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

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when n > 0.89. From the results of analysis of the apparent diffusion pattern, the value of n,has represented the diffusion pattern according to the Fickian diffusion [17] .Table 8.3: Dissolution rate constants and determination coefficients of HCS release fromcoated and uncoated tablets; n dissolution exponent.Dissolution modelsHCS/EC N10HCS/EC P7HCS/EC N10HCS/EC P7UncoatedUncoatedCoatedCoatedFirst order K 1 (h -1 ) 0.29 ± 0.013R 2 0.99220.31 ± 0.0270.97090.4215 ± 0.0570.92950.456±0.0680.9153Higuchi K 2 (% hr -1/2 ) 29.29 ± 1.56R 2 0.949829.48 ± 2.070.911334.41 ± 2.300.904034.418±2.3030.9040Hixson–CrowellK 3 (%h -1/3 ) 0.08 ± 0.005R 2 0.98380.089 ± 0.0080.96220.1182± 0.1760.89640.126±0.1970.8829Krosmer-Peppas K 4 (hr -n )31.32 ± 3.9132.95 ± 5.1440.48 ± 4.7742.20±6.11R 20.95320.92140.93750.8966n0.46 ± 0.060.44 ± 0.080.40± 0.0690.40±0.0694.0 ConclusionsIn the current study HME was used as a robust technique to develop time delayedcoated extruded tablet to provide sustained-release of HCS. The release patterns are governedby the polymer selection while performing the extrusion process and the coating respectively.The tablet was designed to release HCS in a pattern that imitates a healthy individual. Thedevelopment of the HCS extruded tablet by HME is preferable since its preparation is quick,economical with fewer process steps which will make the future pilot scale formulationdevelopments much easier. Furthermore, a full comparative analysis of drug releasemechanism confirmed the release of HCS in extruded tablets according to first order kineticmodel.167 | P a g e
5.0 References1. Breitenbach J. Melt extrusion: from process to drug delivery technology. Eur J PharmBiopharm 2002; 54:107–117.2. M.A. Repka, S.K. Battu, S.B. Upadhye, S. Thumma, M.M. Crowley, F. Zhang, C.Martin, J.W. McGinity, Pharmaceutical applications of hot-melt extrusion: Part II,Drug Dev Ind Pharm 2007; 33:1043–1057.3. Cilurzo F, Cupone I, Minghetti P, Selmin F, Montanari L. Fast dissolving films madeof maltodextrins, Eur J Pharm Biopharm 2008; 70: 895-900.4. Zhang F, McGinity JW. Properties of sustained-release tablets prepared by hot-meltextrusion. Pharm Dev Tech 1999; 4(2), 241–250.5. Maniruzzaman M, Boateng J, Douroumis D. Taste masking of bitter APIs by usinghot melt extrusion (HME). AAPS Journal 2011; 13 (S2): T3273-T3273. ISSN 1550-7416.6. Grunhagen HH, Muller O. Melt extrusion technology. Pharm Manu Int.1995 1, 167–170.7. Breitkreutz J, El-Saleh F, Kiera C, Kleinebudde P, Wiedey W. Pediatric drugformulations of sodium benzoate: II. Coated granules with a lipophilic binder. Eur JPharm Biopham 2003; 56, 255-60.8. De Brabander C, Vervaet C, Fiermans L, Remon JP. Matrix mini-tablets based onstarch/microcrystalline wax mixtures. Int J Pharm 2000; 199: 195-203.9. De Brabander C, Vervaet C, Remon JP. Development and evaluation of sustainedrelease mini-matrices prepared via hot melt extrusion. J Cont Rel 2003; 89: 235–247.10. Roblegg E, Jäger E, Hodzic A, Koscher G, Mohr S, Zimmer A, Khinast J.Development of sustained-release lipophilic calcium stearate pellets via hot meltextrusion. Eur J Pharm Biopharm 2011; 79:635–645.11. Clark MR, Johnson TJ, McCabe RT, Clark JT, Tuitupou A, Elgendy H, Friend DR,Kiser PF. A hot-melt extruded intravaginal ring for the sustained delivery of theantiretroviral microbicide UC781.J Pharm Sci 2012; 101(2):576-87.12. Vithani K, Maniruzzaman M, Mostafa S, Cuppok Y, Douroumis D. Compritol® 888ATO Lipid Matrices for Sustained Release Processed by Hot-Melt Extrusion. 39 thAnnual meeting and Exposition of CRS 2012, Quebec, Canada.13. Maniruzzaman M, Hossain MA, Douroumis D. Sustained release of hydrocortisonetablets processed by hot-melt extrusion (HME). UKPharmSci 2012a. UK168 | 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
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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
Page 150 and 151: Since L100 contained higher proport
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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 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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