Gastrointestinal anatomy, physiology and permeation pathways

Enhancement in Drug Delivery

Volumn , Issue , 2006, Pages 3-35

  Rubinstein, Abraham ^a  

^a HEBREW UNIVERSITY OF JERUSALEM   (Israel)

Author keywords

[No Author keywords available]

Indexed keywords

EID: 77949414034     PISSN: None     EISSN: None     Source Type: Book    
DOI: None     Document Type: Chapter

References (197)

1. Gold, H., et al. 1953. Clinical pharmacology of digoxin. J Pharmacol Exp Ther 109:45.
2. Wagner, J.G. 1981. History of pharmacokinetics. Pharmacol Ther 12:537.
3. Lee, P.I. 2001. Design and power of a population pharmacokinetic study. Pharm Res 18:75.
4. Ma, J.D., A.N. Nafziger, and J.S. Bertino, Jr. 2004. Genetic polymorphisms of cytochrome P450 enzymes and the effect on interindividual, pharmacokinetic variability in extensive metabolizers. J Clin Pharmacol 44:447.
5. Wacher, V.J., L. Salphati, and L.Z. Benet. 1996. Active secretion and enterocytic drug metabolism barriers to drug absorption. Adv Drug Deliv Rev 20:99.
6. Ekins, S., et al. 2000. Progress in predicting human ADME parameters in silico. J Pharmacol Toxicol Methods 44:251.
7. Balimane, P.V., and S. Chong. 2005. Cell culture-based models for intestinal permeability: A critique. Drug Discov Today 10:335.
8. Stainier, D.Y.R. 2005. No organ left behind: Tales of gut development and evolution. Science 307:1902.
9. Khanvilkar, K., M.D. Donovan, and D.R. Flanagan. 2001. Drug transfer through mucus. Adv Drug Deliv Rev 48:173.
10. Schubert, M.L. 2004. Gastric secretion. Curr Opin Gastroenterol 20:519.
11. Engel, E., P.H. Guth, Y. Nishizaki, and J.D. Kaunitz. 1995. Barrier function of the gastric mucus gel. Am J Physiol 269:G994.
12. Nimmerfall, F., and J. Rosenthaler. 1980. Significance of the goblet-cell mucin layer, the outermost luminal barrier to passage through the gut wall. Biochem Biophys Res Commun 94:960.
13. Johnson, L.R. 2001. Gastrointestinal physiology, 6th ed. St. Louis: Mosby.
14. Rendleman, D.F., et al. 1958. Reflux pressure studies on the ileocecal valve of dogs and humans. Surgery 44:640.
15. Phillips, S.F., J.H. Pemberton, and R.G. Shorter. 1991. The large intestine: Physiology, pathophysiology and disease. New York: Raven Press.
16. Cherbut, C., A.C. Aube, H.M. Blottiere, and J.P. Galmiche. 1997. Effects of short-chain fatty acids on gastrointestinal motility. Scand J Gastroenterol Suppl 222:58.
17. Read, N.W., A. McFarlane, R.I. Kinsman, and S.R. Bloom. 1984. The ileal brake: A potent mechanism for feedback control of gastric emptying and small bowel transit. In Gastrointestinal motility, ed. C. Roman, 335. Lancaster: MTP Press.
18. Bieck, P.R. 1993. Colonic drug absorption and metabolism. New York: Marcel Dekker.
19. Kurz, H. 1975. Principles of drug absorption. In Pharmacology of intestinal absorption: Gastrointestinal absorption of drugs, eds. W. Forth and W. Rummel, 245. Oxford: Pergamon Press.
20. Neutra, M.R., and J.F. Forstner. 1987. Gastrointestinal mucus: Synthesis, secretion, and function. In Physiology of the gastrointestinal tract, 2nd ed., ed. R.L. Johnson, 975. New York: Raven Press.
21. Sarna, S.K. 1991. Physiology and pathophysiology of colonic motor activity (1). Dig Dis Sci 36:827.
22. Scheline, R.R. 1973. Metabolism of foreign compounds by gastrointestinal microorganisms. Pharmacol Rev 25:451.
23. Chadwick, R.W., S.E. George, and L.D. Claxton. 1992. The role of the gastrointestinal mucosa and microflora in the bioactivation of dietary and environmental mutagens or carcinogens. Drug Metab Rev 24:425.
