Oral bioavailability of mesna tablets.
To test the feasibility of uroprotection with sodium 2-mercaptoethane-sulfonate (mesna) in tablet form the bioavailability of mesna tablets was determined in healthy volunteers by HPLC. The area under the plasma concentration-time curve (AUC) of free mesna was significantly lower following oral (110 mumol.l-1 x h-1; 95% CI 98-122) than following i.v. administration of 1.2 g of mesna (201 mumol.l-1 x h-1; 95% CI 158-244). The AUC for total mesna, i.e. dimesna and mixed disulfides, however, were comparable in the two groups, with 628 (539-717) and 772 (713-831) mumol.l-1 x h-1, respectively. The mean residence time was significantly longer following oral mesna, at 79 (76-83) min vs 239 (229-250) min. Following oral mesna 51.1% (46.2-56.0%) of the administered dose was recovered in the urine in 24 h, compared with 60.6 (53.6-67.6)% in 4 h following i.v. mesna, and the average concentration of mesna in the urine exceeded 3 mmol.l-1 for 8 h. The data indicate that mesna in tablet form has an adequate bioavailability for uroprotection and therefore may be preferable to liquid mesna, which has an unpleasant taste. Oral mesna has a longer mean residence time than i.v. mesna, which means that uroprotection can be achieved with longer dosing intervals.
Stofer-Vogel
B
B
Department of Clinical Pharmacology, University of Berne, Switzerland.
Cerny
T
T
Borner
M
M
Lauterburg
B H
BH
D000284:Administration, Oral; D000328:Adult; D001682:Biological Availability; D005260:Female; D006801:Humans; D008297:Male; D015080:Mesna / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000652:urine; D010349:Patient Compliance; D013607:Tablets; D013649:Taste
D013607:Tablets; D015080:Mesna