Solubilisierung stark lipophiler Arzneistoffe in lipidhaltige ...

Solubilisierung stark lipophiler Arzneistoffe in lipidhaltige ... Solubilisierung stark lipophiler Arzneistoffe in lipidhaltige ...

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Literaturverzeichnis 63. Larhed, A. W., The Mucus Layer and Other Barriers to Intestinal Drug Absorption, Diss., Faculty of Pharmacy, Uppsala, Sweden, Almqvist & Wiksell International, Stockholm, Sweden, (1997). 64. Mizuno, M., Yoshida, M., Hashida, M., Kimura, T., und Sezaki, H., Effect of mucosal lipid components on the membrane permeation of water -soluble drugs, Chem. Pharm. Bull. 33 (1985) 2932-2940. 65. Behrens, I., Stenberg, P., Artursson, P., und Kissel, T., The effect of mucus on the transepithelial transport of lipophilic drugs in a mucus-producing cell line HT29-MTX, Proc. Int. Symp. Controlled Release Bioact. Mater. 27 th (2000) 1218-1219. 66. MacAdam, A., The effect of gastro-intestinal mucus on drug absorption, Adv. Drug Deliv. Rev. 11 (1993) 201-220. 67. Nimmerfall, F. und Rosenthaler, J., Significance of the goblet-cell mucin layer, the outermost luminal barrier to passage through the gut wall, Biochem. Biophys Res. Commun. 94 (1980) 960-966. 68. Smithson, K. W., Millar, D. B., Jacobs, L. R., und Gray, G. M., Intestinal diffusion barrier: unstirred water layer or membrane surface mucous coat?, Science 214 (1981) 1241-1244. 69. Behrens, I., Stenberg, P., Artursson, P., und Kissel, T., Transport of lipophilic drug molecules in a new mucus-secreting cell culture model based on HT29-MTX cells, Pharm. Res. 18 (2001) 1138- 1145. 70. Jackson, M. J., Drug transport across gastrointestinal epithelia, In: Johnson, L. R. [Hrsg.], Physiology of the gastrointestinal tract (2 nd Edn.), Raven Press, NY, USA, (1987), S. 1795-1621. 71. Hidalgo, I. J., Hillgren, K. M., Grass, G. M., und Borchardt, R. T., Characterization of the unstirred water layer in Caco-2 cell monolayers using a novel diffusion apparatus, Pharm. Res. 8 (1991) 222-227. 72. Larhed, A. W., Artursson, P., und Bjork, E., The influence of intestinal mucus components on the diffusion of drugs., Pharm. Res. 15 (1998) 66-71. 73. LaMont, J. T., Mucus: the front line of intestinal mucosal defense, Ann. N. Y. Acad. Sci. 664 (1992) 190-201. 74. Bhat, P. G., Flanagan, D. R., und Donovan, M. D., The limiting role of mucus in drug absorption: Drug permeation through mucus solution, Int. J. Pharm. 126 (1995) 179. 75. Mantle, M. und Thakore, E., Rabbit intestinal and colonic mucins: isolation, partial characterization, and measurement of secretion using an enzyme-linked immunoassay, Biochem. Cell Biol. 66 (1988) 1045-1054. 76. Champe, P. C. und Harvey, R. A., Biochemistry, (2 nd Edn.), Lippincott, Philadelphia, PA, USA, (1994), S. 157-162. 77. Wiedmann, T. S., Herrington, H., Deye, C., und Kallick, D., Distribution and diffusion of sodium taurocholate and egg phosphatidylcholine aggregates in rat intestinal mucin, Pharm. Res. 18 (2001) 1489-1496. 78. Lee, S. P. und Nicholls, J. F., Diffusion of charged ions in mucus gel: effect of net charge, Biorheology 24 (1987) 565-569. 79. Karlsson, J., Wikman, A., und Artursson, P., The mucus layer as a barrier to drug absorption in monolayers of human intestinal epithelial HT29-H goblet cells, Int. J. Pharm. 99 (1993) 209-218. 80. Jastrow, H., Glykokalix, Elektronenmikroskopischer Atlas im Internet, (2004), http://www.unimainz.de/FB/Medizin/Anatomie/workshop/EM/EMGlykokalix.html. 81. Nuhn, P., Transport proteins as drug targets. Biochemical principles of membrane transport, Pharm. Ztg. 144 (1999) 541-544. 82. Tsuji, A. und Tamai, I., Carrier-mediated intestinal transport of drugs, Pharm. Res. 13 (1996) 963- 977. 83. Wacher, V. J., Wu, C. Y., und Benet, L. Z., Overlapping substrate specificities and tissue distribution of cytochrome P450 3A and P-glycoprotein: implications for drug delivery and activity in cancer chemotherapy, Mol. Carcinog. 13 (1995) 129-134. cxii