24. Sintov, A., M. Simberg, and A. Rubinstein. 1996. Absorption enhancement of captopril in the rat colon as a putative method for captopril delivery by extended release formulations. Int J Pharm 143:101.
25. Kim, J.S., et al. 1994. Absorption of ACE inhibitors from small intestine and colon. J Pharm Sci 83:1350.
26. Fetih, G., et al. 2005. Improvement of absorption enhancing effects of n-dodecyl-beta-D-maltopyranoside by its colon-specific delivery using chitosan capsules. Int J Pharm 293:127.
27. Sutton, S.C., E.L. LeCluyse, L. Cammack, and J.A. Fix. 1992. Enhanced bioavailability of cefoxitin using palmitoyl L-carnitine. I. Enhancer activity in different intestinal regions. Pharm Res 9:191.
28. de Boer, A.G., E.J. van Hoogdalem, and D.D. Breimer. 1992. Rate-controlled rectal peptide drug absorption enhancement. Adv Drug Deliv Rev 8:237.
29. Yoshikawa, H., S. Muranishi, and H. Sezakai. 1983. Mechanisms of selective transfer of bleomycin into lymphatics by a bifunctional delivery system via the lumen of the large intestine. Int J Pharm 13:321.
30. Hauss, D.J., H.Y. Ando, D.M. Grasela, and E.T. Sugita. 1991. The relationship of salicylate lipophilicity to rectal insulin absorption enhancement and relative lymphatic uptake. J Pharmacobiodyn 14:139.
31. Touitou, E., and M. Donbrow. 1983. Promoted rectal absorption of insulin: Formulative parameters involved in the absorption from hydrophilic bases. Int J Pharm 15:13.
32. Lindmark, T., et al. 1997. Mechanism of absorption enhancement in humans after rectal administration of ampicillin in suppositories containing sodium caprate. Pharm Res 14:930.
33. Noach, A.B., M.C. Blom-Roosemalen, A.G. de Boer, and D.D. Breimer. 1995. Absorption enhancement of a hydrophilic model compound by verapamil after rectal administration to rats. J Pharm Pharmacol 47:466.
34. Mathias, J.R., and C.A. Sninsky. 1985. Motility of the small intestine: A look ahead. Am J Physiol 248:G495.
35. Macheras, P., C. Reppas, and J.B. Dressman. 1995. Physiological factors related to drug absorption. In Biopharmaceutics of orally administered drugs. London: Ellis Horwood.
36. Kumar, D., and D. Wingate. 1993. An illustrated guide to gastrointestinal motility, 2nd ed. Edinburgh: Churchill Livingstone.
37. Code, C.F., and J.A. Marlett. 1975. The interdigestive myo-electric complex of the stomach and small bowel of dogs. J Physiol 246:289.
38. Sarna, S.K. 1985. Cyclic motor activity: Migrating motor complex. Gastroenterology 89:894.
39. Schemann, M., and H.J. Ehrlein. 1986. Mechanical characteristics of phase II and phase III of the interdigestive migrating motor complex in dogs. Gastroenterology 91:117.
40. Rubinstein, A., H.K.V. Kin Li, P. Gruber, and J.R. Robinson. 1988. Gastrointestinal physiological variables affecting the performance of oral sustained release dosage forms. In Oral sustained release formulations, design and evaluation, eds. A. Yacobi and E. Halperin-Walega, 125. New York: Pergamon Press.
41. Hunt, J.N., and I. MacDonald. 1954. The influence of volume on gastric emptying. J Physiol (Lond) 126:459.
42. Hunt, J.N. 1959. Gastric emptying and secretion in man. Physiol Rev 39:491.
43. Keinke, O., M. Schemann, and H.J. Ehrlein. 1984. Mechanical factors regulating gastric emptying of viscous nutrient meals in dogs. J Exp Physiol 69:781.
44. Hunt, J.N. 1984. Regulation of gastric emptying by neurohumoral factors and by gastric and duodenal receptors. In Esophageal and gastric emptying, eds. A. Dubois and D.O. Castell, 65. Boca Raton: CRC Press.
45. Hunt, J.N. 1980. A possible relation between the regulation of gastric emptying and food intake. Am J Physiol 239:G1.
46. Meyer, J.H., J. Dressman, A. Fink, and G. Amidon. 1985. Effect of size and density on canine gastric emptying of nondigestible solids. Gastroenterology 89:805.
47. Khosla, R., and S.S. Davis. 1990. The effect of tablet size on the gastric emptying of nondisintegrating tablets. Int J Pharm 62:R9.
