In Vitro and In Vivo Evaluation of the Effect of Puerarin on Hepatic Cytochrome P450-Mediated Drug Metabolism

Kim, Sang-Bum; Yoon, In‐Soo; Kim, Kyu-Sang; Cho, Sung-Jun; Kim, Yeong Shik; Cho, Hyun‐Jong; Chung, Suk‐Jae; Chong, Samuel S.; Kim, Dae‐Duk

doi:10.1055/s-0034-1368350

Cited by 38 publications

(39 citation statements)

References 29 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Kim et al . () carried out an in vitro investigation to determine the CYP inhibitory potential of puerarin on variety of substrates using human and rat liver microsomes. The probe substrates consisted of diclofenac, dextromethorphan, testosterone and phenacetin for CYP2C, CYP2D, CYP3A and CYP1A, respectively.…”

Section: Individual Case Studies Of Flavonoidsmentioning

confidence: 97%

See 1 more Smart Citation

Recent trends in preclinical drug–drug interaction studies of flavonoids — Review of case studies, issues and perspectives

Srinivas¹

2015

Phytotherapy Research

View full text Add to dashboard Cite

Because of health benefits that are manifested across various disease areas, the consumption of herbal products and/or health supplements containing different kinds of flavonoids has been on the rise. While the drug-drug interaction potential between flavonoids and co-ingested drugs still remain an issue, opportunities exist for the combination of flavonoids with suitable anti-cancer drugs to enhance the bioavailability of anti-cancer drugs and thereby reduce the dose size of the anti-cancer drugs and improve its therapeutic index. In recent years, scores of flavonoids have undergone preclinical investigation with variety of drugs encompassing therapeutic areas such as oncology (etoposide, doxorubicin, paclitaxel, tamoxifen etc.), immunosuppression (cyclosporine) and hypertension (losartan, felodipine, nitrendipine etc.). The review provides examples of the recent trends in the preclinical investigation of 14 flavonoids (morin, quercetin, silibinin, kaempferol etc.) with various co-administered drugs. The relevance of combination of flavonoids with anti-cancer drugs and a framework to help design the in vitro and in vivo preclinical studies to gain better mechanistic insights are discussed. Also, concise discussions on the various physiological factors that contribute for the reduced bioavailability of flavonoids along with the significant challenges in the data interpretation are provided.

show abstract

Section: Individual Case Studies Of Flavonoidsmentioning

confidence: 97%

“…Regardless of buspirone dosing route, puerarin caused an inhibition of buspirone metabolism resulting in a higher oral bioavailability. Hence, the CYP3A related inhibitory potential of puerarin was unequivocally demonstrated after a mere single intravenous dose administration (Kim et al ., ).…”

Section: Individual Case Studies Of Flavonoidsmentioning

confidence: 99%

Recent trends in preclinical drug–drug interaction studies of flavonoids — Review of case studies, issues and perspectives

Srinivas¹

2015

Phytotherapy Research

View full text Add to dashboard Cite

show abstract

“…The femoral artery and vein of the rats were cannulated with a polyethylene tube (Becton Dickinson Diagnostics, Sparks, MD, U.S.A.) under anesthesia with Zoletil (20 mg/kg, intramuscular injection) (Virbac, Carros, France). 15) Rats were given a single intravenous dose (via the femoral vein; 5 mg/ kg) or an oral dose (using a feeding tube; 20 mg/kg) of buspirone (dissolved in normal saline). An approximately 250 µL aliquot of blood samples was collected via the femoral artery at predetermined time points (0, 1, 5, 15, 30, 45, 60, 90, 120, 180 min for the intravenous study; 0, 2, 5, 10, 15, 20, 30, 45, 60, 90, 120 min for the oral study).…”

Section: Methodsmentioning

confidence: 99%

“…12,15) However, in these previous studies, full bioanalytical method validation data were not provided, and chromatographic conditions and sample preparation procedures were randomly selected without optimization. Moreover, the sensitivity of our previous methods (LOQ=100 ng/ mL) was not sufficient for lower-dose preclinical study, which needed further improvement.…”

