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«Dissertation Zur Erlangung des Doktorgrades der Naturwissenschaften Der Fakultät für Mathematik, Informatik und Naturwissenschaften der ...»

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The mechanisms of drug release from solid dispersions in water-soluble polymers.

Int. J. Pharm. 231: 131-144 (2002) [70] Corrigan, O.I.

Mechanisms of dissolution of fast release solid dispersions.

Drug Dev. Ind. Pharm. 11: 697-724 (1985)

–  –  –

[72] Nazzal, S., Nutan, M., Palamakula, A., Shah, R., Zaghloul, A.A., Khan, M.A.

Optimization of a self-nanoemulsified tablet dosage form of ubiquinone using response surface methodology: effect of formulation ingredients.

Int. J. Pharm. 240: 103-114 (2002) [73] Agarwal, V., Siddiqui, A., Ali, H., Nazzal, S.

Dissolution and powder flow characterization of solid self-emulsified drug delivery system (SEDDS).

Int. J. Pharm. 366: 44-52 (2009) [74] Bansal, T., Mustafa, G., Khan, Z.I., Ahmad, F.J., Khar, R.K., Talegaonkar, S.

Solid self-nanoemulsifying delivery systems as a platform technology for formulation of poorly soluble drugs.

Crit. Rev. Ther. Drug Carrier Syst. 25: 63-116 (2008) [75] Mahmoud, E.A., Bendas, E.R., Mohamed, M.I.

Preparation and evaluation of self-nanoemulsifying tablets of carvedilol.

AAPS PharmSciTech 10: 183-192 (2009) [76] Dehaan, P., Lerk, C.F.

Oral controlled release dosage forms. A review.

Pharm. Weekbl. Sci. 6: 57-67 (1984) [77] Khan, M.Z.I.

Recent trends and progress in sustained or controlled oral delivery of some water soluble drugs: morphine salts, diltiazem and captopril.

Drug Dev. Ind. Pharm. 21: 1037-1070 (1995)

–  –  –

[79] Lotfipour, F., Nokhodchi, A., Saeedi, M., Norouzi-Sani, S., Sharbafi, J., SiahiShadbad, M.R.

The effect of hydrophilic and lipophilic polymers and fillers on the release rate of atenolol from HPMC matrices.

Farmaco 59: 819-825 (2004) [80] Razzak, M.S.M.I., Khan, F., Hossain, M., Khan, M.Z.R., Azad, M.A.K., Reza, M.S.

Effect of channeling agents on the release pattern of theophylline from Kollidon SR based matrix tablets.

Pak. J. Pharm. Sci. 22: 303-307 (2009) [81] Dvorackova, K., Rabiskova, M., Masteikova, R., Muselik, J., Krejcova, K.

Soluble filler as a dissolution profile modulator for slightly soluble drugs in matrix tablets.

Drug Dev. Ind. Pharm. 35: 930-940 (2009) [82] Dahl, T.C., Calderwood, T., Bormeth, A., Trimble, K., Piepmeier, E.

Influence of physicochemical properties of hydroxypropyl methylcellulose on naproxen release from sustained-release matrix tablets.

J. Control. Release 14: 1-10 (1990) [83] Baveja, S.K., Rao, K.V.R., Devi, K.P.

Zero-order release hydrophilic matrix tablets of β-adrenergic blockers.

Int. J. Pharm. 39: 39-45 (1987)

–  –  –

[85] Husson, I., Leclerc, B., Spenlehauer, G., Veillard, M., Couarraze, G.

Modeling of drug release from pellets coated with an insoluble polymeric membrane.

J. Control. Release 17: 163-173 (1991) [86] Dittgen, M., Durrani, M., Lehmann, K.

Acrylic polymers - a review of pharmaceutical applications.

STP Pharma Sci. 7: 403-437 (1997) [87] Baveja, S.K., Rao, K.V.R., Singh, A.

Sustained release tablet formulation of diethylcarbamazine.

Int. J. Pharm. 19: 229-231 (1984) [88] Qiao, M., Luo, Y., Zhang, L., Ma, Y., Stephenson, T.S., Zhu, J.

Sustained release coating of tablets with Eudragit® RS/RL using a novel electrostatic dry powder coating process.