48. Coupe, A.J., S.S. Davis, D.F. Evans, and I.R. Wilsing. 1993. Do pellets empty from the stomach with food? Int J Pharm 92:167.
49. Timmermans, J., and A.J. Moes. 1993. The cutoff size for gastric emptying of dosage forms. J Pharm Sci 82:854.
50. Smith, J.L., C.L. Jiang, and J.N. Hunt. 1984. Intrinsic emptying pattern of the human stomach. Am J Physiol 246:R959.
51. Minami, H., and R.W. McCallum. 1984. The physiology and pathophysiology of gastric emptying in humans. Gastroenterology 86:1592.
52. Kraus, L.C., and J.N. Fell. 1984. Effect of stress on the gastric emptying of capsules. J Clin Hosp Pharm 9:249.
53. Nimmo, W.S., and F. Prescott. 1978. The influence of posture on paracetamol absorption. Br J Clin Pharmacol 5:348.
54. Renwick, A.G., et al. 1992. The influence of posture on the pharmacokinetics of orally administered nifedipine. Br J Clin Pharmacol 34:332.
55. Backon, J., and A. Hoffman. 1991. The lateral decubitus position may affect gastric emptying through an autonomic mechanism: The skin pressure-vegetative reflex. Br J Clin Pharmacol 32:138.
56. Gupta, P., and J.R. Robinson. 1988. Gastric emptying of liquids in the fasted dog. Int J Pharm 43:45.
57. Thompson, D.G., et al. 1980. Normal patterns of human upper small bowel motor activity recorded by prolonged radiotelemetry. Gut 21:500.
58. Park, H.M., et al. 1984. Gastric emptying of enteric-coated tablets. Dig Dis Sci 29:207.
59. Gruber, P., et al. 1987. Gastric emptying of nondigestible solids in the fasted dog. J Pharm Sci 76:117.
60. Graham, D.Y., J.L. Smith, and A.A. Bouvet. 1990. What happens to tablets and capsules in the stomach: Endoscopic comparison of disintegration and dispersion characteristics of two microencapsulated potassium formulations. J Pharm Sci 79:420.
61. Tirosh, B., and A. Rubinstein. 1998. Migration of adhesive and non-adhesive particles in the rat intestine under altered mucus secretion conditions. J Pharm Sci 87:453.
62. Barr, W.H., et al. 1994. Different absorption of amoxicillin from the human small and large intestine. Clin Pharmacol Ther 56:279.
63. Davis, S.S., J.G. Hardy, and J.W. Fara. 1986. Transit of pharmaceutical dosage forms through the small intestine. Gut 27:886.
64. Davis, S.S., et al. 1986. Gastrointestinal transit of controlled release naproxen tablet formulation. Int J Pharm 32:85.
65. Adkin, D.A., et al. 1995. The effect of pharmaceutical excipients on small intestinal transit. Br J Clin Pharmacol 39:381.
66. Adkin, D.A., et al. 1995. The effect of different concentrations of mannitol in solution on small intestinal transit: Implications for drug absorption. Pharm Res 12:393.
67. Adkin, D.A., et al. 1995. The effect of mannitol on the oral bioavailability of cimetidine. J Pharm Sci 84:1405.
68. Hardy, J.G., C.G. Wilson, and E. Wood. 1985. Drug delivery to the proximal colon. J Pharm Pharmacol 37:874.
69. Debongnie, J.C., and S.F. Phillips. 1978. Capacity of the human colon to absorb fluid. Gastroenterology 74:698.
70. Levinson, S., et al. 1985. Comparison of intraluminal and intravenous mediators of colonic response to eating. Dig Dis Sci 30:33.
71. Snap, W.J.J., S.A. Matarazzo, and S. Cohen. 1978. Effect of eating and gastrointestinal hormones on human colonic myoelectrical and motor activity. Gastroenterology 75:373.
72. Wiley, J.N., D. Tatum, R. Keinath, and C. Owyang. 1988. Participation of gastric mechanoreceptors and intestinal chemoreceptors in the gastrocolonic response. Gastroenterology 94:1144.
73. Wright, S.H., et al. 1980. Effect of dietary components on gastrocolonic response. Am J Physiol 238:G228.
74. Sarna, S.K. 1991. Physiology and pathophysiology of colonic motor activity (2). Dig Dis Sci 36:998.
75. Adkin, D.A., S.S. Davis, R.A. Sparrow, and I.R. Wilding. 1993. Colonic transit of different sized tablets in healthy subjects. J Contr Rel 23:147.
