Jaroslav Kvetina, Ilja Tacheci, Milan Nobilis, Marcela Kopacova, Martin Kunes and Jan Bures* Pages 1873 - 1876 ( 4 )
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 bioanalytical 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.Intestinal absorption window of xenobiotics, mesalazine, pharmacokinetic parameters, wireless capsule enteroscopy.
Second Department of Internal Medicine - Gastroenterology, Charles University Faculty of Medicine, University Hospital, Hradec Kralove, Second Department of Internal Medicine - Gastroenterology, Charles University Faculty of Medicine, University Hospital, Hradec Kralove, Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Charles University, Hradec Kralove, Second Department of Internal Medicine - Gastroenterology, Charles University Faculty of Medicine, University Hospital, Hradec Kralove, Biomedical Research Centre, University Hospital, Hradec Kralove, Department of Internal Medicine - Gastroenterology, University Hospital, Sokolska 581, 500 05 Hradec Kralove