Colonic drug targeting

Journal of Drug Targeting

Volumn 6, Issue 2, 1998, Pages 129-149

  Kinget, Renaat ^a   Kalala, Willbrord ^a   Vervoort, Liesbeth ^a   Van Den Mooter, Guy ^a  

^a UNIVERSITY OF LEUVEN   (Belgium)

Author keywords

Biodegradable polymers; Colonic targeting; pH dependent polymers; Prodrugs; Time dependent release

Indexed keywords

ANTHELMINTIC AGENT; DIAGNOSTIC AGENT; PANCREAS ENZYME;

ANATOMY; ANGINA PECTORIS; ARTHRITIS; ARTICLE; ASTHMA; COLON; COLORECTAL CANCER; CROHN DISEASE; DRUG ABSORPTION; DRUG DELIVERY SYSTEM; DRUG METABOLISM; DRUG TARGETING; GASTROINTESTINAL TRACT; PHYSIOLOGY; PRIORITY JOURNAL; STOMACH ACID; ULCERATIVE COLITIS;

EID: 0032437738     PISSN: 1061186X     EISSN: None     Source Type: Journal    
DOI: 10.3109/10611869808997888     Document Type: Article

References (150)

1. Adkin, D.A., Davis, S.S., Sparow, R.A. and Wilding, I.R. (1993) Colonic transit of different sized tablets in healthy subjects. J. Controlled Rel., 23, 147-153.
2. Alwood, M.C., Archer, D.B. and Ring, S.G. (1989) Delayed release formulations. Eur. Pat. Appl. 0343993A1.
3. Ashford, M., Fell, J.T., Attwood, D. and Woodhead, P.J. (1992) An in vitro investigation into the suitability of pH-dependent polymer for colonic targeting. Int. J. Pharm., 94, 241-245.
4. Ashford, M., Fell, J.T., Attwood, D., Sharma, H. and Woodhead, P.J. (1993a) An in vivo investigation into the suitability of pH-dependent polymers for colon targeting. Int. J. Pharm., 95, 193-199.
5. Ashford, M., Fell, J.J., Attwood, D., Sharma, H.L. and Woodhead, P.J. (1993b) An evaluation of pectin as carrier for drug targeting to the colon. J. Controlled Rel., 26, 213-220.
6. Ashford, M., Fell, J., Attwood, D., Sharma, H. and Woodhead, P. (1994) Studies on pectin formulations for colonic drug delivery. J. Controlled Rel., 30, 225-232.
7. Azad Khan, A.K., Piris, J. and Truelove, S.C. (1977) An experiment to determine the active therapeutic moiety of sulphasalazine. The Lancet, 2, 895-895.
8. Bauer, K.H. and Kesselhut, J.F. (1995) Novel pharmaceutical excipients for colon targeting. S.T.P. Pharma Sci., 5, 54-59.
9. Binder, H.J., Foster, E.S., Budinger, M.E. and Hayslett, J.P. (1987) Mechanism of electroneural sodium chloride absorption in distal colon of the rat. Gastroenterology, 93, 449-455.
10. Binns, J.S., Stevens, H.N.E., Bakhshaee, M. and Wilson, C.G. (1994) Colon targeted release using the Pulsincap delivery system. Proc. Intern. Symp. Control. Rel. Bioact. Mater., 21, 260-261.
11. Bown, R.L., Gibson, J.A., Sladen, G.E., Hicks, B. and Dawson, A.M. (1974) Effects of lactulose and other laxatives on ileal and colonic pH as measured by a radiotelemetry device. Gut, 15, 999-1004.
12. Brondsted, H. and Kopecek, J. (1991) Hydrogels for site-specific oral drug delivery: Synthesis and characterization. Biomaterials, 12, 584-592.
13. Brondsted, H. and Kopecek, J. (1992) Hydrogels for site-specific drug delivery to the colon: In vitro and in vivo degradation. Pharm. Res., 9, 1540-1545.
14. Brondsted, H., Hovgaard, I. and Simonsen, I. (1995) Dextran hydrogels for colon-specific drug delivery IV. Comparative release study of hydrocortisone and prednisolone phosphate. STP Pharma Sciences, 5, 65-69.
