Dosage forms of oral mesalazine and their clinical use

Česká verzia

Authors: M. Lapka
Authors place of work: Ústav farmakologie 3. LF UK, Praha
Published in the journal: Gastroent Hepatol 2023; 77(4): 342-346
Category:
doi: https://doi.org/10.48095/ccgh2023342

Summary

Mesalazine or 5-aminosalicylic acid is important substance which is used in therapy of inflammatory bowel disease (IBD), like ulcerative colitis (UC) and Crohn’s disease (CD). On the market, various mesalazine formulations for local (supositoria, rectal foam and enema) and for systemic administration (covered tablets, slow releasing tablets or slow releasing granulates) are available. Some differences between mesalazine formulations are enabling higher flexibility for clinical practice to choose the optimal drug in terms of distribution active drug according to disease activity and location. The pharmacokinetic profile of various mesalazine formulations and impact on the clinical practice are discussed in the text.

Keywords:

Ulcerative colitis – pharmacokinetics – inflammatory bowel diseases – mesalazine

Zdroje

1. Bantel H, Berg C, Vieth M et al. Mesalazine inhibits activation of transcription factor NF-kappaB in inflamed mucosa of patients with ulcerative colitis. Am J Gastroenterol 2000; 95 (12): 3452–3457. doi: 10.1111/j.1572-0241.2000.033 60.x.

2. Rousseaux C, Lefebvre B, Dubuquoy L et al. Intestinal antiinflammatory effect of 5-aminosalicylic acid is dependent on peroxisome proliferator-activated receptor-gamma. J Exp Med 2005; 201 (8): 1205–1215. doi: 10.1084/jem.20041948.

3. Schreiner P, Neurath MF, Ng SC et al. Mechanism-Based Treatment Strategies for IBD: Cytokines, Cell Adhesion Molecules, JAK Inhibitors, Gut Flora, and More. Inflamm Intest Dis 2019; 4 (3): 79–96. doi: 10.1159/000500721.

4. Annese V, Rogai F, Settesoldi A et al. PPARg in Inflammatory Bowel Disease. PPAR Res 2012; 2012: 620839. doi: 10.1155/2012/620839.

5. Moura M. Antioxidant effect of mesalazine in the experimental colitis model induced by acetic acid. J Coloproctol 2016; 36 (3). doi: 10.1016/ j.jcol.2016.03.003.

6. Feagan BG, Macdonald JK. Oral 5-aminosalicylic acid for maintenance of remission in ulcerative colitis. Cochrane Database Syst Rev 2012; 10: CD000544. doi: 10.1002/14651858.CD000544.pub3.

7. Klein S, Stein J, Dressman J. Site-specific delivery of anti-inflammatory drugs in the gastrointestinal tract: an in-vitro release model. J Pharm Pharmacol 2005; 57 (6): 709–719. doi: 10.1211/0022357056172.

8. Pentasa sachet, 4g. Státní ústav pro kontrolu léčiv. 2023 [online]. Dostupné z: https: //prehledy.sukl.cz/prehled_leciv.html#/detail-reg/0213250.

9. D‘Haens GR, Sandborn WJ, Zou G et al. Randomised non-inferiority trial: 1600 mg versus 400 mg tablets of mesalazine for the treatment of mild-to-moderate ulcerative colitis. Aliment Pharmacol Ther 2017; 46 (3): 292–302. doi: 10.1111/apt.14164.

10. Leifeld L, Pfützer R, Morgenstern J et al. Mesalazine granules are superior to Eudragit-L-coated mesalazine tablets for induction of remission in distal ulcerative colitis – a pooled analysis. Aliment Pharmacol Ther 2011; 34 (9): 1115–1122. doi: 10.1111/j.1365-2036.2011.04840.x.

11. Clemett D, Markham A. Prolonged-release mesalazine: a review of its therapeutic potential in ulcerative colitis and Crohn‘s disease. Drugs 2000; 59 (4): 929–956. doi: 10.2165/0000 3495-200059040-00016.

12. Salofalk granule s prodlouženým uvolňováním 1 500 mg. Státní ústav pro kontrolu léčiv. 2023 [online]. Dostupné z: https: //prehledy.sukl.cz/prehled_leciv.html#/detail-reg/0195899

13. Karkossa F, Klein S. A Biopredictive In Vitro Comparison of Oral Locally Acting Mesalazine Formulations by a Novel Dissolution Model for Assessing Intraluminal Drug Release in Individual Subjects. J Pharm Sci. 2018; 107 (6): 1680–1689. doi: 10.1016/j.xphs.2018.02.016.

14. Abinusawa A, Tenjarla S. Release of 5-Aminosalicylic Acid (5-ASA) from Mesalamine Formulations at Various pH Levels. Adv Ther 2015; 32 (5): 477–484. doi: 10.1007/s12325-015-0206-4.

15. Christensen LA, Slot O, Sanchez G et al. Release of 5-aminosalicylic acid from Pentasa during normal and accelerated intestinal transit time. Br J Clin Pharmacol. 1987; 23 (3): 365–369. doi: 10.1111/j.1365-2125.1987.tb03061.x.

