Prednisolone 21-sulfate sodium: A colon-specific pro-drug of prednisolone

Journal of Pharmacy and Pharmacology

Volumn 55, Issue 8, 2003, Pages 1075-1082

  Jung, Yun Jin ^a,b   Doh, Min Ju ^a   Kim, In Ho ^a   Kong, Hye Sik ^a   Lee, Jeoung Soo ^a,c   Kim, Young Mi ^a  

^a Pusan National University   (South Korea)

^b NATIONAL CANCER INSTITUTE   (United States)

^c UNIVERSITY OF UTAH   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

PREDNISOLONE; PREDNISOLONE 21 SULFATE SODIUM; PRODRUG; SULFATASE; SULFATE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CECUM; COLON; CONTROLLED STUDY; DOSE RESPONSE; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG DELIVERY SYSTEM; DRUG HYDROLYSIS; DRUG RELEASE; DRUG SOLUBILITY; DRUG SPECIFICITY; DRUG STABILITY; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG TISSUE LEVEL; ENZYME ACTIVITY; IN VITRO STUDY; IN VIVO STUDY; MALE; NONHUMAN; PARTITION COEFFICIENT; PH; RAT; SMALL INTESTINE; STOMACH; STRUCTURE ANALYSIS;

ADMINISTRATION, ORAL; ANIMALS; COLON; DOSAGE FORMS; INTESTINAL ABSORPTION; MALE; PREDNISOLONE; PRODRUGS; RATS; RATS, SPRAGUE-DAWLEY; SULFATASES; SULFATES;

EID: 0042526078     PISSN: 00223573     EISSN: None     Source Type: Journal    
DOI: 10.1211/0022357021413     Document Type: Article

References (22)

1. Brown, J. P., McGarraugh, G. V., Parkinson, T. M., Wingard, R. E., Onderdonk, A. B. (1983) A polymeric drug for treatment of inflammatory bowel disease. J. Med. Chem. 26: 1300-1307
2. Crotty, B, Jewel, J. P. (1992) Drug therapy of ulcerative colitis. Br. J. Clin. Pharmacol. 34: 189-198
3. Faigle, J. W. (1993) Drug metabolism in the colon wall and lumen: In: Bieck, P. R. (ed.) Colonic Drug Absorption and Metabolism. Marcel Dekker Inc., New York, NY, pp 29-54
4. Fedorak, R. N., Haeberlin, B., Empey, L. R., Cui, N., Nolen, H., Jewell, L. D., Friend, D. R. (1995) Colonic delivery of dexamethasone from a prodrug accelerates healing of colitis in rats without adrenal suppression. Gastroenterology 108: 1688-1699
5. Friedman, S., Blumberg, R. S. (2001) Inflammatory bowel disease. In: Harrison's Principles of Internal Medicine. 15th edn, CD-ROM, McGraw-Hill, New York
6. Friend, D. R., Chang, G. W. (1984) A colon-specific drug-delivery system based on drug glycosides and the glycosidases of colonic bacteria. J. Med. Chem. 27: 261-266
7. Friend, D. R., Chang, G. W. (1985) Drug glycosides: Potential prodrugs for colon-specific drug delivery. J. Med. Chem. 28: 51-57
8. Huijghebaert, S., Sim, S. M., Back, D. J., Eyssen, H. J. (1984a) Distribution of estrone sulfatase activity in the intestine of germ-free and conventional rats. J. Steroid Biochem. 20: 1175-1179
9. Huijghebaert, S., Parmentier, G., Eyssen, H. J. (1984b) Specificity of bile salt sulfatase activity in man, mouse and rat intestinal microflora. J. Steroid Biochem. 20: 907-912
10. Istran, C., Gabor, S., Ferene, S. (1991) Glycosides of 5-aminosalicylic acid. Magy. Kem. FOLY 97: 143-147
11. Jung, Y. J., Lee, J. S., Kim, Y. M. (2000) Synthesis and in vitro/in vivo evaluation of 5-aminosalicyl-glycine as a colon-specific prodrug of 5-aminosalicyclic acid. J. Pharm. Sci. 89: 594-602
12. Jung, Y. J., Lee, J. S., Kim, Y. M. (2001) Colon-specific prodrug of 5-aminosalicylic acid: Synthesis and in vitro/in vivo properties of acidic amino acid derivatives of 5-aminosalicylic acid. J. Pharm. Sci. 90: 1767-1775
13. Kopeckova, P., Kopecek, J. (1990) Release of 5-aminosalicylic acid from bioadhesive N-(2-hydroxypropyl) methacrylamide copolymers by azoreductases in vitro. Makromol. Chem. 191: 2037-2045
14. Larsen, C., Johansen, M. (1985) Dextrans as carriers for drug compounds - Realized and potential applications. Arch. Pharm. Chem. 92: 809-830
15. McLeod, A. D., Friend, D. R., Tozer, T. N. (1993) Synthesis and chemical stability of glucocorticoid-dextran ester: Potential prodrugs for colon-specific delivery. Int. J. Pharm. 92: 105-114
16. McLeod, A. D., Friend, D. R., Tozer, T. N. (1994) Glucocorticoid-dextran conjugate as potential prodrugs for colon-specific delivery: Hydrolysis in rat gastrointestinal tract contents. J. Pharm. Sci. 83: 1284-1288
17. Robinson, M. (1998) Medical therapy in inflammatory bowel disease for the 21st century. Eur. J. Surg. Suppl. 582: 90-98
18. Rubinstein, A. (1990) Microbially controlled drug delivery to the colon. Biopharm. Drug Dispos. 11: 465-475
19. Ryde, E. M. (1992) Low-molecular-weight azo compounds. In: Friend, D. R. (ed.) Oral Colon Specific Drug Delivery. CRC Press, Boca Raton, FL, pp 143-152
20. Schimmer, B. P., Parker, K. L. (2001) Adrenocorticotropic hormone; Adrenocortical steroids and their synthetic analogs; Inhibitors of the synthesis and actions of adrenocortical hormones. In: Hardman, J. G., Limbird, L. E. (Editors-in-chief) Goodman and Gilman's the Pharmacological Basis of Therapeutics. 10th edn, McGraw-Hill, New York, NY, pp 1649-1677
21. Van Eldere, J., Robben, J., De Pauw, G., Merckx, R., Eyssen, H. (1988) Isolation and identification of intestinal steroid-desulfating bacteria from rats and humans. Appl. Environ. Microbiol. 54: 2112-2117
22. William-Smith, H. (1965) Observations on the flora of the alimentary tract of animals and factors affecting its composition. J. Pathol. Bacteriol. 89: 95-122