15. Brown, J.P., McGarraugh, G.V., Parkinson, T.M., Wingerd, R.E. Jr. and Oderndonck, A.B. (1983) A polymeric drug for treatment of inflammatory bowel disease. J. Med. Chem., 26, 1300-1307.
16. Cann, P.A., Read, N.W., Brown, C., Hobson, N. and Holdsworth, (1983) Irritable bowel syndrome: Relationship of disorders in the transit of a single solid meal to symptom patterns. Gut, 24, 405-411.
17. Chan, R.P., Pope, D.J., Gilbert, A.P., Sacra, P.J., Baron, J.H. and Lennard-Jones, J.E. (1983) Studies of two novel sulphasalazine analogs, ipsalazide and balsalazide. Dig. Dis. Sci., 28, 609-615.
18. Cheng, C.L., Gehrke, St. H. and Ritschel, W.A. (1994) Development of an azopolymer based colonic release capsule for delivering proteins/macromolecules. Meth. Find. Exp. Clin. Pharmacol., 16, 271-278.
19. Connel, A.M. (1968) Motor action of the large bowel. In Coda, C.F. and Heidel, W. (ed.), Handbook of Physiology, Sect 6, Vol. IV (Washington D.C.: American Physiology Society), pp. 66-92.
20. Cooper, M.D., Perey, D.Y., McKnealiky, M.F., Gabrielsa, A.E., Sutherland, D.E.R. and Good, R.A. (1966) A mammalian equivalent of the avian Bursa of fabricus. Lancet, 1, 1388-1391.
21. Davis, S.S. (1989) Assessment of gastrointestinal transit and drug absorption. In Prescott L.F. and Nimmo S.W. (ed.) Novel Drug Delivery and its Therapeutic Application (Chichester: Wiley), pp. 89-101.
22. Davis, S.S., Hardy, J.G. and Fara, J.W. (1986) Transit of pharmaceutical dosage forms through the small intestine. Gut, 27, 886-892.
23. Davis, S.S., Hardy, J.G., Newman, S.P. and Wilding, I.R. (1992) Gamma scintigraphy in the evaluation of pharmaceutical dosage forms. Eur. J. Nucl. Med., 19, 971-986.
24. Edlund, C., Lidbeck, A., Kager, L. and Nord, C.E. (1987) Comparative effects of enoxacin and norfloxacin on human colonic microflora. Antimicrob. Agents Chemother., 31, 1846-1848.
25. Enck, P., Merlin, V., Erckenbrecht, J.F. and Wienbeck, M. (1989) Stress effects on gastrointestinal transit in the rat. Gut, 30, 455-459.
26. Evans, D.F., Pye, G., Bramley, R., Clark, A.G., Dyson, T.J. and Hardcastle, J.D. (1988) Measurement of gastrointestinal pH profiles in normal ambulant human subjects. Gut, 29, 1035-1041.
27. Fara, J.W. (1989) Colonic drug absorption and metabolism. In Prescott, L.F. and Nimmo, W.S. (ed.) Novel Drug Delivery and Therapeutics (Chichester: Wiley), pp. 103-112.
28. Fix, J.A. (1987) Absorption enhancing agents for gastrointestinal system. J. Controlled Rel., 6, 151-162.
29. Fix, J.A. (1996) Strategies for delivery peptides utilizing absorption-enhancing agents. J. Pharm. Sci., 85, 1282-1285.
30. Friend, D.R. and Chang, G.W. (1984) A colon-specific drug delivery system based on drug glycosides and glycosidases of colonic bacteria. J. Med. Chem., 27, 261-266.
31. Friend, D.R. and Chang, G.W. (1985) Drug glycosides: Potential prodrugs for colon-specific drug delivery. J. Med. Chem., 28, 51-57.
32. Friend, D.R. and Tozer, T.N. (1992) Drug glycosides in oral colon-specific drug delivery. J. Controlled Rel., 19, 109-120.
33. Friend, D.R. (1995) Glycoside prodrugs: novel pharmacotherapy for colonic diseases. S.T.P. Pharma Sci., 5, 70-76.
34. Gazzaniga, A., Bussetti, C., Moro, L., Sangali, M.E. and Giordano, F. (1995) Time dependent oral delivery systems for colon targeting. S.T.P. Pharma. Sci., 5, 83-88.
