title: Reduced Oral Bioavailability and Altered Pharmacokinetics of Saquinavir by Co-administration with Biochanin A in Rats.
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.
authors.affiliation: Department of Pharmacy, Peking University People's Hospital, Beijing, China.
authors.forename: J
authors.initials: J
authors.lastname: Li
authors.affiliation: Department of Pharmacy, Peking University People's Hospital, Beijing, China.
authors.forename: Y
authors.initials: Y
authors.lastname: Liu
authors.affiliation: Department of Pharmacy, Peking University People's Hospital, Beijing, China.
authors.forename: X
authors.initials: X
authors.lastname: Yu
authors.affiliation: Department of Pharmacy, Peking University People's Hospital, Beijing, China.
authors.forename: J
authors.initials: J
authors.lastname: Zhang
authors.affiliation: Department of Pharmacy, Peking University People's Hospital, Beijing, China.
authors.forename: J
authors.initials: J
authors.lastname: Gu
authors.affiliation: Department of Pharmacy, Beijing Children's Hospital, Capital Medical University, Beijing, China.
authors.forename: L
authors.initials: L
authors.lastname: Zhao
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D004347:Drug Interactions; D019833:Genistein / Q000494:pharmacology*; D008297:Male; D051381:Rats; D019258:Saquinavir / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*
chemical_list: D019833:Genistein; D019258:Saquinavir; C004541:biochanin A