You have full text access to this OnlineOpen article

Gastrointestinal transit and release of 5-aminosalicylic acid from 153Sm-labelled mesalazine pellets vs. tablets in male healthy volunteers

  1. M. Brunner1,
  2. R. Greinwald2,
  3. K. Kletter3,
  4. H. Kvaternik4,
  5. M. E. Corrado5,
  6. H. G. Eichler1,
  7. M. Müller1

Article first published online: 2 MAY 2003

DOI: 10.1046/j.1365-2036.2003.01564.x

Issue

Alimentary Pharmacology & Therapeutics

Alimentary Pharmacology & Therapeutics

Volume 17, Issue 9, pages 1163–1169, 1st May 2003

Additional Information

How to Cite

Brunner, M., Greinwald, R., Kletter, K., Kvaternik, H., Corrado, M. E., Eichler, H. G. and Müller, M. (2003), Gastrointestinal transit and release of 5-aminosalicylic acid from 153Sm-labelled mesalazine pellets vs. tablets in male healthy volunteers. Alimentary Pharmacology & Therapeutics, 17: 1163–1169. doi: 10.1046/j.1365-2036.2003.01564.x

Author Information

  1. 1

    Department of Clinical Pharmacology, Division of Clinical Pharmacokinetics, University of Vienna Medical School, Vienna, Austria;

  2. 2

    Dr Falk Pharma GmbH, Freiburg, Germany;

  3. 3

    Department of Nuclear Medicine, University of Vienna Medical School, Vienna, Austria;

  4. 4

    Austrian Research Centers Seibersdorf, Seibersdorf, Austria;

  5. 5

    CROSS S.A., Arzo, Switzerland

*Correspondence to: Dr M. Brunner, Department of Clinical Pharmacology, Division of Clinical Pharmacokinetics, University of Vienna Medical School, Allgemeines Krankenhaus, Währinger Gürtel 18–20, A-1090 Vienna, Austria. E-mail: martin.brunner@univie.ac.at

Publication History

  1. Issue published online: 2 MAY 2003
  2. Article first published online: 2 MAY 2003
  3. Accepted for publication 26 October 2002

SEARCH

SEARCH BY CITATION

ARTICLE TOOLS

View Full Article (HTML) Get PDF (171K)

Summary

Background : Mesalazine (5-aminosalicylic acid)-containing formulations, designed to optimize drug delivery to the ileo-caecal region, represent a cornerstone in the treatment of inflammatory bowel diseases.

Aim : To test, by means of pharmaco-scintigraphy, whether novel mesalazine-containing pellets release 5-aminosalicylic acid in the same target region as mesalazine tablets (Salofalk).

Methods : Fourteen healthy male volunteers received a single dose of either pellets or tablets containing 500 mg of mesalazine and 2 mg of 152Sm2O3 with a 1-week washout period. The gastrointestinal transit of 153Sm, incorporated into the formulations, was followed by gamma-scintigraphy. Mesalazine release was verified by assessing 5-aminosalicylic acid plasma pharmacokinetics.

Results : The formulations reached the ileo-caecal target region almost at the same time (3.3 ± 1 and 3.8 ± 1 h for pellets and tablets, respectively). Plasma 5-aminosalicylic acid tmax values were comparable and corresponded to the time during which the formulations were located in the target region. Plasma AUC values were significantly lower for pellets, which might be explained by a more prolonged release of 5-aminosalicylic acid.

Conclusions : Novel mesalazine pellets and Salofalk tablets release active 5-aminosalicylic acid in the same target region and pass through the gastrointestinal tract under fasting conditions in healthy volunteers in a comparable time. From a comparison of in vitro dissolution and plasma concentration data, a slower and more prolonged release of 5-aminosalicylic acid from pellets is suggested.

View Full Article (HTML) Get PDF (171K)