35. Gazzaniga, A., Iamartino, P., Maffione, G. and Sangalli, M.E. (1994) Oral delayed release system for colonic specific delivery. Int. J. Pharm., 108, 77-83.
36. Ghandehari, H., Kopeckova, P. and Kopecek, J. (1997) In vitro biodegradation of pH-sensitive hydrogels containing aromatic azo bonds. Biomaterials, 18, 861-872.
37. Gibson, S.A.W., Mcfarlan, C., Hay, S. and Macfarlane, G.T. (1989) Significance of microflora in proteolysis in the colon. Appl. Environm. Microbiol., 55, 679-683.
38. Gingell, J.C., Davies, M.W. and Shields, R. (1968) Effect of synthetic gastrin-like pentapeptide upon the intestinal transport of sodium, potassium and water. Gut, 9, 111-115.
39. Gleiter, C.H., Antonin, K.H., Bieck, P., Godbillon, J., Schonleber, W. and Malchow, H. (1985) Colonoscopy in the investigation of drug absorption in healthy volunteers. Gastrointest. Endosc., 31, 71-73.
40. Goldstein, D.A., Tan, Y.K. and Soldin, S.J. (1987) Pharmacokinetics and absolute bioavailability of salbutamol in healthy adult volunteers. Eur. J. Clin. Pharmacol., 32, 631-634.
41. Gorbach, S.L. (1971) Intestinal microflora, Gastroenterology, 60, 1110-1129.
42. Gruber, P., Longer, M.A. and Robinson, J.R. (1987) Some biological issues in oral, controlled drug delivery. Adv. Drug Del. Rev., 1, 1-18.
43. Haeberlin, B. and Friend, D.R. (1992) Anatomy and physiology of the gastrointestinal tract. In Friend, D.R. (ed.) Oral Colon-Specific Drug Delivery (Boca Raton: CRC Press), pp. 1-43.
44. Hagikara, P.F. and Griffin, W.O.J. (1977) Physiology of the colon and the rectum. Surg. Clin. North. Am., 52, 797-805.
45. Harboe, E., Larsen, C., Johansen, M. and Diesen, H.P. (1989) Macromolecular prodrugs XV. Colon targeted delivery bioavailability of naproxen from orally administered dextran-naproxen prodrugs varying in molecular size in the pig. Pharm. Res., 6, 919-923.
46. Hardy, J.G. (1989) Colonic transit and drug delivery. In Hardy, J.G., Davis, S.S. and Wilson, C.G. (ed.) Drug Delivery to the Gastrointestinal Tract (Chichester: Ellis Horwood), pp. 75-81.
47. Hardy, J.G., Healy, J.N.C. and Reynolds, J.R. (1987) Evaluation of an enteric coated delayed release 5-aminosalicylic acid tablet in patients with inflammatory bowel disease. Alimentary Pharmacol. Therap., 1, 273-280.
48. Hardy, J.G., Davis, S.S., Khosla, R. and Robertson, C.S. (1988) Gastrointestinal transit of small tablets in patients with ulcerative colitis. Int. J. Pharm., 48, 79-82.
49. Hardy, J.G., Wilson, C.G. and Wood, E. (1985) Drug delivery to the proximal colon. J. Pharm. Pharmacol., 37, 874-877.
50. Hawker, P.C., Mashier, K.E. and Turnberg, L.A. (1978) Mechanism of transport of sodium chloride and potassium in the human colon. Gastroenterology, 74, 1241-1247.
51. Hill, M.J. and Drasar, B.S. (1975) The normal colonic bacterial flora. Gut, 16, 318-323.
52. Hirayama, F., Minami, K. and Uekama, K. (1996) In vitro evaluation of biphenyl acetic acid-β-cyclodextrin conjugates as colon targeting prodrugs: drug release behaviour in rat biological media. J. Pharm. Pharmacol., 48, 27-31.
53. Hirsch, S., Binder, V., Kolter, K., Kesselhut, J.F. and Bauer, K.H. (1997) Lauroyldextran as a coating material for site-specific drug delivery to the colon: in vitro dissolution of coated tablets. Proc. Int. Symp. Control. Rel. Bioact. Mater., 24, 379-380.
54. Hovgaard, L. and Bronsted, H. (1995) Dextran hydrogels for colon-specific drug delivery. J. Controlled Rel., 36, 159-166.