76. Proano, M., et al. 1991. Unprepared human colon does not discriminate between solids and liquids. Am J Physiol 260:G13.
77. Eckburg, P.B., et al. 2005. Diversity of the human intestinal microbial flora. Science 308:1635.
78. Simon, G.L., and S.L. Gorbach. 1984. Intestinal flora in health and disease. Gastroenterology 86:174.
79. Salyers, A.A. 1984. Bacteroides of the human lower intestinal tract. Ann Rev Microbiol 38:293.
80. Macfarlane, G.T., and J.H. Cummings. 1991. The colonic flora, fermentation, and large bowel digestive function. In The large intestine: Physiology, pathophysiology, and disease, eds. S.F. Phillips, J.H. Pemberton, and R.G. Shorter, 51. New York: Raven Press.
81. Cummings, J.H. 1984. Microbial digestion of complex carbohydrates in man. Proc Nutr Soc 43:35.
82. Werch, S.C., and A.C. Ivy. 1941. On the fate of ingested pectin. Am J Digest Dis 8:101.
83. Dressman, J.B., et al. 1990. Upper gastrointestinal (GI) pH in young, healthy men and women. Pharm Res 7:756.
84. Russell, T.L., et al. 1993. Upper gastrointestinal pH in seventy-nine healthy, elderly, North American men and women. Pharm Res 10:187.
85. Evans, D.F., et al. 1988. Measurement of gastrointestinal pH profiles in normal ambulant human subjects. Gut 29:1035.
86. Evans, D.F., et al. 1986. Gastrointestinal pH profiles in man. Gastroenterology 90:1410.
87. Allen, A., and G. Flemstrom. 2005. Gastroduodenal mucus bicarbonate barrier: Protection against acid and pepsin. Am J Physiol Cell Physiol 288:C1.
88. Sherman, P., et al. 1987. Bacteria and the mucus blanket in experimental small bowel bacterial overgrowth. Am J Pathol 126:527.
89. Lamont, J.T. 1992. Mucus: The front line of intestinal mucosal defense. In Neuro-immuno physiology of the gastrointestinal mucosa, implications for inflammatory diseases, eds. R.H. Stead, M.H. Perdue, H. Cook, D.W. Powel, and K.E. Barrett, 190. New York: New York Academy of Sciences.
90. Lehr, C.M., F.G.P. Poelma, H.E. Junginger, and J.J. Tukker. 1991. An estimate of turnover time of intestinal mucus gel layer in the rat in situ loop. Int J Pharm 70:235.
91. Wilson, F.A., V.L. Sallee, and J.M. Dietschy. 1971. Unstirred water layers in intestine: Rate determination of fatty acid absorption from micellar solutions. Science 174:1031.
92. Li, C.Y., C.L. Zimmerman, and T.S. Wiedmann. 1996. Diffusivity of bile salt/phospholipid aggregates in mucin. Pharm Res 13:535.
93. Amidon, G.L., J. Kou, R.L. Elliot, and E.N. Lightfoot. 1980. Analysis of models for determining intestinal wall permeabilities. J Pharm Sci 69:1369.
94. Levitt, M.D., et al. 1987. Quantitative assessment of luminal stirring in the perfused small intestine of the rat. Am J Physiol 252:G325.
95. Ito, S. 1969. Structure and function of the glycocalyx. Fed Proc 28:12.
96. Smithson, K.W., and D.B. Millar. 1981. Intestinal diffusion barrier: Unstirred water layer or membrane surface mucous coat? Science 214:1241.
97. Katori, N., N. Aoyagi, and T. Terao. 1995. Estimation of agitation intensity in the GI tract in humans and dogs based on in vitro/in vivo correlation. Pharm Res 12:237.
98. Winne, D., H. Goig, and U. Muller. 1987. Closed rat jejunum segment in situ: Role of pre-epithelial diffusion resistance (unstirred layer) in absorption process and model analysis. Naunyn Schmiedebergs Arch Pharmacol 335:204.
99. Kou, J.H., D. Fleisher, and G.L. Amidon. 1991. Calculation of the aqueous diffusion layer resistance for absorption in a tube: Application to intestinal membrane permeability determination. Pharm Res 8:298.
100. Sinko, P.J., et al. 1996. Analysis of intestinal perfusion data for highly permeable drugs using a numerical aqueous resistance-Nonlinear regression method. Pharm Res 13:570.