Literaturverzeichnis 84. Wacher, V. J., Salphati, L., und Benet, L. Z., Active secretion and enterocytic drug metabolism barriers to drug absorption, Adv. Drug Deliv. Rev. 46 (2001) 89-102. 85. Benet, L. Z., Izumi, T., Zhang, Y., Silverman, J. A., und Wacher, V. J., Intestinal MDR transport proteins and P-450 enzymes as barriers to oral drug delivery, J. Contr. Release 62 (1999) 25-31. 86. Suzuki, H. und Sugiyama, Y., Role of metabolic enzymes and efflux transporters in the absorption of drugs from the small intestine, Eur. J. Pharm. Sci. 12 (2000) 3-12. 87. Bretschneider, B., Brandsch, M., und Neubert, R., Intestinal transport of beta-lactam antibiotics: analysis of the affinity at the H+/peptide symporter (PEPT1), the uptake into Caco-2 cell monolayers and the transepithelial flux, Pharm. Res. 16 (1999) 55-61. 88. Peters, W. H., Allebes, W. A., Jansen, P. L., Poels, L. G., und Capel, P. J., Characterization and tissue specificity of a monoclonal antibody against human uridine 5'-diphosphate-glucuronosyltransferase, Gastroenterology 93 (1987) 162-169. 89. Wynalda, M. A., Hutzler, J. M., Koets, M. D., Podoll, T., und Wienkers, L. C., In vitro metabolism of clindamycin in human liver and intestinal microsomes, Drug Metab. Dispos. 31 (2003) 878- 887. 90. Obach, R. S., Zhang, Q. Y., Dunbar, D., und Kaminsky, L. S., Metabolic characterization of the major human small intestinal cytochrome p450s, Drug Metab. Dispos. 29 (2001) 347-352. 91. Emoto, C., Yamazaki, H., Iketaki, H., Yamasaki, S., Satoh, T., Shimizu, R., Suzuki, S., Shimada, N., Nakajima, M., und Yokoi, T., Cooperativity of alpha-naphthoflavone in cytochrome P450 3Adependent drug oxidation activities in hepatic and intestinal microsomes from mouse and human, Xenobiotica 31 (2001) 265-275. 92. Yamamoto, T., Hagima, N., Nakamura, M., Kohno, Y., Nagata, K., und Yamazoe, Y., Differences in cytochrome P450 forms involved in the metabolism of N,N-dipropyl-2-[4-methoxy-3-(2phenylethoxy)phenyl]ethylamine monohydrochloride (NE-100), a novel sigma ligand, in human liver and intestine, Drug Metab. Dispos. 31 (2003) 60-66. 93. Chiba, M., Hensleigh, M., und Lin, J. H., Hepatic and intestinal metabolism of indinavir, an HIV protease inhibitor, in rat and human microsomes. Major role of CYP3A, Biochem. Pharmacol. 53 (1997) 1187-1195. 94. Johnson, T. N., Tanner, M. S., Taylor, C. J., und Tucker, G. T., Enterocytic CYP3A4 in a paediatric population: developmental changes and the effect of coeliac disease and cystic fibrosis, Br. J. Clin. Pharmacol. 51 (2001) 451-460. 95. Ungell, A.-L., Ex vivo models for studying intestinal transport. A lecture in the 4 th International Intensive Course and Workshop on Cell Culture and in-vitro Models for Drug Absorption and Delivery (20 Feb.-1 Mar./2002), Universität Saarland, Saarbrücken, DE, (unveröffentlichte Arbeit). 96. Takemoto, K., Yamazaki, H., Tanaka, Y., Nakajima, M., und Yokoi, T., Catalytic activities of cytochrome P450 enzymes and UDP-glucuronosyltransferases involved in drug metabolism in rat everted sacs and intestinal microsomes, Xenobiotica 33 (2003) 43-55. 97. Wortelboer, H. M., van der Linden, E. C., De Kruif, C. A., Noordhoek, J., Blaauboer, B. J., van Bladeren, P. J., und Falke, H. E., Effects of indole-3-carbinol on biotransformation enzymes in the rat: in vivo changes in liver and small intestinal mucosa in comparison with primary hepatocyte cultures, Food Chem. Toxicol. 30 (1992) 589-599. 98. Milewich, L., MacDonald, P. C., und Carr, B. R., Activity of 17 beta-hydroxysteroid oxidoreductase in tissues of the human fetus, J. Endocrinol. 123 (1989) 509-518. 99. Farthing, M. J., Vinson, G. P., Edwards, C. R., und Dawson, A. M., 17 beta-Hydroxysteroid dehydrogenase activity in the mucosa of rat and human small intestine, J. Steroid Biochem. 14 (1981) 1107-1113. 100. Sano, T., Hirasawa, G., Takeyama, J., Darnel, A. D., Suzuki, T., Moriya, T., Kato, K., Sekine, H., Ohara, S., Shimosegawa, T., Nakamura, J., Yoshihama, M., Harada, N., und Sasano, H., 17 beta- Hydroxysteroid dehydrogenase type 2 expression and enzyme activity in the human gastrointestinal tract, Clin. Sci. (Lond) 101 (2001) 485-491. cxiii