55. Ikesue, K., Kopeckova, P. and Kopecek, J. (1991) Degradation of proteins by enzymes of the gastrointestinal tract. Proc. Intern. Symp. Control. Rel. Bioact. Mater., 18, 580-581.
56. Jay, M., Beihn, R.M., Digenis, G.A., Deland, F.H., Caldwell, L. and Mlodozeniec, A.R. (1985) Disposition of radiolabelled suppositories in humans. J. Pharm. Pharmacol., 37, 266-268.
57. Kalala, W., Kinget, R., Van den Mooter, G. and Samyn, C. (1996) Colonic drug targeting: in vitro release of ibuprofen from capsules coated with poly(ether-ester) azo polymers. Int. J. Pharm., 139, 187-195.
58. Khosla, R. and Davis, S.S. (1989) Gastric emptying and small and large bowel transit of non-disintegrating tablets in fasted subjects. Int. J. Pharm., 52, 1-10.
59. Kim, J.S., Oberle, R.L. , Krummel, D.A., Dressman, J.B. and Fleisher, D. (1994) Absorption of ACE inhibitors from small intestine and colon. J. Pharm. Sci., 83, 1350-1356.
60. Kimura, Y., Makita, Y., Kumagai, T., Yamane, H., Kitao, T., Sasatani, H. and Kim, S.I. (1992) Degradation of azo containing polyurethane by the action of intestinal microflora. Polymer, 33, 5294-5299.
61. Kopecek, J., Kopeckova, P., Brondsted, H., Rathi, R., Rihova, B., Yeh, P.Y. and Ikesue, K. (1992) Polymers for colon-specific drug delivery. J. Controlled Rel., 19, 121-130.
62. Kopeckova, P. and Kopecek, J. (1990) Release of 5-aminosalicylic acid from bioadhesive N-(2-hydroxypropyl)methacrylamide copolymers by azoreductases in vitro. Makromol. Chem., 191, 2037-2045.
63. Kopeckova, P., Rathi, R., Takada, S., Rihova, B., Berenson, M.M. and Kopecek, J. (1994) Bioadhesive N-(2-hydroxypropyl)methacrylamide copolymers for colon-specific drug delivery. J. Controlled Rel., 28, 211-222.
64. Langguth, P., Breves, G., Stokli, A., Merkle, H.P. and Wolffram, S. (1994) Colonic absorption and bioavailability of the pentapeptide metkephamid in the rat. Pharm. Res., 11, 1640-1645.
65. Lee, V.H.L. (1991) Changing needs in drug delivery in the era of peptide and protein drugs. In Lee, V.H.L. (ed.) Peptide and Protein Drug Delivery (New York: Marcel Dekker), pp. 1-56.
66. Lee, V.H.L., Doddo-Kashi, S., Grasss, G.M. and Rubas, W. (1991) Oral route of peptide and protein drug delivery. In Lee, V.H.L (ed.) Peptide and Protein Drug Delivery (New York: Marcel Dekker), pp. 691-738.
67. Lee, V.H.L. (1992) Oral route of peptide and protein drug delivery. BioPHARM, 5, 39-50.
68. Lehmann, K. (1975) Magensaftresistente und retardierende Arzneimittelüberzüge aus wässrigen Acrylharzdispersionen. Acta Pharm. Techn., 21, 255-260.
69. Lehmann, K.O.R. and Dreher, K.D. (1991) Methacrylate-galactomannan coating for colon-specific drug delivery. Proceed. Intern. Symp. Control. Rel. Bioact. Mater., 18, 331-332.
70. Leopold, C.S. and Friend, D.R. (1994) Poly (L-aspartic acid) as drug carrier for colon-specific drug delivery. An in vitro assesment. Proc. Intern. Symp. Control. Rel. Bioact. Mater., 21, 258-259.
71. Lindsey, J.T., Smith, J.W., McCluggage, S.G.J. and Nicholas, R.L. (1990) Effects of commonly used bowel preparations on the large bowel mucosa-associated and luminal microflora in the rat model. Dis. Col. Rectum, 33, 554-560.
72. Macfarlane, G.T., Cummings, J.H. and Allison, C. (1986) Protein degradation by human intestinal bacteria. J. Gen. Biol., 132, 1647-1656.
73. Macfarlane, G.T., Allison, C., Gibson, S.A.W. and Cummings, J.H. (1988) Contribution of the microflora to proteolysis in the human large intestine. J. Appl. Bacteriol., 64, 37-46.
