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

More documents

Recommendations

Info

6) Bonferoni, M.C.; Rossi, S.; Ferrari, F.; Bettinetti, G.P.; Caramella, C.Characterization of a diltiazem–lambda carrageenan complex. Int. J. Pharm.2000,200, 207–216.7) Lelham, N.C.; Sundelof, L.O. Some aspects on characterization and properties ofcharged polysaccharides. An investigation of the system carrageenan/amitriptyline/water with relation to amphiphile adsorption and charge density. Int. J.Pharm. 1995, 115, 103–111.8) Takka, S. Propranolol hydrochloride/anionic polymer binding interaction. Il Farmaco.2003, 58, 1051-1056.9) Puttipipatkhachorna, S.; Nunthanidb, J.; Yamamotoc, K.; Peckd, G. E. Drug physicalstate and drug–polymer interaction on drug release from chitosan matrix films. J ofControlled Release. 201, 75,143–153.10) Baer, D. R.; Engelhard, M.H. XPS analysis of nanostructured materials and biologicalsurfaces Journal of Electron Spectroscopy and Related Phenomena. 2010, 178, 415–432.11) Li, J.; Masso, J. J.; Guertin, J. A. Prediction of drug solubility in an acrylate adhesivebased on the drug–polymer interaction parameter and drug solubility in acetonitrile.Journal of Controlled Release. 2003, 83, 211–221.12) Davies, M. C.; Wilding, I. R.; Short, R. D.; Khan,M. A.; Watts, J. F.; Melia, C. D. Ananalysis of the surface chemical structure of polymethacrylate (Eudragit) film coatingpolymers by XPS. International Journal of Pharmaceutics.1989, 57, 183-187.13) Takka, S.; Rajbhandari, S.; Sakr, A. Effcet of anionic polymers on the release ofpropranolol hydrochloride from matrix tablets. Eur. J. Pharm. Biopharm. 2001, 52,75-82.14) Maniruzzaman, M.; Boateng, J. S.; Bonnefille, M.; Aranyos, A.; Mitchell, J. C.;Douroumis, D. Taste masking of paracetamol by hot-melt extrusion: an in vitro and invivo evaluation. Eur J Pharm Biopharm. 2012, 80(2), 433-42.15) Gauss View, Version 5, Roy Dennington, Todd Keith and John Millam, SemichemInc., Shawnee Mission KS, 2009.16) Beamson, G.; Briggs, D. High resolution XPS of organic polymers: The ScientaESCA 300 Database. J. Chem. Educ. 1993, 70, PA25.17) Wang, L.; Cui, F. D.; Hayase, T.; Sunada, H. Preparation and evaluation of soliddispersion for nitrendipine-carbopol and nitrendipine-HPMCP systems using a twinscrew extruder. Chem. Pharm. Bull. 2005, 53(10), 1240–1245.125 | P a g e
18) Forster, A.; Hempenstall, J.; Tucker, I.; Rades, T. Selection of excipients for meltextrusion with two poorly water-soluble drugs by solubility parameter calculation andthermal analysis. Int J Pharm 2001, 226(1–2), 147–161.19) Zheng, X.; Yang, R.; Tang, X.; Zheng, L. Part I: Characterization of Solid Dispersionsof Nimodipine Prepared by Hot-melt Extrusion. Drug Dev Ind Pharm 2007, 33, 791–802.20) Gryczke, A.; Schminke, S.; Maniruzzaman, M.; Beck, J.; Douroumis D. Developmentand evaluation of orally disintegrating tablets (ODTs) containing Ibuprofen granulesprepared by hot melt extrusion. Colloids Surf B. Biointerfaces. 2011, 86(2),275-84.21) Tabary, N.; Mahieu, A.; Willart, J-F.; Dudognon, E.; Danède, F.; Descamps, M.;Bacquet, M.; Martel, B. Characterization of the hidden glass transition of amorphouscyclomaltoheptaose. Carbohydrate Res. 2011, 346, 2193–2199.22) Delplacea, C.; Kreyea, F. Klosea, D.; Danedec, F.; Descampsc, M.; Siepmanna, J.;Siepmanna, F. Impact of the experimental conditions on drug release from parenteraldepot systems: From negligible to significant. Int. J. of Pharm. 2012, 432, 11– 22.23) Frisch, M. J.; Trucks, G. W.; Schlegel, H. B.; Scuseria, G. E.; Robb, M. A.;Cheeseman, J. R.; Scalmani, G.; Barone, V.; Mennucci, B.; Petersson, G. A.;Nakatsuji, H.; Caricato, M.; Li, X.; Hratchian, H. P.; Izmaylov, A. F.; Bloino, J.;Zheng, G.; Sonnenberg, J. L.; Hada, M.; Ehara, M.; Toyota, K.; Fukuda, R.;Hasegawa, J.; Ishida, M.; Nakajima, T.; Honda, Y.; Kitao, O.; Nakai, H.; Vreven, T.;Montgomery, J., J. A. ; Peralta, J. E.; Ogliaro, F.; Bearpark, M.; Heyd, J. J.; Brothers,E.; Kudin, K. N.; Staroverov, V. N.; Kobayashi, R.; Normand, J.; Raghavachari, K.;Rendell, A.; Burant, J. C.; Iyengar, S. S.; Tomasi, J.; Cossi, M.; Rega, N.; Millam, N.J.; Klene, M.; Knox, J. E.; Cross, J. B.; Bakken, V.; Adamo, C.; Jaramillo, J.;Gomperts, R.; Stratmann, R. E.; Yazyev, O.; Austin, A. J.; Cammi, R.; Pomelli, C.;Ochterski, J. W.; Martin, R. L.; Morokuma, K.; Zakrzewski, V. G.; Voth, G. A.;Salvador, P.; Dannenberg, J. J.; Dapprich, S.; Daniels, A. D.; Farkas, Ö.; Foresman, J.B.; Ortiz, J. V.; Cioslowski, J.; Fox, D. J. Gaussian 09, Revision B.1, Gaussian, Inc.,Wallingford CT, 2009.24) R. Dennington, T. Keith, J. Millam. Gauss View, Version 5, Semichem Inc., ShawneeMission KS. 2009.25) Choong, C.; Griffiths, J-P.; Moloney, M. G.; Triffitt, J.; Swallow, D. Directintroduction of phosphonate by the surface modification of polymers enhancesbiocompatibility. Reactive & Functional Polymers. 2009, 69, 77–85.126 | 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 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 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 ...

Create successful ePaper yourself

Delete template?

Save as template?