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<p>5-Aminosalicylic acid (5-ASA) has been shown to form complexes with α-, β- and γ-cyclodextrins (α-, β- and γ -CD) with a 1:1 composition, i.e., one molecule of α-, β- and γ-CD per one molecule of 5-ASA. The stability constants of the resulting complexes were calculated in the range 296-321 K. The thermodynamic parameters of complexation were determined. A method for the synthesis of the complexes was developed based on the obtained data. The antiulcer activity of one of the complexes (5-ASA···β-CD) was studied. Pharmacological studies (on models of acetylsalicylic and histamine ulcers) established that the 5-ASA··· β-CD complex at a dose of 50 mg/kg showed pronounced antiulcer activity comparable to that of the reference drug (carbenoxolone) at a dose of 100 mg/kg. This complex in a model of ulcers caused by indomethacin showed antiulcer activity comparable to the reference drug (omeprazole). At the same time, the amount of 5-ASA in the complex was only 12 wt% with β-CD accounting for the remaining 88 wt%.</p>

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Composition, Stability, and Antiulcer Activity of Complexes Formed by 5-Aminosalicylic Acid and Cyclodextrins

  • 期刊论文

  • 发表日期：

    2025年5月1日

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  • Yu. S. Zimin,
  • N. S. Borisova,
  • L. I. Murzakova,
  • A. R. Gimadieva

摘要

5-Aminosalicylic acid (5-ASA) has been shown to form complexes with α-, β- and γ-cyclodextrins (α-, β- and γ -CD) with a 1:1 composition, i.e., one molecule of α-, β- and γ-CD per one molecule of 5-ASA. The stability constants of the resulting complexes were calculated in the range 296-321 K. The thermodynamic parameters of complexation were determined. A method for the synthesis of the complexes was developed based on the obtained data. The antiulcer activity of one of the complexes (5-ASA···β-CD) was studied. Pharmacological studies (on models of acetylsalicylic and histamine ulcers) established that the 5-ASA··· β-CD complex at a dose of 50 mg/kg showed pronounced antiulcer activity comparable to that of the reference drug (carbenoxolone) at a dose of 100 mg/kg. This complex in a model of ulcers caused by indomethacin showed antiulcer activity comparable to the reference drug (omeprazole). At the same time, the amount of 5-ASA in the complex was only 12 wt% with β-CD accounting for the remaining 88 wt%.