Section: Representative Chromatograms Of Buspirone and Is In Rat Plmentioning

confidence: 99%

Development of HPLC Method for the Determination of Buspirone in Rat Plasma Using Fluorescence Detection and Its Application to a Pharmacokinetic Study

et al. 2016

Self Cite

View full text Add to dashboard Cite

A simple and sensitive analytical method for the quantitative determination of buspirone in rat plasma by HPLC with fluorescence detection was developed and validated using naproxen as an internal standard. A relatively small-volume (150 µL) aliquot of rat plasma sample was prepared by a simple deproteinization procedure using acetonitrile as a precipitating organic solvent. Chromatographic separation was performed using Kinetex ® C8 column with an isocratic mobile phase consisting of acetonitrile and 10-mM potassium phosphate buffer (pH 6.0) at a flow rate of 1.0 mL/min. The eluent was monitored by fluorescence detector at a wavelength pair of 237/380 nm (excitation/emission). The linearity was established at 20.0-5000 ng/ mL, and the limit of detection was 6.51 ng/mL. The precision (≤14.6%), accuracy (89.2-108%), and stability (89.1-101%) were within acceptable ranges. The newly developed method was successfully applied to intravenous and oral pharmacokinetic studies of buspirone in rats.Key words buspirone; HPLC; fluorescence detection; rat plasma; pharmacokinetics [4,5] decane-7,9-dione), an azapirone, is an antianxiety agent that has dopaminergic, noradrenergic, and serotonin-modulating activity.1) It is chemically unrelated to benzodiazepines or barbiturates, and it exerts a pharmacologically unique anxiolytic effect without sedative, muscle relaxant, and anticonvulsant properties.2,3) Oral buspirone formulation (e.g., Buspar ® ) is currently used in the treatment of anxiety disorders and the short-term relief of the symptoms of anxiety. 4) Orally administered buspirone is rapidly absorbed but it undergoes first-pass metabolism, resulting in a low bioavailability of less than 5%. 5,6) Buspirone is metabolized primarily by CYP450 3A4-mediated oxidation. 7,8) However, little information is available regarding important pharmacokinetic issues that include the exact reason for the low bioavailability, kinetics of organ clearance, and mechanisms of elimination of buspirone in animals or humans.9) Therefore, development of analytical tools for quantification of buspirone in various biological fluids will contribute to the progress of mechanistic pharmacokinetic and pharmacological studies of buspirone in a pre-clinical or clinical setting.A few analytical methods have been reported for the determination of buspirone in human plasma by HPLC with ultraviolet spectrophotometry (UV) method 2) and HPLC with tandem mass spectrometry (HPLC-MS/MS) method, 8,10) and in rabbit serum by HPLC-UV method.5) However, these methods have several limitations such as a relatively large sample volume (i.e., 500 µL) and costly and/or laborious sample preparation procedures that include a liquid-liquid or solid phase extraction. Moreover, mass spectrometry requires relatively expensive equipment and highly skilled technical expertise, which may not always be feasible for most laboratories in resource-limited settings.11) Previously, we reported the plasma concentration versus time profiles of buspirone in rats using a HPLC-UV method ...

show abstract

“…22) Control or 1,25(OH) 2 D 3 -treated rats (n=4 in each group) were given a single intravenous dose (15 µmol/kg as adefovir) of [ In Situ Closed Loop Study in Rats In situ closed loop study was conducted as previously reported. [23][24][25] Briefly, after a minimal abdominal incision was made under light ether anesthetization and the contents within the gastrointestinal (GI) tract were sufficiently washed, a 5-cm long duodenum, jejunum or ileum loop was closed by ligation approximately 2 cm distal to both ends of each intestinal section.…”

Section: Methodsmentioning

confidence: 99%

Effects of 1α,25-Dihydroxyvitamin D<sub>3</sub> on Intestinal Absorption and Disposition of Adefovir Dipivoxil and Its Metabolite, Adefovir, in Rats