74. Macfarlane, G.T., Hay, S. and Gibson, G.R. (1989) Influence of mucin on glycosidase, protease and arylamidase activities of human gut bacteria grown in a 3-stage continuous culture system. J. Appl. Bacteriol., 66, 407-417.
75. Macfarlane, G.T., Gibson, G.R., Beatty, J.H. and Cummings, J.H. (1992) Estimation of short chain fatty acid production from protein by human intestinal bacteria based on branched-chain fatty acid measurements. FEMS Microbiol. Ecol., 101, 81-88.
76. Mackay, M. and Tomlinson, E. (1993) Colonic delivery of therapeutic peptides and proteins. In Biek, P.R. (ed.) Colonic Absorption and Metabolism (New York: Marcel Dekker), pp. 159-176.
77. Macleod, A.D. and Tozer, T.N. (1992) Kinetic perspectives in colonic drug delivery. In Friend, DR. (ed.) Oral Colon-Specific Drug Delivery (Boca Raton: CRC Press), pp. 85-114.
78. Macleod, A.D., Tolentino, L. and Tozer, T.N. (1994) Glucocorticoid dextran conjugates as potential prodrugs for colon-specific delivery: Steady state pharmacokinetics in the rats. Biopharm. Drug Disp., 15, 151-161.
79. MacNeil, M.E. and Stevens, H.N.E. (1990) Patent WO 90/09168.
80. Madara, J.L. and Dharmsathaphorn, K. (1985) Occluding junction structure-function relationships in cultured epithelial monolayer. J. Cell Biol., 101, 2124-2133.
81. Malagelada, J.R., Robertson, J.S., Brown, M.L., Remington, M., Duenes, J.A., Thomforde, G.M. and Carryer, P.W. (1984) Intestinal transit of solid and liquid components of a meal in health. Gastroenterology, 87, 1255-1263.
82. Meldrum, S.J., Watson, B.W., Riddle, H.C., Bown, R.L. and Sladen, G.E. (1972) pH profile of gut as measured by radiotelemetry capsule. Br. Med. J., 2, 104-106.
83. Meschan, I. (1975) Small intestine, colon and biliary tract. In Meschan, I. An Atlas of Basic Anatomy to Radiology (Philadelphia: W.B. Saunders Co.), pp. 843-925.
84. Milojevic, S., Newton, J.M., Cummings, J.H., Gibson, G.R., Botham, R.L., Ring, S.O., Stockham, M. and Allwood, M.C. (1996) Amylose as a coating for drug delivery to the colon: preparation and in vitro evaluation using 5-aminosalicylic acid pellets. J. Controlled Rel., 38, 75-84.
85. Misiewics, J.J. (1975) Colonic motility. Gut, 16, 311-314.
86. Molly, K., Vande Woestyne, M. and Verstraete, W. (1993) Development of a 5-step multi chamber reactor as a simulation of the human intestinal microbial ecosystem. Appl. Microbiol. Biotechnol., 39, 254-258.
87. Moore, W.E.C. and Holdeman, L.V. (1975) Discussion of current bacteriologic investigations of the relationship between intestinal flora, diet and colon cancer. Cancer Res., 35, 3418-3420.
88. Mrsny, R.J. (1992) The colon as a site for drug delivery. J. Controlled Rel., 22, 15-34.
89. Munjeri, O., Collet, J.H. and Fell, J.T. (1997) Hydrogel beads based on amidated pectins for colon-specific drug delivery: the role of chitosan in modifying drug release. J. Controlled Rel., 46, 273-278.
90. Murakami, M., Yoshikawa, H., Takada, K. and Muranishi, S. (1986) Effect of oleic acid vesicles on intestinal absorption of carboxyfluorescein in rats. Pharm. Res., 3, 35-40.
91. Muranishi, S. (1987) Potentials and limitations of absorption enhancers. Proceed. Int. FIP Sat. Symp., p. L18.
92. Muranishi, S. (1990) Absorption enhancers. Crit. Rev. Ther. Drug Car. Sys., 7, 1-33.
93. Muranishi, S., Muranishi, N. and Sezaki, K. (1979) Improvement of absolute bioavailability of normally poorly absorbed drug: Inducement of intestinal absorption of streptomycin and gentamycin by lipid-bile salt mixed micelles in rat and . rabbit. Int. J. Pharm., 2, 101-109.
