THE LACK EFFECT OF FOOD ON THE BIOAVAILABILITY OF NEFAZODONE TABLETS

Abstract

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 (Cmax) 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 Cmax (Tmax ) 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 Cmax and Tmax 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.