Effects of quercetin on pharmacokinetics of cefprozil in Chinese-Han male volunteers

Abstract

1. The primary objective of this study was to evaluate the effects of quercetin on the pharmacokinetics of cefprozil. The secondary objective was to evaluate the safety of the combined use of cefprozil and quercetin.

2. An open-label, two-period, crossover phase I trial among 24 Han Chinese male subjects was conducted. Participants were given 500 mg of quercetin orally once daily for 15 d followed by single dose of cefprozil (500 mg) on day 15. Serum concentrations of cefprozil were then measured in all participants on day 15. A 15-d washout period was then assigned after which a 500 mg dose of cefprozil was administered and measured in the serum on day 36.

3. All subjects completed the trial, and no serious adverse events were reported. We measured mean serum concentrations of cefprozil in the presence and absence of quercetin in all participants. The maximum serum concentration of cefprozil in the presence of quercetin was 8.18 ug/ml (95% CI: 7.55–8.81) versus a maximum cefprozil concentration of 8.35 ug/ml (95% CI: 7.51–9.19) in the absence of quercetin. We conclude that the concurrent use of quercetin has no substantial effect on serum concentrations of orally administered cefprozil.

4. Co-administration of quercetin showed no statistically significant effects on the pharmacokinetics of cefprozil in healthy Chinese subjects.

• Drug–drug interaction
• healthy subjects
• pharmacokinetics
• quercetin
• transporters

Acknowledgements

We would like to thank Dr. Howard L. McLeod, Medical Director, The DeBartolo Family Personalized Medicine Institute Moffitt Cancer Center, for his contribution of this manuscript. We thank the volunteers who participated in this study and their families. We also thank Meng-Xue Ge, Tao Zhang, Chong-zhen Qin, Lei Hu and Dao-yu Zhang for assistance with volunteer recruitment and the clinical information collection process.

Declaration of interest

This work was supported by the Department of Clinical Pharmacology, Xiangya Hospital, and Central South University. All authors declare that they have no potential competing interests.