Int. J. Pharm. 399: 37-43 (2010) [89] Bodmeier, R., Paeratakul, O.

Theophylline tablets coated with aqueous latexes containing dispersed pore formers.

J. Pharm. Sci. 79: 925-928 (1990) [90] Guo, X., Chang, R.K., Hussain, M.A.

Ion-exchange resins as drug delivery carriers.

J. Pharm. Sci. 98: 3886-3902 (2009) [91] Sriwongjanya, M., Bodmeier, R.

Effect of ion exchange resins on the drug release from matrix tablets.

Eur. J. Pharm. Biopharm. 46: 321-327 (1998)

–  –  –

[93] Bi, Y., Mao, S., Gan, L., Li, Y., Wang, C., Xu, N., Zheng, Y., Cheng, Q., Hou, S.

A controlled porosity osmotic pump system with biphasic release of theophylline.

Chem. Pharm. Bull. 55: 1574-1580 (2007) [94] Guthmann, C., Lipp, R., Wagner, T., Kranz, H.

Development of a novel osmotically driven drug delivery system for weakly basic drugs.

Eur. J. Pharm. Biopharm. 69: 667-674 (2008) [95] Gupta, R.N., Gupta, R., Basniwal, P.K., Rathore, G.S.

Osmotically controlled oral drug delivery systems: a review.

Int. J. Ph. Sci. 1: 269-275 (2009) [96] Saha, S., Shahiwala, A.F.

Multifunctional coprocessed excipients for improved tabletting performance.

Expert Opin. Drug Del. 6: 197-208 (2009) [97] Edge, S., Steele, D.F., Chen, A.S., Tobyn, M.J., Staniforth, J.N.

The mechanical properties of compacts of microcrystalline cellulose and silicified microcrystalline cellulose.

Int. J. Pharm. 200: 67-72 (2000) [98] Hwang, R.C., Peck, G.R.

A systematic evaluation of the compression and tablet characteristics of various types of microcrystalline cellulose.

Pharm. Technol. 25: 112-132 (2001)

–  –  –

[100] Bolhuis, G.K., Armstrong, N.A.

Excipients for direct compaction - an update.

Pharm. Dev. Technol. 11: 111-124 (2006) [101] Sherwood, B.E., Becker, J.W.

A new class of high-functionality excipients: silicified microcrystalline cellulose.





Pharm. Technol. 22: 78-88 (1998) [102] Aljaberi, A., Chatterji, A., Shah, N.H., Sandhu, H.K.

Functional performance of silicified microcrystalline cellulose versus microcrystalline cellulose: a case study.

Drug Dev. Ind. Pharm. 35: 1066-1071 (2009) [103] Tobyn, M.J., McCarthy, G.P., Staniforth, J.N., Edge, S.

Physicochemical comparison between microcrystalline cellulose and silicified microcrystalline cellulose.

Int. J. Pharm. 169: 183-194 (1998) [104] Steele, D.F., Tobyn, M., Edge, S., Chen, A., Staniforth, J.N.

Physicochemical and mechanical evaluation of a novel high density grade of silicified microcrystalline cellulose.

Drug Dev. Ind. Pharm. 30: 103-109 (2004) [105] Schlack, H., Bauer-Brandl, A., Schubert, R., Becker, D.

Properties of Fujicalin®, a new modified anhydrous dibasic calcium phosphate for direct compression: comparison with dicalcium phosphate dihydrate.

Drug Dev. Ind. Pharm. 27: 789-801 (2001)

–  –  –

[107] Hentzschel, C.M., Sakmann, A., Leopold, C.S.

Suitability of various excipients as carrier and coating materials for liquisolid compacts.

Drug Dev. Ind. Pharm., in press (2011) [108] Brunauer, S., Emmet, P.H., Teller, E.

Adsorption of gases in multimolecular layers.

J. Am. Chem. Soc. 60: 309-319 (1938) [109] Fell, J.T., Newton, J.M.

The tensile strength of lactose tablets.

J. Pharm. Sci. 20: 657-659 (1968) [110] Fell, J.T., Newton, J.M.

Determination of tablet strength by the diametral-compression test.

J. Pharm. Sci. 59: 688-691 (1970) [111] Fell, J.T., Newton, J.M.

The prediction of the tensile strength of tablets.

