The balance of indications for use and pharmaceutical properties of mesalazine in modern gastroenterological practice

Inflammatory bowel diseases (IBD) – ulcerative colitis (UC) and Crohnʼs disease (CD) represent a significant medical and social problem, with the number of patients continuing to rise worldwide. Mesalazine (5-aminosalicylic acid, 5-ASA) has for several decades held a leading position in the pharmacotherapy of both conditions. However, the evidence accumulated to date indicates that its efficacy differs fundamentally between UC and CD, and mesalazine has been excluded from clinical guidelines for CD both in Russia and internationally. This review focuses on the etiology, pathogenesis, and classification of IBD; the history of mesalazineʼs development and its mechanisms of action; the characteristics of its dosage forms; and a comparative analysis of the composition of enteric coatings designed to release mesalazine either in the small intestine – typically affected in CD – or in the large intestine, affected in UC. Thus, in the manufacture of enteric coatings for medicinal products whose active substance is intended to be released in the small intestine, a number of pH-dependent polymers are used, among which the most widely applied is a copolymer of methacrylic acid and ethyl acrylate [1:1]. Release of active substances in the large intestine is achieved through the use of enteric coatings based on a copolymer of methacrylic acid and methyl methacrylate [1:1]. On the Russian pharmaceutical market, mesalazine formulations are available with both types of polymers, which was relevant when the drug was used in the treatment of Crohn’s disease and ulcerative colitis. At present, the restriction of mesalazine use in Crohn’s disease raises the question of the appropriateness of using mesalazine in enteric dosage forms with the methacrylic acid-ethyl acrylate copolymer [1:1] for any indications. Current clinical guidelines on IBD are also examined with regard to whether the mesalazine preparations registered in the Russian Federation are suitable for use in CD and UC.

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