Comparative pharmacokinetics of equimolar doses of 5-aminosalicylate administered as oral mesalamine (Asacol) and balsalazide: A randomized, single-dose, crossover study in healthy volunteers

Alimentary Pharmacology and Therapeutics

Volumn 19, Issue 10, 2004, Pages 1089-1098

  Sandborn, W J ^a   Hanauer, S B ^b   Buch, A ^c  

^a MAYO CLINIC   (United States)

^b UNIVERSITY OF CHICAGO   (United States)

^c PROCTER AND GAMBLE PHARMACEUTICALS   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

5 ACETAMIDOSALICYLIC ACID; BALSALAZIDE; MESALAZINE;

ADULT; AREA UNDER THE CURVE; BLOOD SAMPLING; BURN; CLINICAL TRIAL; CONFERENCE PAPER; CONSTIPATION; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DIARRHEA; DRUG ABSORPTION; DRUG BLOOD LEVEL; FEMALE; FLANK PAIN; GEOMETRY; HEADACHE; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN EXPERIMENT; MALE; MASS SPECTROMETRY; NORMAL HUMAN; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; RHINITIS; SINGLE BLIND PROCEDURE; TOOTH PAIN; URINALYSIS;

ADMINISTRATION, ORAL; ADULT; AMINOSALICYLIC ACIDS; ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL; ANTI-ULCER AGENTS; CROSS-OVER STUDIES; FEMALE; HUMANS; MALE; MESALAMINE; PHENYLHYDRAZINES;

EID: 2542553386     PISSN: 02692813     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.1365-2036.2004.01964.x     Document Type: Conference Paper

References (34)