Literaturverzeichnis<br />

63. Larhed, A. W., The Mucus Layer and Other Barriers to Intest<strong>in</strong>al Drug Absorption, Diss., Faculty<br />

of Pharmacy, Uppsala, Sweden, Almqvist & Wiksell International, Stockholm, Sweden, (1997).<br />

64. Mizuno, M., Yoshida, M., Hashida, M., Kimura, T., und Sezaki, H., Effect of mucosal lipid<br />

components on the membrane permeation of water -soluble drugs, Chem. Pharm. Bull. 33<br />

(1985) 2932-2940.<br />

65. Behrens, I., Stenberg, P., Artursson, P., und Kissel, T., The effect of mucus on the transepithelial<br />

transport of lipophilic drugs <strong>in</strong> a mucus-produc<strong>in</strong>g cell l<strong>in</strong>e HT29-MTX, Proc. Int. Symp.<br />

Controlled Release Bioact. Mater. 27 th (2000) 1218-1219.<br />

66. MacAdam, A., The effect of gastro-<strong>in</strong>test<strong>in</strong>al mucus on drug absorption, Adv. Drug Deliv. Rev. 11<br />

(1993) 201-220.<br />

67. Nimmerfall, F. und Rosenthaler, J., Significance of the goblet-cell muc<strong>in</strong> layer, the outermost<br />

lum<strong>in</strong>al barrier to passage through the gut wall, Biochem. Biophys Res. Commun. 94 (1980)<br />

960-966.<br />

68. Smithson, K. W., Millar, D. B., Jacobs, L. R., und Gray, G. M., Intest<strong>in</strong>al diffusion barrier: unstirred<br />

water layer or membrane surface mucous coat?, Science 214 (1981) 1241-1244.<br />

69. Behrens, I., Stenberg, P., Artursson, P., und Kissel, T., Transport of lipophilic drug molecules <strong>in</strong> a<br />

new mucus-secret<strong>in</strong>g cell culture model based on HT29-MTX cells, Pharm. Res. 18 (2001) 1138-<br />