101. Bickel, M., and G.L. Kauffman, Jr. 1981. Gastric gel mucus thickness: Effect of distention, 16,16- dimethyl prostaglandin e2, and carbenoxolone. Gastroenterology 80:770.
102. Pullan, R.D., et al. 1994. Thickness of adherent mucus gel on colonic mucosa in humans and its relevance to colitis. Gut 35:353.
103. Ryu, K.H., and E. Grim. 1982. Unstirred water layer in canine jejunum. Am J Physiol 242:G364.
104. Winne, D., and W. Verheyen. 1990. Diffusion coefficient in native mucus gel of rat small intestine. J Pharm Pharmacol 42:517.
105. Flemstrom, G., et al. 1999. Adherent surface mucus gel restricts diffusion of macromolecules in rat duodenum in vivo. Am J Physiol 277:G375.
106. Braybrooks, M.P., B.W. Barry, and E.T. Abbs. 1975. The effect of mucin on the bioavailability of tetracycline from the gastrointestinal tract; in vivo, in vitro correlations. J Pharm Pharmacol 27:508.
107. Barry, B.W., and M.P. Braybrooks. 1975. Proceedings: Influence of a mucin model system upon the bioavailability of phenylbutazone and warfarin sodium from the small intestine. J Pharm Pharmacol 27(Suppl. 2):74P.
108. Nakamura, J., et al. 1978. Role of intestinal mucus in the absorption of quinine and water soluble dyes from rat small intestine. Chem Pharm Bull (Tokyo) 26:857.
109. Flemstrom, G., and E. Kivilaakso. 1983. Demonstration of a pH gradient at the luminal surface of rat duodenum in vivo and its dependence on mucosal alkaline secretion. Gastroenterology 84:787.
110. Shorrock, C.J., and W.D. Rees. 1988. Overview of gastroduodenal mucosal protection. Am J Med 84:25.
111. McEwan, G.T., B. Schousboe, and E. Skadhauge. 1990. Direct measurement of mucosal surface pH of pig jejunum in vivo. Zentralbl Veterinarmed A 37:439.
112. Shiau, Y.F., P. Fernandez, M.J. Jackson, and S. McMonagle. 1985. Mechanisms maintaining a low-pH microclimate in the intestine. Am J Physiol 248:G608.
113. Shiau, Y.F. 1990. Mechanism of intestinal fatty acid uptake in the rat: The role of an acidic microclimate. J Physiol 421:463.
114. Shiau, Y.F., R.J. Kelemen, and M.A. Reed. 1990. Acidic mucin layer facilitates micelle dissociation and fatty acid diffusion. Am J Physiol 259:G671.
115. Phillips, S.F. 1973. Integration of secretory and absorptive function. Mayo Clin Proc 48:630.
116. Crouthamel, W.G., L. Diamond, L.W. Dittert, and J.T. Doluisio. 1975. Drug absorption VII:Influence of mesenteric blood flow on intestinal drug absorption in dogs. J Pharm Sci 64:664.
117. Winne, D. 1980. Influence of blood flow on intestinal absorption of xenobiotics. Pharmacology 21:1.
118. Hober, R., and J. Hober. 1937. Experiments on the absorption of organic solutes in the small intestine of rats. J Cell Comp Physiol 10:401.
119. Schanker, L.S., P.A. Shore, B.B. Brodie, and C.A.M. Hogben. 1957. Absorption of drugs from the stomach I. The rat. J Pharmacol Exp Ther 120:528.
120. Hogben, C.A.M., L.S. Schanker, D.J. Tocco, and B.B. Brodie. 1957. Absorption of drugs from the stomach II. The human. J Pharmacol Exp Ther 120:540.
121. Landay, M.A., and H.E. Schroeder. 1979. Differentiation in normal human buccal mucosa epithelium. J Anat 128:31.
122. Meyer, J., J. Squier, and S.J. Gerson. 1984. The structure and function of oral mucosa. Oxford:Pergamon Press.
123. Kurosaki, Y., and T. Kimura. 2000. Regional variation in oral mucosal drug permeability. Crit Rev Ther Drug Carrier Syst 17:467.
124. Birudaraj, R., R. Mahalingam, X. Li, and B.R. Jasti. 2005. Advances in buccal drug delivery. Crit Rev Ther Drug Carrier Syst 22:295.