J. Pharm. Pharmacol. 22: 247-248 (1970) [112] Heckel, R.W.

An analysis of powder compaction phenomena.

Trans. Metall. Soc. AIME 221: 1001-1008 (1961) [113] Heckel, R.W.

Density-pressure relationships in powder compaction.

Trans. Metall. Soc. AIME 221: 671-675 (1961)

–  –  –

[115] Iloanusi, N.O., Schwartz, J.B.

The effect of wax on compaction of microcrystalline cellulose beads made by extrusion and spheronization.

Drug Dev. Ind. Pharm. 24: 37-44 (1998) [116] Duberg, M., Nystroem, C.

Studies on direct compression of tablets. XVII. Porosity-pressure curves for the characterization of volume reduction mechanisms in powder compression.

Powder Technol. 46: 67-75 (1986) [117] Kawakita, K., Luedde, K.H.

Some considerations on powder compression equations.

Powder Technol. 4: 61-68 (1970) [118] Garr, J.S.M., Rubinstein, M.H.

The effect of rate of force application on the properties of microcrystalline cellulose and dibasic calcium phosphate mixtures.

Int. J. Pharm. 73: 75-80 (1991) [119] Ilkka, J., Paronen, P.

Prediction of the compression behaviour of powder mixtures by the Heckel equation.

Int. J. Pharm. 94: 181-187 (1993) [120] Kochhar, S.K., Rubinstein, M.H., Barnes, D.

Slugging and recompression characterisation of some blends of pharmaceutical excipients.

Int. J. Pharm. 112: 225-231 (1994)

–  –  –

[122] Malamataris, S., Rees, J.E.

Viscoelastic properties of some pharmaceutical powders compared using creep compliance, extended Heckel analysis and tablet strength measurements.

Int. J. Pharm. 92: 123-135 (1993) [123] Sun, C., Grant, D.J.W.

Influence of elastic deformation of particles on Heckel analysis.

Pharm. Dev. Technol. 6: 193-200 (2001) [124] Garr, J.S.M., Rubinstein, M.H.

An investigation into the capping of paracetamol at increasing speeds of compression.

Int. J. Pharm. 72: 117-122 (1991) [125] Paronen, P.

Heckel plots as indicators of elastic properties of pharmaceuticals.

Drug Dev. Ind. Pharm. 12: 1903-1912 (1986) [126] Vromans, H., Lerk, C.F.

Densification properties and compactibility of mixtures of pharmaceutical excipients with and without magnesium stearate.

Int. J. Pharm. 46: 183-192 (1988) [127] Zuurman, K., Maarschalk, K.V., Bolhuis, G.K.

Effect of magnesium stearate on bonding and porosity expansion of tablets produced from materials with different consolidation properties.

Int. J. Pharm. 179: 107-115 (1999)

–  –  –

[129] Tomas, J., Kleinschmidt, S.

Improvement of flowability of fine cohesive powders by flow additives.

Chem. Eng. Technol. 32: 1470-1483 (2009) [130] Augsburger, L.L., Shangraw, R.F.

Effect of glidants in tableting.

J. Pharm. Sci. 55: 418-423 (1966) [131] Gold, G., Duvall, R.N., Palermo, B.T., Slater, J.G.

Powder flow studies. II. Effect of glidants on flow rate and angle of repose.

J. Pharm. Sci. 55: 1291-1295 (1966) [132] Fricke, J., Tillotson, T.

Aerogels: Production, characterization, and applications.

Thin Solid Films 297: 212-223 (1997) [133] Gupta, M.K., Vanwert, A., Bogner, R.H.

Formation of physically stable amorphous drugs by milling with Neusilin.

J. Pharm. Sci. 92: 536-551 (2003) [134] Bahl, D., Hudak, J., Bogner, R.H.

Comparison of the ability of various pharmaceutical silicates to amorphize and enhance dissolution of indomethacin upon co-grinding.

Pharm. Dev. Technol. 13: 255-269 (2008)

–  –  –

[136] Gupta, M.K., Bogner, R.H., Goldman, D., Tseng, Y.C.

Mechanism for further enhancement in drug dissolution from solid-dispersion granules upon storage.

