A simple and rapid spectrofluorimetric method for determining the pharmacokinetics and metabolism of rhaponticin in rat plasma, feces and urine using a cerium probe.
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.
Department of Chemistry & Chemical Engineering, Xi'an University of Arts and Science, Xi'an, Shaanxi 710069, China. 66160692@qq.com
Yang
Y
Sun
Yingyong
Y
Zhao
Xiaohui
X
Yang
D002563:Cerium / Q000737:chemistry*; D005456:Fluorescent Dyes / Q000032:analysis* / Q000737:chemistry; D006863:Hydrogen-Ion Concentration; D008968:Molecular Conformation; D013050:Spectrometry, Fluorescence / Q000379:methods*; D013267:Stilbenes / Q000032:analysis* / Q000097:blood / Q000378:metabolism / Q000493:pharmacokinetics* / Q000652:urine; D013997:Time Factors
D005456:Fluorescent Dyes; D013267:Stilbenes; D002563:Cerium; C023538:rhapontin
cerium probe; metabolism; pharmacokinetics; rhaponticin; spectrofluorometry