125. Ho, N.F.H., C.L. Barsuhn, P.S. Burton, and H.P. Merkle. 1992. Mechanistic insights to buccal delivery of proteinaceous substances. Adv Drug Deliv Rev 8:197.
126. Giannitsis, D.J., G.J. Giakoumakis, K.J. Louisos, and A. Antonopoulos. 1972. Aminopeptidasische eigenschaften der mundschleimhaut beim menschen (Properties of aminopeptidase of human buccal mucosa). Enzymologia 43:143.
127. Harris, D., and J.R. Robinson. 1992. Drug delivery via the mucous membranes of the oral cavity. J Pharm Sci 81:1.
128. Wheater, P.R., et al. 1993. Wheater’s functional histology, a text and colour atlas, 3rd ed. Edinburgh:Churchill Livingstone.
129. Doluisio, J.T., et al. 1970. Drug absorption III: Effect of membrane storage on the kinetics of drug absorption. J Pharm Sci 59:72.
130. Martin, A., P. Bustamante, and A.H.C. Chun. 1993. Physical pharmacy, physical chemical principles in the pharmaceutical sciences, 4th ed. Philadelphia: Lea & Febiger.
131. Comer, J.E.A. 2004. High-throughput measurements of log D and pKa. In Drug bioavailability:Estimation of solubility, permeability, absorption and bioavailability, eds. H. van de Waterbeemd, H. Lennernas, P. Artursson, R. Mannhold, H. Kubinyi, and G. Folkers, 21. Weinheim: Wiley-Verlag.
132. Avdeef, A. 2003. Absorption and drug development, solubility, permeability and charge state. Hoboken, NJ: John Willey.
133. Po, H.N., and N.M. Senozan. 2003. The Henderson-Hasselbalch equation: Its history and limitations. J Chem Ed 78:1499.
134. Perrin, D.D., B. Dempsey, and E.P. Serjeant. 1981. pKa Prediction for organic acid and bases. London: Chapman & Hall.
135. Lodish, H., et al. 2000. Transport across cell membrane. In Molecular cell biology, 4th ed. New York: Freeman & Co.
136. Kellett, G.L. and P.A. Helliwell. 2000. The diffusive component of intestinal glucose absorption is mediated by the glucose-induced recruitment of GLUT2 to the brush-border membrane. Biochem J 350(Pt 1):155.
137. Gross, C.J., L.M. Henderson, and D.A. Savaiano. 1986. Uptake of L-carnitine, D-carnitine and acetyl-L-carnitine by isolated guinea-pig enterocytes. Biochim Biophys Acta 886:425.
138. Hunjan, M.K. and D.F. Evered. 1985. Absorption of glutathione from the gastro-intestinal tract. Biochim Biophys Acta 815:184.
139. Chow, S.L., and D. Hollander. 1978. Arachidonic acid intestinal absorption: Mechanism of transport and influence of luminal factors of absorption in vitro. Lipids 13:768.
140. Crane, R.K. 1965. Na-dependent transport in the intestine and other animal tissues. Fed Proc 24:1000.
141. Thorens, B. 1993. Facilitated glucose transporters in epithelial cells. Ann Rev Physiol 55:591.
142. Tamai, I., et al. 1995. Participation of a proton-cotransporter, MCT1, in the intestinal transport of monocarboxylic acids. Biochem Biophys Res Commun 214:482.
143. Gill, R.K., et al. 2005. Expression and membrane localization of MCT isoforms along the length of the human intestine. Am J Physiol Cell Physiol 289:C846.
144. Walton, J., and T.K. Gray. 1979. Absorption of inorganic phosphate in the human small intestine. Clin Sci (Lond) 56:407.
145. Dudeja, P.K., S.A. Torania, and H.M. Said. 1997. Evidence for the existence of a carrier-mediated folate uptake mechanism in human colonic luminal membranes. Am J Physiol 272:G1408.
146. Rose, R.C., et al. 1986. Transport and metabolism of vitamins. Fed Proc 45:30.
147. Tamai, I., and A. Tsuji. 1996. Carrier-mediated approaches for oral drug delivery. Adv Drug Deliv Rev 20:5.
148. Mizuma, T., et al. 2005. Intestinal SGLT1-mediated absorption and metabolism of benzyl betaglucoside contained in Prunus mume: Carrier-mediated transport increases intestinal availability. Biochim Biophys Acta 1722:218.
149. Hashimoto, T., et al. Improvement of intestinal absorption of peptides: Adsorption of B1-Phe monoglucosylated insulin to rat intestinal brush-border membrane vesicles. Eur J Pharm Biopharm 50:197.
