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The effect of food on the bioavailability of dolasetron mesylate tablets
Author(s) -
Lippert Christina,
Keung Anther,
Arumugham Thangam,
Eller Mark,
Hahne William,
Weir Scott
Publication year - 1998
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/(sici)1099-081x(199801)19:1<17::aid-bdd71>3.0.co;2-#
Subject(s) - bioavailability , cmax , bioequivalence , pharmacokinetics , confidence interval , medicine , vomiting , nausea , absorption (acoustics) , mesylate , pharmacology , zoology , chemistry , biology , physics , organic chemistry , acoustics
Abstract Anzemet® (dolasetron mesylate) is being developed for the prevention of chemotherapy‐induced emesis and postoperative nausea and vomiting. Twenty‐four healthy male subjects were orally dosed with dolasetron mesylate, 200 mg, after either an overnight fast or a high‐fat breakfast. The ratio of the mean area under the plasma concentration–time curve of the reduced active metabolite (MDL 74 156) to infinity (AUC(0–∞)) values in fed compared to fasting subjects was 86.3% with a 90% confidence interval for the ratio within (80, 125)%, indicating bioequivalence. The ratio of the mean MDL 74 156 maximum plasma concentration ( C max ) values was 70.6% in fed versus fasted subjects. The time to C max was statistically significantly longer after the high‐fat breakfast (mean values, 1.11 h fasting and 1.80 h fed), probably due to delayed gastric emptying. It may be concluded that, although the rate of absorption was somewhat delayed, the extent of absorption did not change significantly when dolasetron mesylate was given with food. © 1998 John Wiley & Sons, Ltd.