94. Niibuchi, J.J., Aramaki, Y. and Tchusiya, S. (1986) Binding of antibiotics to rat intestinal mucin. Int. J. Pharm., 30, 181-187.
95. Niwa, K., Takaya, T., Morimoto, T. and Takada, K. (1995) Preparation and evaluation of a time-controlled release capsule made of ethylcellulose for colon delivery of drugs. J. Drug Target., 3, 83-89.
96. Nord, C.E. and Heimdahl, A. (1986) Impact of orally administered antimicrobial agents on human oropharyngeal and colonic microflora. J. Antimicrob. Chemother., 18, Suppl. C, 159-164.
97. Ovesen, L., Bendsten, F., Tage-Jensen, K., Pedersen, N.T., Gram, B.R. and Rune, S.J. (1986) Intraluminal pH in the stomach, duodenum and proximal jejenum in normal subjects and patients with exocrine pancreatic insufficiency. Gastroenterology, 90, 258-262.
98. Peeters, R. (1990) Studie over de ontwikkeling van een colon-specifieke artsenijvorm. Doctoral Thesis K.U. Leuven.
99. Peeters, R. and Kinget, R. (1993) Film-forming polymers for colonic drug delivery. I. Synthesis and physical and chemical properties of methyl derivatives of Eudragit S. Int. J. Pharm., 94, 125-134.
100. Phillips, S.F. (1993) Gastrointestinal physiology and its relevance to targeted drug delivery. In Current Status on Targeted Drug Delivery to the Gastrointestinal Tract (Capsugel Symposia Series), pp. 8-18.
101. Pozzi, F., Furlani, P., Gazzaniga, A., Davis, S.S. and Wilding, I.R. (1994) The TIME-CLOCK® system: a new oral dosage form for fast and complete release of drug after a pre-determined lag time. J. Controlled Rel., 31, 99-108.
102. Rahman, A., Barrowman, J.A. and Rahimtula, A. (1986) The influence of bile on the bioavailability of polynuclear aromatic hydrocarbons from rat intestines. Can. J. Physiol. Pharmacol., 64, 1214-1218.
103. Rihova, B., Rathi, R.C., Kopeckova, P. and Kopecek, J. (1992) In vitro bioadhesion of carbohydrate-containing N-(2-hydroxypropyl)methacrylamide copolymers to the GI tract of guinea pigs. Int. J. Pharm., 87, 105-116.
104. Roslyn, J.J. and Zinner, M.Y. (1991) Surgical anatomy and operative procedures. In Sabiston, D.L. (ed.) Textbook of Surgery (Philadelphia: W.B. Saunders Co.), pp. 899-901.
105. Rowland, I.R. (1988) Factors affecting metabolic activity of the intestinal microflora. Drug Metabol. Rev., 19, 243-261.
106. Rubinstein, A. (1990) Microbially controlled drug delivery to the colon. Biopharm. Drug Dispos., 11, 465-475.
107. Rubinstein, A. and Gliko-Kabir, I. (1995) Synthesis and swelling-dependent enzymatic degradation of borax-modified guar gum for colonic delivery purposes. S.T.P. Pharma Sci., 5, 41-46.
108. Rubinstein, A., Nakar, D. and Sintov, A. (1992a) Colonic drug delivery enhanced release of indomethacin from cross-linked chondroitin matrix in rat caecal contents. Pharm. Res., 9, 276-278.
109. Rubinstein, A., Nakar, D. and Sintov, A. (1992b) Chondroitin sulfate: a potential biodegradable carrier for colon-specific drug delivery. Int. J. Pharm., 84, 141-150.
110. Rubinstein, A., Radai, R., Ezna, M. and Pathnack, S. (1993) In vitro evaluation of calcium pectate: A potential colon-specific drug delivery carrier. Pharm. Res., 10, 258-263.
111. Rubinstein, A. and Radai, R. (1995) In vitro and in vivo analysis of colon specificity of calcium pectinate formulations. Eur. J. Pharm. Biopharm., 41, 291-295.
112. Saffran, M., Kumar, G.S., Savariar, C., Burnham, J.C., Williams, S. and Neckers, D.C. (1986) A new approach to the oral administration of insulin and other peptide drugs. Science, 233, 1081-1084.
