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

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Fig. 5.6b: Release profiles of VRP extruded formulations (paddle speed 100 rpm, pH 1.2 (6.8after 2 hr), n=3).4.0 ConclusionsIn this current chapter hot melt extrusion has been employed as a robust processingtechnique for the manufacture of taste masked formulations based on VRP and CTZ. Both ofthe APIs were found to be in amorphous state after extrusion due to the formation of soliddispersions. The optimized formulations evaluated by both in vivo and in vitro taste maskingtests correlated with each other. The extruded formulations of L100 demonstrated better tastemasking compared to those of EZE while the e – tongue was found to be a valuable tool fortaste masking assessments and formulation development.5.0 References1. Maniruzzaman M, Boateng JS, Bonnefille M, Aranyos A, Mitchell JC, Douroumis D.Taste Masking Evaluation of Hot Melt Extruded Paracetamol using an ElectronicTongue. AAPS Journal. 2011,13: 5357.2. 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 Biointerfaces. 2011; 86(2):275-84.3. Ayenew Z, Puri V, Kumar L, Bansal AK. Trends in pharmaceutical taste maskingtechnologies: a patent review. Recent Pat Drug Deliv Formul.2009; 3: 26–39.103 | P a g e
4. Douroumis DD, Gryczke A, Schminke S. Development and evaluation of cetirizineHCl taste-masked oral disintegrating tablets. AAPS PharmSciTech. 2011;12:141-151.5. 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 ofacetaminophen granules: comparison between different preparation methods in ahigh-shear mixer. Eur J Pharm Sci. 2004;21:295–303.8. Benoit JP, Rolland H, Thies C, Vande Velde V. Method of coating particles andcoated spherical particles. US Patent. 2000;6(087):003.9. Mazen H, York P. Particle formation methods and their products. US Patent.2006;7(115):28010. Bora D, Borude P, Bhise K. Taste masking by spray-drying technique. AAPSPharmSciTech. 2008; 9: 1159–1164.11. Ono N, Miyamoto Y, Ishiguro T, Motoyama K, Hirayama F, Iohara D, Seo H,Tsuruta S, Arima H, Uekama K. Reduction of bitterness of antihistaminic drugs bycomplexation with ß-cyclodextrins. J Pharm Sci. 2010;100: 1935–1943.12. Woertz K, Tissen C, Kleinebudde P, Breitkreutz J. Rational development of tastemasked oral liquids guided by an electronic tongue. Int J Pharm. 2010; 400: 114–123.13. Suthar AM, Patel MM. Formulation and evaluation of taste masked suspension ofmetronidazole. Int J Appl Pharm. 2011; 3: 16–19.14. Menegon RF, Blau L, Janzantti NS, Pizzolitto AC, Corrêa MA, Monteiro M, ChungMC. A nonstaining and tasteless hydrophobic salt of chlorhexidine. J Pharm Sci.2011;100: 3130–3138.15. Michalk A, Kanikanti VR, Hamann HJ, Kleinebudde P. Controlled release of activeas a consequence of the die diameter in solid lipid extrusion. J Cont Release. 2008;132: 35–41.16. Woertz K, Tissen C, Kleinebudde P, Breitkreutz J. Taste sensing systems (electronictongues) for pharmaceutical applications. Int J Pharm. 2011; 417: 256– 271104 | 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
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 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
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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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