Yoon

Son

Kim

et al. 2015

Biological & Pharmaceutical Bulletin

Self Cite

View full text Add to dashboard Cite

The aim of this study was to investigate the effect of 1α,25-dihydroxyvitamin D 3 (1,25(OH) 2 D 3 ), an active form of vitamin D, on the oral absorption and disposition of adefovir dipivoxil (P-glycoprotein (P-gp) substrate) and its major active metabolite, adefovir (multidrug resistance-associated protein 4 (Mrp4) substrate), in rats. The pharmacokinetics of intravenous adefovir and oral adefovir dipivoxil was evaluated in control and 1,25(OH) 2 D 3 -treated rats. The intestinal absorption of adefovir dipivoxil was investigated through an in situ closed loop study, and the tissue distribution of adefovir after oral administration of adefovir dipivoxil was evaluated in the two groups. There was no significant difference in pharmacokinetic parameters of intravenous adefovir between the two groups. Importantly, the total area under the plasma concentration-time curve from time zero to time infinity (AUC), peak plasma concentration (C max ) and extent of absolute oral bioavailability (F) of adefovir after oral administration of adefovir dipivoxil were significantly higher in 1,25(OH) 2 D 3 -treated rats than in control rats. In the in situ closed loop study, there was no significant difference in the remaining fraction of adefovir dipivoxil in the duodenum, jejunum and ileum loops between the two groups. In the tissue distribution study after oral administration of adefovir dipivoxil, the tissue-toplasma partition coefficients of adefovir in the liver, brain, kidney, and intestine were significantly lower in 4) During the past decades, significant physiological roles of VDR in calcium and bone homeostasis have been well established. 5)However, it is increasingly recognized that VDR is also crucial in the regulation of drug transporters, and 1,25(OH) 2 D 3 can lead to VDR-mediated changes in target genes of drug transporters. [6][7][8][9][10] Since VDR is abundantly expressed in the intestine, 11) the effects of 1,25(OH) 2 D 3 (i.e., VDR activation) on the expression of intestinal drug transporters are frequently investigated. 1,25(OH) 2 D 3 increases the mRNA expression and function of multidrug resistance protein 1 (MDR1) in the human colorectal adenocarcinoma cell lines, LS174T and Caco-2 cells in vitro. 8,12) It also increases the protein expressions of multidrug resistance-associated protein 2 and 4 (MRP2 and MRP4) in Caco-2 cells. 8,13) In rats, 1,25(OH) 2 D 3 treatment in vivo increases the protein expressions of Mrp2, Mrp3, Mrp4, and the oligopeptide transporter 1 (PepT1) without altering the mRNA and protein expressions of Mdr1a (P-glycoprotein; P-gp). 14)Moreover, our previous studies using rat everted intestinal sac technique confirmed that the in vitro functions of rat intestinal Mrp2, Mrp4 and PepT1, but not P-gp are induced by 1,25(OH) 2 D 3 treatment via VDR activation. 15) However, changes in the expression and/or in vitro functions of drug transporters do not always correlate with the fates of therapeutic agents in the whole body system. Therefore, further studies are needed on the effects of 1,25(O...

show abstract

In Vitro and In Vivo Evaluation of the Effect of Puerarin on Hepatic Cytochrome P450-Mediated Drug Metabolism

Cited by 38 publications

References 29 publications

Recent trends in preclinical drug–drug interaction studies of flavonoids — Review of case studies, issues and perspectives

Recent trends in preclinical drug–drug interaction studies of flavonoids — Review of case studies, issues and perspectives

Development of HPLC Method for the Determination of Buspirone in Rat Plasma Using Fluorescence Detection and Its Application to a Pharmacokinetic Study

Effects of 1α,25-Dihydroxyvitamin D<sub>3</sub> on Intestinal Absorption and Disposition of Adefovir Dipivoxil and Its Metabolite, Adefovir, in Rats

Contact Info

Product

Resources

About