113. Saffran, M., Kumar, G.S., Neckers, D.G., Williams, F., Field, J.B., Jones, R.H. and Panepinto, L. (1988) New approaches to the oral administration of peptide drugs. Pharm. Week Sci. Ed., 10, 43-44.
114. Saffran, M., Field, J.B., Pena, J., Jones, R.H. and Okuda, Y. (1991) Oral insulin in diabetic dogs. J. Endocrinol., 131: 267-278.
115. Sakai, K., Kutsuna, T.M., Nishino, T., Fujihara, Y. and Yata, N. (1986) Contribution of calcium ion sequestration by polyoxyethylated nonionic surfactants to the enhanced colonic absorption of p-aminobenzoic acid. J. Pharm. Sci., 75, 387-390.
116. Samuel, P.G., Sypol, G.M., Meilman, E., Mosbach, E.H. and Chafizadeh, M. (1968) Absorption of bile acids from large bowel in man. J. Clin. Invest., 42, 2070-2078.
117. Samyn, C., Kalala, W., Van den Mooter, G. and Kinget, R. (1995) Synthesis and in vitro biodegradation of poly(ether-ester) azo polymers designed for colon targeting. Int. J. Pharm., 121, 211-216.
118. Sarlikiotis, A.W. and Bauer, K.H. (1992) Synthese und unterschung von polyurethanen mit galactomannan-segmenten als hilfsstoffe zur freizetzung von peptid-arzneistoffen im dickdarm. Pharm. Ind., 54, 873-886.
119. Schacht, E., Gevaert, A., Kenawy, E.R., Molly, K., Verstraete, W., Adriaensens, P., Carleer, R. and Gelan, R. (1996) Polymers for colon specific drug delivery. J. Controlled Rel., 39, 327-338.
120. Scheline, R.R. (1973) Metabolism of foreign compounds by gastrointestinal microorganisms. Pharmacol. Rev., 25, 451-523.
121. Shanta, K.L., Ravishandran, P. and Rao, K.P. (1995) Azo polymeric hydrogels for colon targeted drug delivery. Biomaterials, 16, 1313-1318.
122. Simon, G.I. and Gorbach, S.L. (1986) The human intestinal microflora. Dig. Dis. Sc., 31, 147S-162S.
123. Simonsen, L., Hovgaard, L., Mortensen, P.B. and Brondsted, H. (1995) Dextran hydrogels for colon-specific drug delivery. V. Degradation in human intestinal incubation models. Eur. J. Pharm. Sci., 3, 329-337.
124. Spitael, J. and Kinget, R. (1977a) Solubilité et vitesse de dissolution de différents polymères entériques. Lab. Pharm., 25, 847-849.
125. Spitael, J. and Kinget, R. (1977b) Factors affecting the dissolution rate of enteric coatings. Pharm. Ind., 39, 502-505.
126. Spitael, J. and Kinget, R. (1979) Solubility and dissolution rate of enteric polymers. Acta Pharm. Technol., 25 (Suppl 7), 163-168.
127. Spitael, J., Kinget, R. and Naessens, K. (1980) Dissolution rate of cellulose acetate pthalate and the Bronsted catalysis law. Pharm. Ind., 42, 846-849.
128. Stella, V. (1975) Pro-drugs: an overview and definition. In Higuchi, T. and Stella, V. (eds.) Pro-drugs as Novel Drug Delivery Systems (Washington D.C.: ACS), pp. 1-115.
129. Taniguchi, K., Muranishi, S. and Sezaki, H. (1980) Enhanced intestinal permeability to macromolecules. II. Improvement of the large intestinal absorption of heparin by lipid-surfactant mixed micelles in rat. Int. J. Pharm., 4, 219-228.
130. Thomas, P., Richard, A., Rogers, L., Evans, B.K., Dew, M.J. and Rhodes, J. (1985) Absorption of delayed-release prednisolone in ulcerative colitis and Crohn's disease. J. Pharm. Pharmacol., 37, 757-758.
131. Tomita, M., Shiga, M., Hayashi, M. and Awazu, S. (1988) Enhancement of colonic drug absorption by paracellular permeation route. Pharm. Res., 5, 431-435.
