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Drug Res (Stuttg) 2016; 66(09): 484-488
DOI: 10.1055/s-0042-110393
Original Article
© Georg Thieme Verlag KG Stuttgart · New York

Reduced Oral Bioavailability and Altered Pharmacokinetics of Saquinavir by Co-administration with Biochanin A in Rats

J. Li
1   Department of Pharmacy, Peking University People’s Hospital, Beijing, China
2   Department of Pharmacy Administration and Clinical Pharmacy, School of Pharmaceutical Sciences, Peking University, Beijing, China
,
Y. Liu
1   Department of Pharmacy, Peking University People’s Hospital, Beijing, China
2   Department of Pharmacy Administration and Clinical Pharmacy, School of Pharmaceutical Sciences, Peking University, Beijing, China
,
X. Yu
1   Department of Pharmacy, Peking University People’s Hospital, Beijing, China
2   Department of Pharmacy Administration and Clinical Pharmacy, School of Pharmaceutical Sciences, Peking University, Beijing, China
,
J. Zhang
1   Department of Pharmacy, Peking University People’s Hospital, Beijing, China
2   Department of Pharmacy Administration and Clinical Pharmacy, School of Pharmaceutical Sciences, Peking University, Beijing, China
,
J. Gu
1   Department of Pharmacy, Peking University People’s Hospital, Beijing, China
,
L. Zhao
3   Department of Pharmacy, Beijing Children’s Hospital, Capital Medical University, Beijing, China
› Author Affiliations
Further Information

Publication History

received 28 April 2016

accepted 11 June 2016

Publication Date:
13 July 2016 (online)

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Abstract

The study was aim to assess the impact of biochanin A on the oral bioavailability and pharmacokinetics (PK) of saquinavir (SQV), a substrate of P-glycoprotein (P-gp), in rats. 10 male rats were randomized into 2 groups of equal size, and administered orally 30 mg/kg SQV with or without 20 mg/kg biochanin A. The PK of SQV was assessed using non-compartmental analysis. Results revealed that the area under the plasma concentration-time curve of SQV from time zero to time infinity (AUC0-∞) was reduced by 51.39% by biochanin A (P=0.038); while the apparent systemic clearance (CL/F) was increased by 87.62% (P=0.028). Double peak phenomenon was observed in the plasma SQV profiles. Biochanin A increased the first peak, yet decreased the second peak of plasma SQV levels. Our study demonstrates that biochanin A can significantly reduce SQV oral bioavailability and alter SQV PK profiles in rats. Findings in this study suggest a precaution in the clinic when SQV is administered with dietary/herbal supplements that contain biochanin A.

Key words

absorption - antiviral drugs - drug-drug interaction - P-glycoprotein
 

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