Pharm. Dev. Technol. 7: 103-112 (2002) [137] Gupta, M.K., Tseng, Y.C., Goldman, D., Bogner, R.H.

Hydrogen bonding with adsorbent during storage governs drug dissolution from solid-dispersion granules.

Pharm. Res. 19: 1663-1672 (2002) [138] Hentzschel, C.M., Alnaief, M., Smirnova, I., Sakmann, A., Leopold, C.S.

Enhancement of griseofulvin release from hydrophilic aerogel formulations and liquisolid compacts.

Eur. J. Pharm. Biopharm., submitted (2010) [139] Ito, Y., Arai, H., Uchino, K., Iwasaki, K., Shibata, N., Takada, K.

Effect of adsorbents on the absorption of lansoprazole with surfactant.

Int. J. Pharm. 289: 69-77 (2005) [140] Ito, Y., Kusawake, T., Prasad, Y.V.R., Sugioka, N., Shibata, N., Takada, K.

Preparation and evaluation of oral solid heparin using emulsifier and adsorbent for in vitro and in vivo studies.

Int. J. Pharm. 317: 114-119 (2006) [141] Sander, C., Holm, P.

Porous magnesium aluminometasilicate tablets as carrier of a cyclosporine selfemulsifying formulation.

AAPS PharmSciTech 10: 1388-1395 (2009)

–  –  –

[143] Alnaief, M., Smirnova, I.

Effect of surface functionalization of silica aerogel on their adsorptive and release properties.

J. Non-Cryst. Solids 356: 1644-1649 (2010) [144] Alnaief, M., Smirnova, I.

In situ production of spherical aerogel microparticles.

J. Supercrit. Fluids 55: 1118-1123 (2011) [145] Luangtana-Anan, M., Fell, J.T.

Bonding mechanisms in tabletting.

Int. J. Pharm. 60: 197-202 (1990) [146] Wray, P.E.

The physics of tablet compaction revisited.

Drug Dev. Ind. Pharm. 18: 627-658 (1992) [147] Loebenberg, R., Amidon, G.L.

Modern bioavailability, bioequivalence and biopharmaceutics classification system. New scientific approaches to international regulatory standards.

Eur. J. Pharm. Biopharm. 50: 3-12 (2000) [148] Lerk, C.F., Bolhuis, G.K., Deboer, A.H.

Effect of microcrystalline cellulose on liquid penetration in and disintegration of directly compressed tablets.

J. Pharm. Sci. 68: 205-211 (1979) [149] Lipinski, C.A.

Drug-like properties and the causes of poor solubility and poor permeability.

J. Pharmacol. Toxicol. Methods 44: 235-249 (2000)

–  –  –

[151] Gonnissen, Y., Remon, J.P., Vervaet, C.

Effect of maltodextrin and superdisintegrant in directly compressible powder mixtures prepared via co-spray drying.

Eur. J. Pharm. Biopharm. 68: 277-282 (2008) Appendix 113

–  –  –

Conference Hentzschel, C.M., Sakmann, A., Leopold, C.S.

contributions – Influence of liquid drug content on the flow properties of liquisolid oral presentations powder blends.

Annual meeting of the DPhG, Bonn, Germany (2008)

–  –  –

Conference Hentzschel, C.M., Saniocki, I., Sakmann, A., Leopold, C.S.

contributions – Particle size, surface area and flowability of novel tableting poster presentations excipients.

XIV. Workshop Porotec, Bad Soden, Germany (2008)

–  –  –

Conference Hentzschel, C.M., Sakmann, A., Leopold, C.S.

contributions – Suitability of various tableting excipients as carriers for liquisolid poster presentations systems.

7th World Meeting on Pharmaceutics, Biopharmaceutics and Pharmaceutical Technology, Malta (2010)

–  –  –

Eidesstattliche Versicherung Hiermit versichere ich an Eides statt, die vorliegende Arbeit selbstständig und ohne fremde Hilfe sowie nur mit den angegebenen Hilfsmitteln und Quellen erstellt zu haben. Ich versichere zudem, keinen weiteren Promotionsversuch an einer anderen Einrichtung unternommen zu haben.

Hamburg, den __________________________

Christina M. Hentzschel



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