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Oral bioavailability of mesna tablets
B Stofer-Vogel1, T Cerny, M Borner
1Department of Clinical Pharmacology, University of Berne, Switzerland.
Cancer Chemotherapy and Pharmacology
|January 1, 1993
Summary
Oral mesna tablets offer adequate bioavailability for uroprotection, providing a palatable alternative to liquid mesna. This formulation allows for longer dosing intervals due to increased mean residence time.
Area of Science:
- Pharmacology
- Urology
Background:
- Sodium 2-mercaptoethane-sulfonate (mesna) is used for uroprotection.
- The oral bioavailability and efficacy of mesna in tablet form require investigation.
Purpose of the Study:
- To assess the feasibility of uroprotection using mesna tablets.
- To determine the bioavailability of mesna administered orally versus intravenously.
Main Methods:
- Healthy volunteers received 1.2 g of mesna orally (tablets) or intravenously.
- Plasma mesna concentrations were analyzed using High-Performance Liquid Chromatography (HPLC).
- Urinary excretion and residence time were measured.
Main Results:
- Oral mesna showed significantly lower free mesna AUC compared to i.v. administration.
- Total mesna AUC was comparable between oral and i.v. routes.
- Oral mesna exhibited a longer mean residence time and adequate urinary recovery for uroprotection.
Conclusions:
- Mesna tablets demonstrate adequate bioavailability for uroprotection.
- Oral mesna offers a more palatable option than liquid formulations.
- The extended residence time of oral mesna supports longer dosing intervals for effective uroprotection.