC transitions of pure APIs and polymers. 935.2b Transitions of CTZ and VRP in L100 polymers systems. 945.2c Transitions of CTZ and VRP in EZE (L100-55) polymers systems. 955.3a Diffractograms of CTZ/polymer formulations. 955.3b Diffractograms of VRP/polymer formulations. 965.4 Sensory taste scores of human volunteers for all formulations and pure 97xxi | P a g e
materials.5.5a Signal comparison between active and placebo formulations with98Eudragit L100 and Acryl EZE coatings on cetirizine HCl and verapamilHCl (dissolution for 60s).5.5b Distance and discrimination comparison between signal of pure99cetirizine and verapamil HCl formulation and each polymer‘sformulation on Astree e-Tongue (after 60s dissolution).5.5c Correlation of human sensory data ―Reference‖ with Astree electronic100tongue measurements (―Measured‖) for both drugs.5.6a Release profiles of CTZ formulations (paddle speed 100 rpm, pH 1.2102(6.8 after 2 hr), n=3).5.6b Release profiles of VRP formulations (paddle speed 100 rpm, pH 1.2(6.8 after 2 hr), n=3).CHAPTER 66.1 SEM images of (a) PRP/L100 (Magnification x 2000), (b) PRP/L100-55103110(Magnification x 10K), (c) DPD/L100 (Magnification x 500) and (d)DPD/L100-55 (magnification x 10K) extruded formulations.6.2a DSC thermograms of pure drugs and pure polymers 1116.2b DSC thermograms of DPD/L100 (PM), DPD/L100 (EXT), DPD/L100-11255 (PM) and DPD/L100-55 (EXT).6.3a Diffractograms of PRP formulations: PRP pure (inset), (a) PRP/L100113PM (b) PRP/ L100 extrudates (c) PRP/L100-55 extrudates,(d) PRP/L100-55 PM.6.3b Diffractograms of DPD formulations: DPD pure (inset), (a) DPD/L100- 113xxii | 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 12 and 13: 3.7 In vitro drug release profiles
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 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,
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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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