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THE LACK EFFECT OF FOOD ON THE BIOAVAILABILITY OF NEFAZODONE TABLETS
Author(s) -
Dockens R. C.,
Greene D. S.,
Barbhaiya R. H.
Publication year - 1996
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(199603)17:2<135::aid-bdd947>3.0.co;2-k
Subject(s) - cmax , pharmacokinetics , bioavailability , pharmacology , nefazodone , area under the curve , dosing , chemistry , high performance liquid chromatography , plasma concentration , food intake , zoology , medicine , chromatography , biology , receptor , serotonin , fluoxetine
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 48 h 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 max ) for NEF was not affected by food and was 416 (220) ng mL −1 and 446 (271) ng mL −1 after the fed and fasted treatments, respectively. The median time to reach C max ( T max ) 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) ng h mL −1 to 1409 (695) ng h mL −1 . Although there was an 18% decrease in NEF AUC when administered with food, food had no effect on C max and T max 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.