16. Wilding IR. A scintigraphic study to evaluate what happens to PENTASA® and ASACOL® in the human gut. Pract Gastroenterol 1999; 1: 392–397.

17. Wilding IR, Kenyon CJ, Hooper G. Gastrointestinal spread of oral prolonged-release mesalazine microgranules (Pentasa) dosed as either tablets or sachet. Aliment Pharmacol Ther 2000; 14 (2): 163–169. doi: 10.1046/j.1365-2036. 2000.00696.x.

18. Rijk MC, van Schaik A, van Tongeren JH. Disposition of mesalazine from mesalazine-delivering drugs in patients with inflammatory bowel disease, with and without diarrhoea. Scand J Gastroenterol 1992; 27 (10): 863–868. doi: 10.3109/00365529209000155.

19. Newton A, Kumar N. IBD–Impact of Colonic pH, Onset of Action and other Factors in Modern Therapeutic Approach. Interdiscip J Microinflam 2014; 1 (2): 1–7. doi: 10.4172/ijm.1000116.

20. Sinha A, Ball DJ, Connor AL et al. Intestinal performance of two mesalamine formulations in patients with active ulcerative colitis as assessed by gamma scintigraphy. Pract Gastroenterol 2003; 27 (10): 56–69.

21. Ordás I, Eckmann L, Talamini M et al. Ulcerative colitis. Lancet 2012; 380 (9853): 1606–1619. doi: 10.1016/S0140-6736 (12) 60150-0.

22. De Vos M. Clinical Pharmacokinetics of Slow Release Mesalazine. Clin Pharmacokinet 2000; 39 (2): 85–97. doi: 0312-5963/00/0008-00 85/$20.00/0.

23. Satsangi J, Silverberg MS, Vermeire S et al. The Montreal classification of inflammatory bowel disease: controversies, consensus, and implications. Gut 2006; 55 (6): 749–753. doi: 10.1136/gut.2005.082909.

24. Texas Health and Human Services. 2021 [online]. Dostupné z: https: //www.hhs.texas.gov/sites/default/files/documents/about-hhs/ communications-events/meetings-events/dur/ july-2021-durb-agenda-item4aa.pdf

25. Patel D, Bertz R, Ren S et al. A Systematic Review of Gastric Acid-Reducing Agent-Mediated Drug-Drug Interactions with Orally Administered Medications. Clin Pharmacokinet 2020; 59 (4): 447–462. doi: 10.1007/s40262-019-008 44-3.

26. Deissler H, Krammer H, Gillessen A. pH-dependent vs. constant release of mesalazine in the treatment of ulcerative colitis: Do drug delivery concepts determine therapeutic efficacy? Biomed Rep 2021; 15 (5): 96. doi: 10.3892/br.2021.1472.

27. Flourié B, Hagège H, Tucat G et al. Randomised clinical trial: once- vs. twice-daily prolonged-release mesalazine for active ulcerative colitis. Aliment Pharmacol Ther 2013; 37 (8): 767–775. doi: 10.1111/apt.12266.

28. Dignass AU, Bokemeyer B, Adamek H et al. Mesalamine once daily is more effective than twice daily in patients with quiescent ulcerative colitis. Clin Gastroenterol Hepatol 2009; 7 (7): 762–769. doi: 10.1016/j.cgh.2009.04.004.

29. Hirayama M, Toda R, Ozaki T et al. Concentration dependence of 5-aminosalicylic acid pharmacological actions in intestinal mucosa after oral administration of a pH-dependent formulation. Mol Pharm 2011; 8 (4): 1083–1089. doi: 10.1021/mp200088z.

30. Murray A, Nguyen TM, Parker CE et al. Oral 5-aminosalicylic acid for induction of remission in ulcerative colitis. Cochrane Database Syst Rev 2020; 8 (8): CD000543. doi: 10.1002/14651858.CD000543.pub5.

31. Poturoglu S, Ormeci AC, Duman AE. Treatment of pregnant women with a diagnosis of inflammatory bowel disease. World J Gastroint Pharmacol Ther 2016; 7 (4): 490–502. doi: 10.4292/wjgpt.v7.i4.490.

32. Torres J, Chaparro M, Julsgaard M et al. European Crohn‘s and Colitis Guidelines on Sexuality, Fertility, Pregnancy, and Lactation. J Crohns Colitis 2023; 17 (1): 1–27. doi: 10.1093/ eccojcc/jjac115.

33. Farup PG, Hinterleitner TA, Lukás M et al. Mesalazine 4 g daily given as prolonged-release granules twice daily and four times daily is at least as effective as prolonged-release tablets four times daily in patients with ulcerative colitis. Inflamm Bowel Dis 2001; 7 (3): 237–242. doi: 10.1097/00054725-200108000-00009.

34. Nagahori M, Kochi S, Hanai H et al. Real life results in using 5-ASA for maintaining mild to moderate UC patients in Japan, a multi-center study, OPTIMUM Study. BMC Gastroenterol 2017; 17 (1): 47. doi: 10.1186/s12876-017-06 04-y.