Steady-state pharmacokinetics of corticosteroid delivery from glucuronide prodrugs in normal and colitic rats

Biopharmaceutics and Drug Disposition

Volumn 18, Issue 8, 1997, Pages 681-695

  Nolen III, Harold W ^a   Fedorak, Richard N ^b   Friend, David R ^a,c  

^a SRI INTERNATIONAL   (United States)

^b UNIVERSITY OF ALBERTA   (Canada)

^c CIBUS Pharmaceutical Inc   (United States)

Author keywords

Budesonide; Colonic delivery; Dexamethasone; Glucuronide; Prodrug; Ulcerative colitis

Indexed keywords

BUDESONIDE; CORTICOSTEROID; DEXAMETHASONE; GLUCURONIDE; PRODRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG DELIVERY SYSTEM; INTRAGASTRIC DRUG ADMINISTRATION; MALE; NONHUMAN; PHARMACOKINETICS; RAT; STEADY STATE; SUBCUTANEOUS DRUG ADMINISTRATION; ULCERATIVE COLITIS;

ANIMALS; ANTI-INFLAMMATORY AGENTS; BIOLOGICAL AVAILABILITY; BUDESONIDE; COLITIS, ULCERATIVE; COLON; DEXAMETHASONE; DISEASE MODELS, ANIMAL; DRUG DELIVERY SYSTEMS; GLUCOCORTICOIDS; GLUCURONATES; INJECTIONS, SUBCUTANEOUS; MALE; PRODRUGS; RATS; RATS, SPRAGUE-DAWLEY;

EID: 0030725321     PISSN: 01422782     EISSN: None     Source Type: Journal    
DOI: 10.1002/(SICI)1099-081X(199711)18:8<681::AID-BDD56>3.0.CO;2-A     Document Type: Article

References (23)

1. S. B. Hanauer, Medical therapy in ulcerative colitis. In Inflammatory Bowel Disease. 4th edn. J. B. Kirsner and R. G. Shorter (Eds), Williams and Wilkins, Baltimore, MD, 1995, pp. 664-694.
2. R Löftberg, New steroids for inflammatory bowel disease. Inflamm. Bowel Dis., 1, 135-141 (1995).
3. J. G. Hardy, J. N. C. Healey and J. R. Reynolds, Evaluation of an enteric-coated delayed release 5-aminosalicylic acid tablet in patients with inflammatory bowel disease. Aliment. Pharmacol. Ther., 1, 273-280 (1987).
4. M. Saffran, G. S. Kumar, C. Savariar, J. C. Burnham, F. Williams and D. C. Neckers, A new approach to the oral administration of insulin and other peptides. Science. 233, 1081-1084 (1986).
5. R system: a new oral dosage form for fast and complete release of drug after predetermined lag time. J. Controlled Rel., 31, 99-108 (1994).
6. R) in the gastro-intestinal tract using gamma scintigraphy. J. Clin. Pharmacol., 33, 712-718 (1993).
7. D. R. Friend and G. W. Chang, Drug glycosides: potential prodrugs for colon-specific drug delivery. J. Med. Chem., 28, 51-57 (1985).
8. B. Haeberlin, W. Rubas, H. W. Nolen III and D. R. Friend, In vitro evaluation of dexamethasone-ß-D-glucuronide for colon-specific drug delivery. Pharm. Res., 10, 1553-1562 (1993).
9. D. R. Friend, Glycosidases in colonie drug delivery. In Oral Colon-Specific Drug Delivery, D. R. Friend (Ed.), Chemical Rubber Company, Boca Raton, FL, 1992, pp. 153-187.
10. J. P. Brown, Hydrolysis of glycosides and esters. In Role of Gut Microflora in Toxicity and Cancer, I. R. Roland (Ed.), Academic, New York, 1988, pp. 109-144.
11. T. N. Tozer, J. Rigod, A. D. McLeod, R. Gungon, M. K. Hoag and D. R. Friend, Colon-specific delivery of dexamethasone from a glucoside prodrug in the guinea pig. Pharm. Res., 8, 445-454 (1991).
12. D. R. Friend, S. Phillips, A. McLeod and T. N. Tozer, Relative antiinflammatory effect of oral dexamethasone-ß-D-glucoside and dexamethasone in experimental inflammatory bowel disease. J. Pharm. Pharmacol., 43, 353-355 (1991).
13. R. N. Fedorak, B. Haeberlin, L. Empey, N. Cui, H. Nolen, L. D. Jewell and D. R. Friend, Colonic delivery of dexamethasone from a prodrug accelerates healing of experimental colitis without adrenal suppression. Gastroenterology. 108, 1688-1699 (1995).
14. R. N. Fedornk, N. Cui, D. R. Friend, K. L. Madsen and L. R. Empey, A novel colon-specific prodrug enhances sodium chloride absorption in rat colitis. Am. J. Physiol., 32, G210-G218 (1995).
15. H. Nolen III. R. N. Fedorak and D. R. Friend, Budesonide-ß-D-glucuronide: a potential prodrug for treatment of ulcerative colitis. J. Pharm. Sci., 84, 677-681 (1995).
16. R. N. Fedorak, Ningren Cui and D. R. Friend, A budesonide prodrug accelerates treatment of colitis in rats. Gut. 35, 1439-1446 (1994).
17. A. D. McLeod and T. N. Tozer, Kinetic perspectives in colonic drug delivery. In Oral Colon-Specific Drug Delivery, D. R. Friend (Ed.), Chemical Rubber Company, Boca Raton, FL, 1992, pp. 85-115.
18. A. D. McLeod, L. Tolentina and T. N. Tozer, Glucocorticoid dextran conjugates as potential prodrugs for colon-specific delivery: steady-state pharmacokinetics in the rat. Biopharm. Drug Disposit., 15, 151-161 (1994).
19. R. N. Fedorak, L. R. Empey, C. MacArthur and L. D. Jewell, Misoprostol provides a colonic mucosal protective effect during acetic-acid induced colitis in rats. Gastroenterology. 98, 615-625 (1990).
20. L. E. Fisher, E. A. Ludwig, J. A. Wald, R. R. Sloan, E. Middleton and W. J. Jusko, Pharmacokinetics and pharmacodynamics of methylprednisolone when administered at 8 AM versus 4 PM. Clin. Pharmacol. Ther., 51, 677-688 (1992).
21. F. Chanoine, C. Grenot, P. Heidmann and J. L. Junien, Pharmacokinetics of butixocort 21-proprionate, budesonide, and beclomethasone diproprionate in the rat after intratracheal, intravenous, and oral treatments. Drug Metab. Disposit., 19, 546-553 (1991).
22. C. S. Leopold and D. R. Friend, In vivo pharmacokinetic study for the assessment of pols(L-aspartic acid) as a drug carrier for colon-specific drug delivery. J. Pharmacokinet. Biopharm., 23, 397-406 (1995).
23. A. Ryrfeldt, P. Andersson, S. Edsbacker, M. Tonnesson, D. Davies and R. Pauwels, Pharmacokinetics and metabolism of budesonide, a selective glucocorticoid. Eur. J. Respir. Dis., 63, 86-95 (1982).