150. Fisher, R.B. 1981. Active transport of salicylate by rat jejunum. Q J Exp Physiol 66:91.
151. Nishimura, N., et al. 2004. Transepithelial permeation of tolbutamide across the human intestinal cell line, Caco-2. Drug Metab Pharmacokinet 19:48.
152. Wu, X., L.R. Whitfield, and B.H. Stewart. 2000. Atorvastatin transport in the Caco-2 cell model:Contributions of P-glycoprotein and the proton-monocarboxylic acid co-transporter. Pharm Res 17:209.
153. Utoguchi, N., and K.L. Audus. 2000. Carrier-mediated transport of valproic acid in BeWo cells, a human trophoblast cell line. Int J Pharm 195:115.
154. Tsuji, A., and I. Tamai. 1989. Na+ and pH dependent transport of foscarnet via the phosphate carrier system across intestinal brush-border membrane. Biochem Pharmacol 38:1019.
155. Zimmerman, J. 1990. Folic acid transport in organ-cultured mucosa of human intestine. Evidence for distinct carriers. Gastroenterology 99:964.
156. Nussberger, S., and M.A. Hediger. 1995. How peptides cross biological membranes. Exp Nephrol 3:211.
157. Quay, J.F., and S. Foster. 1970. Cephalexin permeation of the surviving rat intestine. J Physiol (Lond) 269:241.
158. Brodin, B., C.U. Nielsen, B. Steffansen, and S. Frokjaer. 2002. Transport of peptidomimetic drugs by the intestinal di/tri-peptide transporter, PepT1. Pharmacol Toxicol 90:285.
159. Goldstein, J.L., R.G. Anderson, and M.S. Brown. 1982. Receptor-mediated endocytosis and the cellular uptake of low density lipoprotein. Ciba Found Symp 77.
160. Larrick, J.W., C. Enns, A. Raubitschek, and H. Weintraub. 1985. Receptor-mediated endocytosis of human transferrin and its cell surface receptor. J Cell Physiol 124:283.
161. Qian, Z.M., H. Li, H. Sun, and K. Ho. 2002. Targeted drug delivery via the transferrin receptormediated endocytosis pathway. Pharmacol Rev 54:561.
162. Fan, J.Y., et al. 1982. Receptor-mediated endocytosis of insulin: Role of microvilli, coated pits, and coated vesicles. Proc Natl Acad Sci 79:7788.
163. Carmel, R., et al. 1969. Vitamin B12 uptake by human small bowel homogenate and its enhancement by intrinsic factor. Gastroenterology 56:548.
164. Clark, M.A., B.H. Hirst, and M.A. Jepson. 2000. Lectin-mediated mucosal delivery of drugs and microparticles. Adv Drug Deliv Rev 43:207.
165. Duncan, R., M.J. Vicent, F. Greco, and R.I. Nicholson. 2005. Polymer-drug conjugates: Towards a novel approach for the treatment of endocrine-related cancer. Endocr Relat Cancer 12(Suppl. 1):S189.
166. Nori, A., and J. Kopecek. 2005. Intracellular targeting of polymer-bound drugs for cancer chemotherapy. Adv Drug Deliv Rev 57:609.
167. Fordtran, J.S., et al. 1965. Permeability characteristics of the human small intestine. J Clin Invest 44:1935.
168. Farquhar, M.G., and G.E. Palade. 1963. Junctional complexes in various epithelia. J Cell Biol 17:375.
169. Ballard, S.T., J.H. Hunter, and A.E. Taylor. 1995. Regulation of tight-junction permeability during nutrient absorption across the intestinal epithelium. Ann Rev Nutr 15:35.
170. Mrsny, R.J. 2005. Modification of epithelial tight junction integrity to enhance transmucosal absorption. Crit Rev Ther Drug Carrier Syst 22:331.
171. Madara, J.L. 1988. Tight junction dynamics: Is paracellular transport regulated? Cell 53:497.
172. Itoh, M., et al. 1999. Direct binding of three tight junction associated MAGUKs, ZO-1, ZO-2 and ZO-3 with the COOH termini of claudins. J Cell Biol 147:1351.
173. Matter, K., and M.S. Balda. 2003. Signalling to and from tight junctions. Nat Rev Mol Cell Biol 4:225.
174. Mrsny, R.J., et al. 2004. Identification of hepoxilin A3 in inflammatory events: A required role in neutrophil migration across intestinal epithelia. Proc Natl Acad Sci 101:7421.
