Determination of 20(S)-protopanaxadiol in human plasma by HPLC-MS/MS: application to a pharmacokinetic study

• Main Authors: Feifan Xie (Author), Sanwang Li (Author), Zeneng Cheng (Author), Xingling Liu (Author), Hong Zhang (Author), Peijiong Li (Author), Zhi Liu (Author), Xin Guo (Author), Peng Yu (Author)
• Format: Book
• Published: Elsevier, 2013-12-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.
• Notes: 2211-3835; 2211-3843; 10.1016/j.apsb.2013.10.002
• Keywords: 20(S)-Protopanaxadiol; HPLC-MS/MS; Human plasma; Pharmacokinetics; Liquid-liquid extraction; Therapeutics. Pharmacology; RM1-950
• Source: Acta Pharmaceutica Sinica B, Vol 3, Iss 6, Pp 385-391 (2013)

A rapid, specific and sensitive HPLC-MS/MS method was developed and validated for the determination of 20(S)-protopanaxadiol (PPD) in human plasma. PPD and the internal standard PD were extracted from plasma by liquid-liquid extraction with cyclohexane-methylene dichloride (2:1, v/v). The separation was performed on a HyPURIYTY C18 column using methanol-5 mM ammonium formate (90:10, v/v) as mobile phase at a flow rate of 0.35 mL/min. Mass spectrometric detection was carried out by electrospray ionization (ESI) in the positive ion mode using multiple reaction monitoring (MRM). The monitored transitions were m/z 425.4→217.2 for PPD and at m/z 461.4→425.5 for PD. The method was linear over the range 0.512-100 ng/mL with a lower limit of quantification (LLOQ) of 0.512 ng/mL. The mean extraction recovery of PPD was greater than 78.2% and no significant matrix effect was detected. The intra- and inter-day precisions were less than 10% and the biases below 4% for PPD. The validated method was applied to a three-level single-dose clinical pharmacokinetics study of 12 healthy Chinese volunteers and the main pharmacokinetic parameters of PPD were obtained.