Anzemet ยฎ (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 m
THE LACK EFFECT OF FOOD ON THE BIOAVAILABILITY OF NEFAZODONE TABLETS
โ Scribed by R. C. Dockens; D. S. Greene; R. H. Barbhaiya
- Publisher
- John Wiley and Sons
- Year
- 1996
- Tongue
- English
- Weight
- 471 KB
- Volume
- 17
- Category
- Article
- ISSN
- 0142-2782
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โฆ Synopsis
The objective of this study was to assess the effect of food on the pharmacokinetics of nefazodone (NEF). A group of 24 healthy adult male volunteers received a single 200 mg dose of NEF under fasting conditions as well as 5 min after a high-fat breakfast. There was a 1 week washout between treatments. Serial blood samples were collected for 48h after dosing and assayed by a validated HPLC method for NEF and the metabolites hydroxynefazodone (HO-NEF), m-chlorophenylpiperazine (mCPP), and triazoledione (dione). The mean (SD) peak concentration (C& for NEF was not affected by food and was 416 (220)ngmL-I and 446 (271)ngmL-' after the fed and fasted treatments, respectively. The median time to reach C,, (T,,) was also unaffected by food and was 2 h for both treatments. However, the mean (SD) area under the curve (AUC) was significantly reduced by food from 1815 (1017)nghmL-' to 1409 (695) ng hmL-'. Although there was an 18% decrease in NEF AUC when administered with food, food had no effect on C,, and T, , values for NEF, HO-NEF, mCPP or dione or AUC values for HO-NEF, mCPP, or dione, indicating that NEF can be administered without regard to meals.
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