Acta Pharm. 66 (2016) 563-568
Short communication
Pharmacokinetic evaluation of the interaction between oral
kaempferol and ethanol in rats
ZHAOXIANG ZHOU, MENG WANG, ZENGJUN GUO and XIAOYING ZHANG
1 College of Veterinary Medicine, Northwest A&F
University, Yangling, Shaanxi 712100,
China
2 Medical College of Xi’an Jiaotong
University, Xi’an, Shaanxi 710061, China
Accepted July 25, 2016
Published online August 2,
2016
This study was aimed at investigating the effect of ethanol on oral bioavailability of kaempferol in rats, namely, at disclosing their possible interaction. Kaempferol (100 or 250 mg kg–1 bm) was administered to the rats by oral gavage with or without ethanol (600 mg kg–1 bm) co-administration. Intravenous administration (10 and 25 mg kg–1 bm) of kaempferol was used to determine the bioavailability. The concentration of kaempferol in plasma was estimated by ultra high performance liquid chromatography. During co-administration, significant increase of the area under the plasma concentration-time curve as well as the peak concentration were observed, along with a dramatic decrease in total body clearance. Consequently, the bioavailability of kaempferol in oral control groups was 3.1 % (100 mg kg–1 bm) and 2.1 % (250 mg kg–1 bm). The first was increased by 4.3 % and the other by 2.8 % during ethanol co-administration. Increased permeability of cell membrane and ethanol-kaempferol interactions on CYP450 enzymes may enhance the oral bioavailability of kaempferol in rats.
Keywords: kaempferol, bioavailability,
pharmacokinetics, ethanol, cytochrome P450s