4.5 Article

The Importance of Wireless Capsule Endoscopy for Research into the Intestin Absorption Window of 5-Aminosalicylic Acid in Experimental Pigs

期刊

CURRENT PHARMACEUTICAL DESIGN
卷 23, 期 12, 页码 1873-1876

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BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1381612822666161201145247

关键词

Intestinal absorption window of xenobiotics; mesalazine; pharmacokinetic parameters; wireless capsule enteroscopy

资金

  1. Charles University [PRVOUK 37-08]

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Background: Absorption windows in particular segments of the small intestine can contribute to the development of orally administered drug formulations and can limit the bioavailability of released compounds. Objective: The aim of this study was to evaluate use of wireless capsule enteroscopy regarding the disintegration kinetic process of tablets in the small intestine and its comparison with the levels of the model drug (5-aminosalicylic acid; 5-ASA), and its majority metabolite (N-acetyl-5-aminosalicylic acid; N-acetyl-5-ASA) in blood plasma. Methods: Tablets were endoscopically introduced into the duodenum and their disintegration was monitored using wireless capsule enteroscopy in anaesthetised pigs. In parallel, blood plasma time profiles of the model drug (5-ASA) released from tablets and its metabolite (N-acetyl-5-ASA) were detected. Results: The disintegration of tablets was evident in the proximal jejunum (until the 90-minute mark) and culminated at the 3rd hour. The maximum plasmatic concentration of 5-ASA was reached at the 3rd hour and in the case of its metabolite (N-acetyl-5-ASA) at the 4th hour. Conclusion: The study demonstrated the advantage of combination of wireless capsule enteroscopy and bio-analytical determination of pharmacokinetic parameters in an animal experiment to localise the disintegration site of solid dosage form and following kinetics of intestinal absorption of the released active agent.

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