175. Pappenheimer, J.R. 1987. Physiological regulation of transepithelial impedance in the intestinal mucosa of rats and hamsters. J Membr Biol 100:137.
176. Pappenheimer, J.R., and K.Z. Reiss. 1987. Contribution of solvent drag through intercellular junctions to absorption of nutrients by the small intestine of the rat. J Membr Biol 100:123.
177. Hochman, J., and P. Artursson. 1994. Mechanism of absorption enhancement and tight junction regulation. J Contr Rel 29:253.
178. Matter, K., and M.S. Balda. 2003. Functional analysis of tight junctions. Methods 30:228.
179. Anderberg, E.K., T. Lindmark, and P. Artursson. 1993. Sodium caprate elicits dilatation in human intestinal tight junctions and enhances drug absorption by the paracellular route. Pharm Res 10:857.
180. Tomita, M., M. Hayashi, and S. Awazu. 1995. Absorption-enhancing mechanism of sodium caprate and decanoylcarnitine in Caco-2 cells. J Pharmacol Exp Ther 272:739.
181. Baluom, M., M. Friedman, and A. Rubinstein. 2001. Improved intestinal absorption of sulpiride in rats with synchronized oral delivery systems. J Contr Rel 70:139.
182. Watanabe, K., T. Sawano, T. Jinriki, and J. Sato. 2004. Studies on intestinal absorption of sulpiride (3): Intestinal absorption of sulpiride in rats. Biol Pharm Bull 27:77.
183. Zaman, G.J., et al. 1994. The human multidrug resistance-associated protein MRP is a plasma membrane drug-efflux pump. Proc Natl Acad Sci 91:8822.
184. Allen, C.N., et al. 1990. Efflux of bis-carboxyethyl-carboxyfluorescein (BCECF) by a novel ATPdependent transport mechanism in epithelial cells. Biochem Biophys Res Commun 172:262.
185. Zimmerman, J. 1992. Methotrexate transport in the human intestine. Evidence for heterogeneity. Biochem Pharmacol 43:2377.
186. Hunter, J., and B.H. Hirst. 1997. Intestinal secretion of drugs. The role of P-glycoprotein and related drug efflux systems in limiting oral drug absorption. Adv Drug Deliv Rev 25:129.
187. Cummins, C.L., W. Jacobsen, and L.Z. Benet. 2002. Unmasking the dynamic interplay between intestinal P-glycoprotein and CYP3A4. J Pharmacol Exp Ther 300:1036.
188. Kivisto, K.T., M. Niemi, and M.F. Fromm. 2004. Functional interaction of intestinal CYP3A4 and P-glycoprotein. Fundam Clin Pharmacol 18:621.
189. Benet, L.Z., et al. 1999. Intestinal MDR transport proteins and P-450 enzymes as barriers to oral drug delivery. J Contr Rel 62:25.
190. Aungst, B.J., et al. 1996. Enhancement of the intestinal absorption of peptides and non-peptides. J Contr Rel 41:91.
191. Swenson, E.S., and W.J. Curatolo. 1992. Intestinal permeability enhancement for proteins, peptides and other polar drugs: Mechanisms and potential toxicity. Adv Drug Deliv Rev 8:39.
192. Swenson, E.S., W.B. Milisen, and W. Curatolo. 1994. Intestinal permeability enhancement:Efficacy, acute local toxicity, and reversibility. Pharm Res 11:1132.
193. Amidon, G.L., H. Lennernas, V.P. Shah, and J.R. Crison. 1995. A theoretical basis for a biopharmaceutic drug classification: The correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res 12:413.
194. Varma, M.V., et al. 2004. Biopharmaceutic classification system: A scientific framework for pharmacokinetic optimization in drug research. Curr Drug Metab 5:375.
195. Sutton, S.C., et al. 1993. Enhanced bioavailability of cefoxitin using palmitoylcarnitine. II. Use of directly compressed tablet formulations in the rat and dog. Pharm Res 10:1516.
196. Baluom, M., et al. 2000. Synchronous release of sulpiride and sodium decanoate from HPMC matrices: A rationale approach to enhance sulpiride absorption in the rat intestine over time. Pharm Res 17:1071.
197. Baluom, M., M. Friedman, and A. Rubinstein. 1998. The importance of intestinal residence time of absorption enhancer on drug absorption and implication on formulative considerations. Int J Pharm 176:21.