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Inhibitory Effects of Multiple‐Dose Treatment with Baicalein on the Pharmacokinetics of Ciprofloxacin in Rats
Author(s) -
Hwang YounHwan,
Yang Hye Jin,
Kim DongGun,
Ma Jin Yeul
Publication year - 2017
Publication title -
phytotherapy research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.019
H-Index - 129
eISSN - 1099-1573
pISSN - 0951-418X
DOI - 10.1002/ptr.5728
Subject(s) - baicalein , ciprofloxacin , pharmacology , pharmacokinetics , scutellaria baicalensis , oral administration , bioavailability , medicine , antibacterial agent , rhodamine 123 , antibiotics , chemistry , multiple drug resistance , biochemistry , pathology , alternative medicine , traditional chinese medicine
Ciprofloxacin is used as a treatment for urinary and respiratory tract infections in clinical practice. Baicalein, a major flavonoid present in Scutellaria baicalensis , is a well‐known and potent antibacterial compound used in complementary and alternative medicine practices. The present study aimed to clarify the effects of multiple‐dose treatment with baicalein on the pharmacokinetics of ciprofloxacin in rats. Following the oral administration of baicalein (20, 40, or 80 mg/kg) for five consecutive days, the rats received an oral administration of ciprofloxacin (20 mg/kg). Blood samples were collected at specific time points, and the plasma concentrations of ciprofloxacin were determined by using high‐performance liquid chromatography. To evaluate the mechanisms underlying the interaction between baicalein and ciprofloxacin, a rhodamine 123 accumulation assay was performed in LS‐180 cells. A pharmacokinetic study revealed that multiple‐dose treatment with baicalein significantly decreased the peak serum concentration ( C max ), area under the curve ( AUC 0 → 480 min ), and relative bioavailability ( F rel ) of ciprofloxacin ( p < 0.05). The rhodamine 123 accumulation assay revealed that treatment with baicalein for 48 h markedly reduced the intracellular accumulation of rhodamine 123. Taken together, these findings suggest that baicalein may result in the therapeutic failure of ciprofloxacin or other quinolone‐based antibiotics used for chemotherapy in clinical practice. Copyright © 2016 John Wiley & Sons, Ltd.