132. Touitou, E. and Rubinstein, A. (1986) Targeted enteral delivery of insulin to rats. Int. J. Pharm., 30, 95-99.
133. Ueda, S., Ibuki, R., Kawamuza, A., Murata, S., Takahashi, T., Kimuza, S. and Hata, T. (1994) Development of a novel drug delivery system, Time-Controlled-Explosion System (TES). J. Drug Targeting., 2, 133-140.
134. Ueda, T., Yamaoka, T., Miyamoto, M., Kimura, Y., Sasatani, H. and Kim, S.I. (1996) Bacterial reduction of azo compounds as a model reaction for the degradation of azo-containing polyurethane by the action of intestinal flora. Bull. Chem. Soc. Jpn., 69, 1139-1142.
135. Vandelli, M.A., Leo, E., Forni, F. and Bernabei, M.T. (1996) In vitro evaluation of a potential colonic delivery system that releases drug after a controllable lag-time. Eur. J. Pharm. Biopharm., 43, 148-151.
136. Van den Mooter, G., Offringa, M., Kalala, W., Samyn, C. and Kinget, R. (1995) Synthesis and evaluation of new linear azo-polymers for colonic targeting. S.T.P. Pharma Sci., 5, 36-40.
137. Van den Mooter, G., Samyn, C. and Kinget, R. (1992) Azo polymers for colon-specific drug delivery. Int. J. Pharm., 87, 37-46.
138. Van den Mooter, G., Samyn, C. and Kinget, R. (1993) Azo polymers for colon-specific drug delivery. Part II: Influence of the type of azo polymer on the degradation by intestinal microflora. Int. J. Pharm., 97, 133-139.
139. Van den Mooter, G., Samyn, C. and Kinget, R. (1994) The relationship between swelling properties and enzymatic degradation of azo polymers designed for colon-specific drug delivery. Pharm. Res., 11, 1737-1741.
140. Van den Mooter, G., Samyn, C. and Kinget, R. (1995) In vivo evaluation of a colon-specific drug delivery system: An absorption study of theophylline from capsules coated with azo polymers in rats. Pharm. Res., 12, 244-247.
141. Van Hozegard, R.A. (1988) Pharmacokinetics of olsalazine and its metabolites. Scand. J. Gastroenterol., 23 Suppl. 148, 17-20.
142. Vervoort, L. and Kinget, R. (1996) In vitro degradation by colonic bacteria of inulin HP incorporated in Eudragit films. Int. J. Pharm., 129, 185-190.
143. Wakerly, Z., Fell, J.T., Attwood, D. and Parkins, D. (1996) Pectin/ethylcellulose film coating formulations for colonic drug delivery. Pharm. Res., 13, 1210-1212.
144. Wilding, I.R., Davis, S.S., Stevens, H.N.E., Bakhshaee, M., Sparrow, R.A. and Brennan, J. (1992) Gastrointestinal transit and systemic absorption of captopril from a pulsed release formulation. Pharm. Res., 9, 654-657.
145. Willoughby, C.P., Cowan, R.E., Gould, S.R., Machell, R.J. and Stewart, J.B. (1988) Double-blind comparison of olsalazine and sulphasalazine in active ulcerative colitis. Scand. J. Gastroenterol., 23 Suppl. 148, 40-44.
146. Wilson, C.G. and Washington, N. (1989) Physiological Pharmaceutics, Biological Barriers to Drug Absorption. Ellis Horwood Ltd., Chichester, UK.
147. Wood, E., Wilson, C.G. and Hardy, J.G. (1985) The spreading of foam and solution enemas. Int. J. Pharm., 25, 191-197.
148. Yeh, P.Y., Kopeckova, P. and Kopecek, J. (1994) Biodegradable and pH-sensitive hydrogels: synthesis by crosslinking of N,N-dimethylacrylamide copolymer precursors. J. Polymer Sci. Part A Polymer Chem., 32, 1627-1637.
149. Yeh, P.Y., Berenson, M.M., Samowitz, W.S., Kopeckova, P. and Kopecek, J. (1995) Site-specific drug delivery and penetration enhancement in the gastrointestinal tract. J. Controlled Rel., 36, 109-124.
150. Zeitoun, P. and Brisard, P. (1988) Im colon zelfallende tabletten und ihre Herstellung, Patent Rousel-Uclaf, Patentschrift DE 3046559 C2.