A simple and rapid spectrofluorimetric method for determining the pharmacokinetics and metabolism of rhaponticin in rat plasma, feces and urine using a cerium probe

Abstract

Rhaponticin (RH) demonstrates a variety of pharmacological activities, including antitumor, antithrombotic and antioxidant effects. It is essential to establish a simple, rapid and reliable analytical method for determining the pharmacokinetics of RH. A simple cerium ion (Ce(3+)) probe method was developed and validated to determine RH in rat plasma, feces and urine. The fluorescence intensities of the cerium ion (Ce(3+)) were quenched by addition of RH, along with a remarkable red shift. Spectral data revealed that fluorescence quenching of Ce(3+) by RH was due to the formation of a Ce(3+)-RH complex. Using to the Stern-Volmer equation, the binding parameters for interactions between Ce(3+) and RH were obtained. Based on these, a rapid and simple spectrofluorimetric method was developed to determine the metabolism and pharmacokinetics of RH using a Ce(3+) probe. The assay was linear over the concentration range of 0.11-9.52, 0.25-8.87 and 0.18-9.10 μM for plasma, feces and urine, respectively and RH recoveries were found to be 98.24 ± 0.8, 97.78 ± 1.2 and 97.54 ± 0.8% for plasma, feces and urine, respectively. The relative standard deviations were < 9.5%. The spectrofluorimetric method was simple and rapid for quantitative determination of RH and its metabolism, and was affordable for most laboratories because of the fluorescence spectroscopy and low equipment cost. These pharmacokinetic, bioavailability and metabolism studies of RH will provide helpful information for the development of suitable dosage forms and clinical references on rational administration.

A review of alpha-glucosidase inhibitors from plants as potential candidates for the treatment of type-2 diabetes

“…The pharmacokinetic properties of rhaponticin were examined by different studies (Zhao et al 2011 ; Sun et al 2013 , 2016 ). Rhaponticin pharmacokinetics was studied in vivo in rats after oral (100 mg/kg) and intravenous (10 mg/kg) administration.…”

Rhaponticin as an anti-inflammatory component of rhubarb: a minireview of the current state of the art and prospects for future research

“…The pharmacokinetics of rhaponticin/rhapontigenin has been examined using various techniques, including UHPLC-Q-TOF/MS, UHPLC-DAD-MSn (Zhao et al 2012), or analysis after complexation with cerium (Ce 3? ) (Sun et al 2013) and erbium (Er 3? ) (Sun et al 2016) ions.…”

<p>Validated Microwell-Based Spectrofluorimetric Method for Quantification of Ravidasvir (New Anti-Chronic Hepatitis C Virus-GT4) in Rat Plasma and Its Application to Pharmacokinetic Study</p>

“…Because of the unpredictable idea of the matrix (regularly plasma or urine) and the requirement for high affectability to take note of concentrations after low dose administration over a significant time, PK is frequently examined utilizing the fluorescence spectrometry procedure. [10][11][12] Presently, there is an interest for the utilization of high sensitivity fluorescence spectrometry for microdosing analysis, which is viewed as a promising option in substitute to animal investigation. 10,11 Pilot research in our lab indicated the native fluorescence property of RAV.…”

“…[10][11][12] Presently, there is an interest for the utilization of high sensitivity fluorescence spectrometry for microdosing analysis, which is viewed as a promising option in substitute to animal investigation. 10,11 Pilot research in our lab indicated the native fluorescence property of RAV. The additional evaluation of this occurrence prompted the recommendation that the utilization of fluorescence spectrometry could be one of the suitable choices for the quantification of RAV in rat plasma.…”