Comparative Pharmacokinetic Profiles of Puerarin in Rat Plasma by UHPLC-MS/MS after Oral Administration of <i>Pueraria lobata</i> Extract and Pure Puerarin

Abstract

Puerarin is the main biologically active isoflavone in <i>Pueraria lobata</i> and has a wide range of biological activities. However, due to its poor water solubility and low oral bioavailability, its clinical applications are restricted. Compared with puerarin, the <i>Pueraria lobata</i> extract (PLE) has better water solubility, lower toxicity, and less side effects. In this study, the pharmacokinetics of orally administered puerarin (100 mg/kg) and PLE (763 mg/kg, equivalent to 100.0 mg/kg of puerarin) to rats was investigated by the UHPLC-MS/MS method. Results showed that when the rats were administered PLE, the area under the concentration-time curve from zero to infinity (<i>AUC</i> _<i>0-inf</i> ) dramatically increased from 219.83 ± 64.37 <i>μ</i>g h/L to 462.62 ± 51.74 <i>μ</i>g h/L (<i>p</i> < 0.01). The elimination half-time (<i>t</i> _<i>1/2</i> ) also increased from 1.60 ± 0.38 h to 12.04 ± 5.10 h (<i>p</i> < 0.01). The maximum concentration (<i>C</i> _max) of puerarin decreased from 101.64 ± 41.82 ng/mL to 48.64 ± 21.47 ng/mL (<i>p</i> < 0.01), and time to reach the maximum plasma concentration (<i>T</i> _max) of puerarin decreased from 1.46 ± 1.08 h to 0.54 ± 0.30 h (<i>p</i> < 0.01). Results indicated that the pharmacokinetics of puerarin in <i>Pueraria lobata</i> may be dramatically different from pure puerarin in the plasma of rat, and oral bioavailability of puerarin may be increased when PLE was administrated to rats.