1145.<br />

70. Jackson, M. J., Drug transport across gastro<strong>in</strong>test<strong>in</strong>al epithelia, In: Johnson, L. R. [Hrsg.],<br />

Physiology of the gastro<strong>in</strong>test<strong>in</strong>al tract (2 nd Edn.), Raven Press, NY, USA, (1987), S. 1795-1621.<br />

71. Hidalgo, I. J., Hillgren, K. M., Grass, G. M., und Borchardt, R. T., Characterization of the unstirred<br />

water layer <strong>in</strong> Caco-2 cell monolayers us<strong>in</strong>g a novel diffusion apparatus, Pharm. Res. 8 (1991)<br />

222-227.<br />

72. Larhed, A. W., Artursson, P., und Bjork, E., The <strong>in</strong>fluence of <strong>in</strong>test<strong>in</strong>al mucus components on the<br />

diffusion of drugs., Pharm. Res. 15 (1998) 66-71.<br />

73. LaMont, J. T., Mucus: the front l<strong>in</strong>e of <strong>in</strong>test<strong>in</strong>al mucosal defense, Ann. N. Y. Acad. Sci. 664<br />

(1992) 190-201.<br />

74. Bhat, P. G., Flanagan, D. R., und Donovan, M. D., The limit<strong>in</strong>g role of mucus <strong>in</strong> drug absorption:<br />

Drug permeation through mucus solution, Int. J. Pharm. 126 (1995) 179.<br />

75. Mantle, M. und Thakore, E., Rabbit <strong>in</strong>test<strong>in</strong>al and colonic muc<strong>in</strong>s: isolation, partial<br />

characterization, and measurement of secretion us<strong>in</strong>g an enzyme-l<strong>in</strong>ked immunoassay, Biochem.<br />

Cell Biol. 66 (1988) 1045-1054.<br />

76. Champe, P. C. und Harvey, R. A., Biochemistry, (2 nd Edn.), Lipp<strong>in</strong>cott, Philadelphia, PA, USA,<br />

(1994), S. 157-162.<br />

77. Wiedmann, T. S., Herr<strong>in</strong>gton, H., Deye, C., und Kallick, D., Distribution and diffusion of sodium<br />

taurocholate and egg phosphatidylchol<strong>in</strong>e aggregates <strong>in</strong> rat <strong>in</strong>test<strong>in</strong>al muc<strong>in</strong>, Pharm. Res. 18<br />

(2001) 1489-1496.<br />

78. Lee, S. P. und Nicholls, J. F., Diffusion of charged ions <strong>in</strong> mucus gel: effect of net charge,<br />

Biorheology 24 (1987) 565-569.<br />

79. Karlsson, J., Wikman, A., und Artursson, P., The mucus layer as a barrier to drug absorption <strong>in</strong><br />

monolayers of human <strong>in</strong>test<strong>in</strong>al epithelial HT29-H goblet cells, Int. J. Pharm. 99 (1993) 209-218.<br />

80. Jastrow, H., Glykokalix, Elektronenmikroskopischer Atlas im Internet, (2004), http://www.unima<strong>in</strong>z.de/FB/Mediz<strong>in</strong>/Anatomie/workshop/EM/EMGlykokalix.html.<br />

81. Nuhn, P., Transport prote<strong>in</strong>s as drug targets. Biochemical pr<strong>in</strong>ciples of membrane transport,<br />

Pharm. Ztg. 144 (1999) 541-544.<br />

82. Tsuji, A. und Tamai, I., Carrier-mediated <strong>in</strong>test<strong>in</strong>al transport of drugs, Pharm. Res. 13 (1996) 963-<br />

977.<br />

83. Wacher, V. J., Wu, C. Y., und Benet, L. Z., Overlapp<strong>in</strong>g substrate specificities and tissue<br />

distribution of cytochrome P450 3A and P-glycoprote<strong>in</strong>: implications for drug delivery and activity<br />

<strong>in</strong> cancer chemotherapy, Mol. Carc<strong>in</strong>og. 13 (1995) 129-134.<br />

cxii

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