1. Schroeder KW, Tremaine WJ, Ilstrup DM. Coated oral 5-aminosalicylic acid therapy for mildly to moderately active ulcerative colitis. A randomized study. N Engl J Med 1987; 317: 1625-9.
2. Sninsky CA, Cort DH, Shanahan F, et al. Oral mesalamine (Asacol) for mildly to moderately active ulcerative colitis. A multicenter study. Ann Intern Med 1991; 115: 350-5.
3. Levine DS, Riff DS, Pruitt R, et al. A randomized, double-blind, dose-response comparison of balsalazide (6.75 g), balsalazide (2.25 g), and mesalamine (2.4 g) in the treatment of active, mild-to-moderate ulcerative colitis. Am J Gastroenterol 2002; 97: 1398-407.
4. Pruitt R, Hanson J, Safdi M, et al. Balsalazide is superior to mesalamine in the time to improvement of signs and symptoms of acute mild-to-moderate ulcerative colitis. Am J Gastroenterol 2002; 97: 3078-86.
5. Green JR, Lobo AJ, Holdsworth CD, et al. Balsalazide is more effective and better tolerated than mesalamine in the treatment of acute ulcerative colitis. The Abacus Investigator Group. Gastroenterology 1998; 114: 15-22.
6. An oral preparation of mesalamine as long-term maintenance therapy for ulcerative colitis. A randomized, placebo-controlled trial. The Mesalamine Study Group. Ann Intern Med 1996; 124: 204-11.
7. Kruis W, Schreiber S, Theuer D, et al. Low dose balsalazide (1.5 g twice daily) and mesalazine (0.5 g three times daily) maintained remission of ulcerative colitis but high dose balsalazide (3.0 g twice daily) was superior in preventing relapses. Gut 2001; 49: 783-9.
8. Green JR, Mansfield JC, Gibson JA, Kerr GD, Thornton PC. A double-blind comparison of balsalazide, 6.75 g daily, and sulfasalazine, 3 g daily, in patients with newly diagnosed or relapsed active ulcerative colitis. Aliment Pharmacol ther 2002; 16: 61-8.
9. Mansfield JC, Giaffer MH, Cann PA, McKenna D, Thornton PC, Holdsworth CD. A double-blind comparison of balsalazide, 6.75 g, and sulfasalazine, 3 g, as sole therapy in the management of ulcerative colitis. Aliment Pharmacol ther 2002; 16: 69-77.
10. Green JR, Gibson JA, Kerr GD, et al. Maintenance of remission of ulcerative colitis: a comparison between balsalazide 3 g daily and mesalazine 1.2 g daily over 12 months. ABACUS Investigator group. Aliment Pharmacol ther 1998; 12: 1207-16.
11. Peppercorn MA, Goldman P. The role of intestinal bacteria in the metabolism of salicylazosulfapyridine. J Pharmacol Exp ther 1972; 181: 555-62.
12. Allgayer H, Ahnfelt NO, Kruis W, et al. Colonic N-acetylation of 5-aminosalicylic acid in inflammatory bowel disease. Gastroenterology 1989; 97: 38-41.
13. Ireland A, Priddle JD, Jewell DP. Acetylation of 5-aminosalicylic acid by isolated human colonic epithelial cells. Clin Sci (Lond) 1990; 78: 105-11.
14. Goebell H, Klotz U, Nehlsen B, Layer P. Oroileal transit of slow release 5-aminosalicylic acid. Gut 1993; 34: 669-75.
15. Layer PH, Goebell H, Keller J, Dignass A, Klotz U. Delivery and fate of oral mesalamine microgranules within the human small intestine. Gastroenterology 1995; 108: 1427-33.
16. Zhou SY, Fleisher D, Pao LH, Li C, Winward B, Zimmermann EM. Intestinal metabolism and transport of 5-aminosalicylate. Drug Metab Dispos 1999; 27: 479-85.
17. Staerk Laursen L, Stokholm M, Bukhave K, Rask-Madsen J, Lauritsen K. Disposition of 5-aminosalicylic acid by olsalazine and three mesalazine preparations in patients with ulcerative colitis: comparison of intraluminal colonic concentrations, serum values, and urinary excretion. Gut 1990; 31: 1271-6.
18. Stretch GL, Campbell BJ, Dwarakanath AD, et al. 5-amino salicylic acid absorption and metabolism in ulcerative colitis patients receiving maintenance sulphasalazine, olsalazine or mesalazine. Aliment Pharmacol ther 1996; 10: 941-7.
19. Johnson LK, Pruitt RE, Green JR. Treatment of ulcerative colitis with balsalazide: response to editorial by Drs. Farrell and Peppercorn and letter to the editor by Dr. Hanauer [comment]. Am J Gastroenterol 2003; 98: 216-9.
20. COSTART: Coding Symbols for Thesaurus of Adverse Reaction Terms, 5th edn. Department of Health and Human Services, Food and Drug Administration (FDA), 1995.
21. Corey AE, Rose GM, Conklin JD. Bioavailability of single and multiple doses of enteric-coated mesalamine and sulphasalazine. J Int Med Res 1990; 18: 441-53.
22. Colazide Monograph. 2nd edn. Oxford: Caudex Medical, Oxford Centre for Innovation, 1998.
23. Hussain FN, Ajjan RA, Kapur K, Moustafa M, Riley SA. Once versus divided daily dosing with delayed-release mesalazine: a study of tissue drug concentrations and standard pharmacokinetic parameters. Aliment Pharmacol ther 2001; 15: 53-62.
24. Hussain FN, Ajjan RA, Riley SA. Dose loading with delayed-release mesalazine: a study of tissue drug concentrations and standard pharmacokinetic parameters. Br J Clin Pharmacol 2000; 49: 323-30.
25. Chan RP, Pope DJ, Gilbert AP, Sacra PJ, Baron JH, Lennard-Jones JE. Studies of two novel sulfasalazine analogs, ipsalazide and balsalazide. Dig Dis Sci 1983; 28: 609-15.
26. Sandborn WJ, Hanauer SB. Systematic review: the pharmacokinetic profiles of oral mesalazine formulations and mesalazine pro-drugs used in the management of ulcerative colitis. Aliment Pharmacol ther 2003; 17: 29-42.
27. Rijk MC, van Schaik A, van Tongeren JH. Disposition of 5-aminosalicylic acid by 5-aminosalicylic acid-delivering compounds. Scand J Gastroenterol 1988; 23: 107-12.
28. Rijk MC, van Schaik A, van Tongeren JH. Disposition of 5-aminosalicylic acid by 5-aminosalicylic acid-delivering compounds. Scand J Gastroenterol Suppl 1988; 148: 54-9.
29. Christensen LA, Fallingborg J, Abildgaard K, et al. Topical and systemic availability of 5-aminosalicylate: comparisons of three controlled release preparations in man. Aliment Pharmacol ther 1990; 4: 523-33.
30. Christensen LA. 5-Aminosalicylic acid containing drugs. Delivery, fate, and possible clinical implications in man. Dan Med Bull 2000; 47: 20-41.
31. Fallingborg J, Christensen LA, Jacobsen BA, Rasmussen SN. Very low intraluminal colonic pH in patients with active ulcerative colitis. Dig Dis Sci 1993; 38: 1989-93.
32. Nugent SG, Kumar D, Rampton DS, Evans DF. Intestinal luminal pH in inflammatory bowel disease: possible determinants and implications for therapy with aminosalicylates and other drugs. Gut 2001; 48: 571-7.
33. Press AG, Hauptmann IA, Hauptmann L, et al. Gastrointestinal pH profiles in patients with inflammatory bowel disease. Aliment Pharmacol ther 1998; 12: 673-8.
34. Ewe K, Schwartz S, Petersen S, Press AG. Inflammation does not decrease intraluminal pH in chronic inflammatory bowel disease. Dig Dis Sci 1999; 44: 1434-9.