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

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8.0 ConclusionsThe presence of intermolecular interactions has successfully led the HME to be arobust technique to form solid dispersions of both APIs into polymer matrix. The existence ofamorphous APIs into the polymer matrices has been confirmed by thermal analysis while anin vivo and in vitro taste masking analysis has substantially complemented each othershowing the masking potential of L100 better than L100-55. The molecular modellingoutlined a possible presence of intermolecular interactions between drug and polymermolecules and estimated the strength. The findings from FT-IR and XPS analysis has finallyconfirmed the mechanism of the interaction through H-bonding between the carboxyl groupof the anionic methacrylate co-polymer and the amide group of the active substances as wellas the interaction strength. These studies finally confirm that the stronger the integrationsbetter the taste masking in an opposite charged drug/polymers based extruded soliddispersions.9.0 References1. Douroumis DD, Gryczke A, Schminke S. Development and evaluation of cetirizineHCl taste-masked oral disintegrating tablets. AAPS PharmSciTech. 2011; 12: 141–151.2. Maniruzzaman M, Boateng JS, Bonnefille M, Aranyos A, Mitchell JC, Douroumis D.Taste masking of paracetamol by hot-melt extrusion: an in vitro and in vivoevaluation. Eur. J Pharm. Biopharm. 2012; 80(2): 433-42.3. Ayenew Z, Puri V, Kumar L, Bansal AK. Trends in pharmaceutical taste maskingtechnologies: a patent review. Recent Pat. Drug Deliv. Formul.2009; 3: 26–39.4. Bora D, Borude P, Bhise K. Taste masking by spray-drying technique. AAPSPharmSciTech. 2008; 9: 1159–1164.5. Al-Omran MF, Al-Suwayeh SA, El-Helw AM, Saleh SI. Taste masking of diclofenacsodium using microencapsulation. J Microencapsul. 2002; 19:45–52.6. Shah PP, Mashru RC, Rane YM, Thakkar A. Design and optimization of mefloquinehydrochloride microparticles for bitter taste masking. AAPS PharmSciTech. 2008;9:377–389.7. Albertini B, Cavallari C, Passerini N, Voinovich D, González-Rodríguez ML,Magarotto L, Rodriguez L. Characterization and taste-masking evaluation of147 | P a g e
acetaminophen granules: comparison between different preparation methods in ahigh-shear mixer. Eur. J Pharm. Sci. 2004; 21:295–303.8. Mazen H, York P. Particle formation methods and their products. US Patent.2006;7(115):2809. Michalk A, Kanikanti VR, Hamann HJ, Kleinebudde P. Controlled release of activeas a consequence of the die diameter in solid lipid extrusion. J Cont. Rel. 2008; 132:35–41.10. Gryczke A, Schminke S, Maniruzzaman M, Beck J, Douroumis D. Development andevaluation of orally disintegrating tablets (ODTs) containing Ibuprofen granulesprepared by hot melt extrusion. Coll. Surf B. Bioin. 2011; 86(2):275-84.11. Vaassena J, Bartscherb J, Breitkreutza J. Breit Taste masked lipid pellets withenhanced release of hydrophobic active ingredient. Int. J of Pharm.2012; 429:99– 10312. Woertz K, Tissen C, Kleinebudde P, Breitkreutz J. Taste sensing systems (electronictongues) for pharmaceutical applications. Int. J. Pharm. 2011; 417: 256– 27113. Woertz K,Tissen C, Kleinebudde P, Breitkreutz J. Performance qualification of anelectronic tongue based on ICH guideline Q2. J. Pharm. Biomed. Anal. 2010; 51: pp.497–506.14. Bonferoni, MC, Rossi S, Ferrari F, Bettinetti GP, Caramella C. Characterization ofa diltiazem–lambda carrageenan complex. Int. J. Pharm.2000; 200: 207–216.15. Lelham, NC, Sundelof LO. 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: 103–111.16. Takka S. Propranolol hydrochloride/anionic polymer binding interaction. Il Farmaco.2003; 58: 1051-1056.17. Puttipipatkhachorna S, Nunthanidb J, Yamamotoc K, Peckd GE. Drug physical stateand drug–polymer interaction on drug release from chitosan matrix films. J Cont. Rel.2011; 75:143–153.18. Baer DR, Engelhard MH. XPS analysis of nanostructured materials and biologicalsurfaces.J Elec. Spec. Rela. Pheno. 2010; 178: 415–432.19. Li J, Masso JJ, Guertin JA. Prediction of drug solubility in an acrylate adhesive basedon the drug–polymer interaction parameter and drug solubility in acetonitrile. J Cont.Rel. 2003; 83: 211–221.148 | P a g e
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DECLARATION“I certify that this w
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taste masking effect of the process
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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
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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
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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
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Table 1.2: Different hot-melt extru
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1.8 Aims and objectivesThe purpose
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29. Zheng X, Yang R, Tang X and Zhe
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56. International Conference on Har
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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
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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
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 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
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